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Importance of a biofouling-resistant phospholipid polymer to create a heparinized blood-compatible surfaceYasuhiko Iwasaki
Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University, Japan
J Biomater Sci Polym Ed 13:323-35. 2002..2-Methacryloyloxyethyl phosphorylcholine (MPC) polymers with 2-aminoethyl methacrylate (AEMA) were synthesized to immobilize heparin through ionic ..
Synthesis and characterisation of cationically modified phospholipid polymersAndrew L Lewis
Biocompatibles UK Ltd, Drug Delivery, Chapman House Farnham Business Park Weydon Lane, Farnham, Surrey GU9 8QL, UK
Biomaterials 25:3099-108. 2004Phospholipid-like copolymers based on 2-(methacryloyloxyethyl) phosphorylcholine were synthesised using monomer-starved free radical polymerisation methods and incorporating cationic charge in the form of the choline methacrylate monomer ..
Miltefosine affects lipid metabolism in Leishmania donovani promastigotesM Rakotomanga
Chimiothérapie Antiparasitaire, UMR 8076 CNRS, Faculte de Pharmacie, Universite Paris Sud XI, F 92290 Chatenay Malabry, France
Antimicrob Agents Chemother 51:1425-30. 2007....
Oral miltefosine for Indian visceral leishmaniasisShyam Sundar
Institutes of Medical Sciences, Banaras Hindu University, Varanasi, India
N Engl J Med 347:1739-46. 2002..Miltefosine may be particularly advantageous because it can be administered orally. It may also be helpful in regions where parasites are resistant to current agents...
Characterisation of Leishmania donovani promastigotes resistant to hexadecylphosphocholine (miltefosine)Karin Seifert
Department of Infectious and Tropical Diseases, London School of Hygiene and Tropical Medicine, Keppel Street, London WC1E 7HT, UK
Int J Antimicrob Agents 22:380-7. 2003..Resistance was stable up to 12 weeks in drug-free culture medium. No amplification of specific genes, including the multidrug resistance P-glycoprotein gene, could be detected in the resistant parasites...
In vitro susceptibility of field isolates of Leishmania donovani to Miltefosine and amphotericin B: correlation with sodium antimony gluconate susceptibility and implications for treatment in areas of endemicityDhiraj Kumar
Institute of Pathology, Safdarjung Hospital Campus, New Delhi, India
Antimicrob Agents Chemother 53:835-8. 2009..The results of gene expression analysis of LdMT and LdRos3 were suggestive of alternate mechanisms of Miltefosine susceptibility in the isolates...
Synergistic proapoptotic activity of recombinant TRAIL plus the Akt inhibitor Perifosine in acute myelogenous leukemia cellsPier Luigi Tazzari
Servizio di Immunoematologia e Trasfusionale, Policlinico S Orsola Malpighi, Universita di Bologna, Italy
Cancer Res 68:9394-403. 2008..In contrast, CD34(+) cells from healthy donors were resistant to perifosine and TRAIL treatment. Our findings suggest that the combination of perifosine and TRAIL might offer a novel therapeutic strategy for AML...
Inactivation of the miltefosine transporter, LdMT, causes miltefosine resistance that is conferred to the amastigote stage of Leishmania donovani and persists in vivoKarin Seifert
Department of Infectious and Tropical Diseases, London School of Hygiene and Tropical Medicine, Keppel Street, London WC1E 7HT, UK
Int J Antimicrob Agents 30:229-35. 2007..90% inhibition in wild-type infections). No cross-resistance to other antileishmanial drugs was observed in M-mutR amastigotes...
B-1 cells: the lineage question revisitedL A Herzenberg
Department of Genetics, Stanford University School of Medicine, CA 94305, USA
Immunol Rev 175:9-22. 2000....
Development of miltefosine as an oral treatment for leishmaniasisH Sindermann
Zentaris GmbH, Weismuellerstrasse 50, 60314 Frankfurt, Germany
Trans R Soc Trop Med Hyg 100:S17-20. 2006..It is therefore contraindicated for use during pregnancy, and contraception is required beyond the end of treatment in women of child-bearing age...
Pharmacokinetics of miltefosine in Old World cutaneous leishmaniasis patientsThomas P C Dorlo
Department of Pharmacy and Pharmacology, Slotervaart Hospital The Netherlands Cancer Institute, Louwesweg 6, 1066 EC, Amsterdam, The Netherlands
Antimicrob Agents Chemother 52:2855-60. 2008....
Comparison of short-course multidrug treatment with standard therapy for visceral leishmaniasis in India: an open-label, non-inferiority, randomised controlled trialShyam Sundar
Kala azar Medical Research Center, Department of Medicine, Institute of Medical Sciences, Banaras Hindu University, Varanasi, India
Lancet 377:477-86. 2011..Improved treatment approaches are needed for visceral leishmaniasis. We assessed the efficacy and safety of three potential short-course combination treatments compared with the standard monotherapy in India...
Streptococcus pneumoniae anchor to activated human cells by the receptor for platelet-activating factorD R Cundell
Laboratory of Molecular Infectious Diseases, Rockefeller University, New York, New York 10021 6399, USA
Nature 377:435-8. 1995..Only virulent pneumococci engage the PAF receptor. Attachment of the bacterial phosphorylcholine to the PAF receptor enhanced adherence, which was coupled to invasion of endothelial, epithelial and PAF-..
Possible mechanism of miltefosine-mediated death of Leishmania donovaniNavin K Verma
Department of Biotechnology, National Institute of Pharmaceutical Education and Research, Punjab, India
Antimicrob Agents Chemother 48:3010-5. 2004..Understanding of miltefosine-mediated death will facilitate the design of new therapeutic strategies against Leishmania parasites...
Sensitivities of Leishmania species to hexadecylphosphocholine (miltefosine), ET-18-OCH(3) (edelfosine) and amphotericin BPatricia Escobar
Department of Infectious and Tropical Diseases, London School of Hygiene and Tropical Medicine, Keppel Street, London WC1E 7HT, UK
Acta Trop 81:151-7. 2002..5-37.1 microM against amastigotes. Amphotericin B deoxycholate was used as the standard drug and gave submicromolar ED(50) values in all assays; L. mexicana was the least sensitive species to this drug...
Phase II study of perifosine in previously untreated patients with metastatic melanomaD Scott Ernst
London Regional Cancer Centre, 790 Commissioners Rd East, London, ON N6A 4L6, UK
Invest New Drugs 23:569-75. 2005..To assess the response rate and toxicity of the alkylphosphocholine analogue, perifosine, in patients with metastatic or recurrent malignant melanoma...
Phase 4 trial of miltefosine for the treatment of Indian visceral leishmaniasisSujit Kumar Bhattacharya
Rajendra Memorial Research Institute of Medical Sciences, Agam Kuan, India
J Infect Dis 196:591-8. 2007..Hospital-based studies have shown that oral miltefosine is a highly effective treatment for VL both in adults and in children...
Alteration of fatty acid and sterol metabolism in miltefosine-resistant Leishmania donovani promastigotes and consequences for drug-membrane interactionsM Rakotomanga
, UMR 8076 CNRS, , , F-92290, ChÄtenay-Malabry, France
Antimicrob Agents Chemother 49:2677-86. 2005..In conclusion, HePC resistance affects three lipid biochemical pathways: fatty acid elongation, the desaturase system responsible for fatty acid alkyl chain unsaturation, and the C-24-alkylation of sterols...
Mechanisms of experimental resistance of Leishmania to miltefosine: Implications for clinical useF Javier Pérez-Victoria
Instituto de Parasitologia y Biomedicina Lopez Neyra, Spanish Research Council C S I C, Technological Park of Health Sciences, Avda del Conocimiento s n, 18100 Armilla, Granada, Spain
Drug Resist Updat 9:26-39. 2006....
Perifosine inhibits multiple signaling pathways in glial progenitors and cooperates with temozolomide to arrest cell proliferation in gliomas in vivoHiroyuki Momota
Department of Cancer Biology and Genetics and Surgery (Neurosurgery) and Neurology, Memorial Sloan-Kettering Cancer Center, New York, New York 10021, USA
Cancer Res 65:7429-35. 2005..01). These results indicate that perifosine is an effective drug in gliomas in which Akt and Ras-Erk 1/2 pathways are frequently activated, and may be a new candidate for glioma treatment in the clinic...
Decoration of lipopolysaccharide with phosphorylcholine: a phase-variable characteristic of Haemophilus influenzaeJ N Weiser
Department of Pediatrics, Children s Hospital of Philadelphia, University of Pennsylvania School of Medicine, 19104 4318, USA
Infect Immun 65:943-50. 1997..Incorporated choline is in the form of phosphorylcholine (ChoP) based on the reactivity with the monoclonal antibody with specificity for this structure, TEPC-15...
Increased junctional diversity in fetal B cells results in a loss of protective anti-phosphorylcholine antibodies in adult miceC L Benedict
Department of Microbiology, University of Alabama at Birmingham, 35294 3300, USA
Immunity 10:607-17. 1999..These results show that maintenance of lower Ig diversity in early life is essential for the acquisition of a complete functional adult repertoire...
Low levels of antibodies against phosphorylcholine predict development of stroke in a population-based study from northern SwedenRoland Fiskesund
Department of Medicine, Karolinska University Hospital Huddinge, Karolinska Institutet, Stockholm, Sweden
Stroke 41:607-12. 2010Natural immunoglobulin M antibodies specific for phosphorylcholine (anti-PC) have been implicated in atherosclerosis...
Coadministration of histone deacetylase inhibitors and perifosine synergistically induces apoptosis in human leukemia cells through Akt and ERK1/2 inactivation and the generation of ceramide and reactive oxygen speciesMohamed Rahmani
Department of Medicine, Virginia Commonwealth University, School of Medicine, Richmond, VA 23298, USA
Cancer Res 65:2422-32. 2005..They also raise the possibility that combining these agents may represent a novel antileukemic strategy...
Anticancer alkylphospholipids: mechanisms of action, cellular sensitivity and resistance, and clinical prospectsWim J van Blitterswijk
Division of Cellular Biochemistry, Department of Radiotherapy, Netherlands Cancer Institute, Antoni van Leeuwenhoek Hospital, Amsterdam, The Netherlands
Curr Pharm Des 14:2061-74. 2008..For example, ALPs increase the cancer cell sensitivity to radiotherapy in vitro and in vivo. We highlight the clinical potential of perifosine, an orally available APL...
Differential role of human choline kinase alpha and beta enzymes in lipid metabolism: implications in cancer onset and treatmentDavid Gallego-Ortega
Translational Oncology Unit, CSIC UAM La Paz, Instituto de Investigaciones Biomedicas, Madrid, Spain
PLoS ONE 4:e7819. 2009..Recently ChoKalpha has been implicated in the carcinogenic process, since it is over-expressed in a variety of human cancers. However, no evidence for a role of ChoKbeta in carcinogenesis has been reported...
Changes in choline metabolism as potential biomarkers of phospholipase C{gamma}1 inhibition in human prostate cancer cellsMounia Beloueche-Babari
Cancer Research UK Clinical Magnetic Resonance Research Group, The Institute of Cancer Research and The Royal Marsden NHS Foundation Trust, Sutton, Surrey, United Kingdom
Mol Cancer Ther 8:1305-11. 2009....
Perifosine: update on a novel Akt inhibitorJoell J Gills
Medical Oncology Branch, National Cancer Institute, NNMC Building 8, Room 5101, 8901 Wisconsin Avenue, Bethesda, MD 20889, USA
Curr Oncol Rep 11:102-10. 2009..In this article, we review the clinical history of perifosine and discuss its many biologic activities...
Perifosine synergistically enhances TRAIL-induced myeloma cell apoptosis via up-regulation of death receptorsEbenezer David
Department of Hematology and Oncology, Winship Cancer Institute, Emory University School of Medicine, Atlanta, Georgia, USA
Clin Cancer Res 14:5090-8. 2008..The aim of this study is to investigate the efficacy of a novel Akt inhibitor, perifosine, in combination with tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) in human myeloma cells and primary patient samples...
The sensitivity of clinical isolates of Leishmania from Peru and Nepal to miltefosineVanessa Yardley
Department of Infectious and Tropical Diseases, London School of Hygiene and Tropical Medicine, London, United Kingdom
Am J Trop Med Hyg 73:272-5. 2005..If this model can be correlated to therapeutic outcome, it may have implications for the interpretation of clinical trials...
Treatment of New World cutaneous leishmaniasis with miltefosineJ Soto
, Calle 60 A 5-54 Suite 201, Bogot, Colombia
Trans R Soc Trop Med Hyg 100:S34-40. 2006..Miltefosine was well tolerated, and as effective as historic values of antimony for treatment of L. panamensis disease...
Phosphorylcholine on the lipopolysaccharide of Haemophilus influenzae contributes to persistence in the respiratory tract and sensitivity to serum killing mediated by C-reactive proteinJ N Weiser
Department of Pediatrics, University of Pennsylvania School of Medicine, Philadelphia, Pennsylvania 19104, USA
J Exp Med 187:631-40. 1998Haemophilus influenzae undergoes phase variation in expression of the phosphorylcholine (ChoP) epitope, a structure present on several invasive pathogens residing in the human respiratory tract...
Miltefosine treatment of Leishmania major infection: an observational study involving Dutch military personnel returning from northern AfghanistanP P A M van Thiel
Department of Internal Medicine, Division of Infectious Diseases, Tropical Medicine and AIDS and Center for Infection and Immunity, Academic Medical Center, University of Amsterdam, Amsterdam, The Netherlands
Clin Infect Dis 50:80-3. 2010..Thirty patients experienced cure after receipt of miltefosine, 3 after receipt of additional ilSb(v), and 1 after 28 daily intravenous injections of antimony. Temporary diminution of ejaculate volume was reported by 21 patients...
Miltefosine, a promising novel agent for schistosomiasis mansoniMaha M Eissa
Department of Medical Parasitology, Faculty of Medicine, Alexandria University, Alexandria, Egypt
Int J Parasitol 41:235-42. 2011..In conclusion, we believe this is the first study highlighting miltefosine as a promising novel agent for schistosomiasis mansoni...
Increased prevalence of vulnerable atherosclerotic plaques and low levels of natural IgM antibodies against phosphorylcholine in patients with systemic lupus erythematosusCristina Anania
Department of Medicine, Karolinska University Hospital, Huddinge, 141 86 Stockholm, Sweden
Arthritis Res Ther 12:R214. 2010..We recently reported a negative association between natural IgM-antibodies against phosphorylcholine (anti-PC) in the general population, high anti-PC levels leading to decreased atherosclerosis development ..
Phosphocholine and sphingosine-1-phosphate synergistically stimulate DNA synthesis by a MAP kinase-dependent mechanismZ Kiss
The Hormel Institute, University of Minnesota, Austin 55912, USA
FEBS Lett 412:197-200. 1997....
First case of typical Old World cutaneous leishmaniasis treated with miltefosineMarija Stojkovic
Section of Clinical Tropical Medicine, Heidelberg University Hospital, Heidelberg, and General Practice, Dreisamstr 11, Freiburg, Germany
Int J Dermatol 46:385-7. 2007..Ten days after completion of treatment, the rolled edge had disappeared and the central ulcer had almost healed (Fig. 3). Figure 4 shows the lesion 5 months after completion of treatment...
Proapoptotic activity and chemosensitizing effect of the novel Akt inhibitor perifosine in acute myelogenous leukemia cellsV Papa
Dipartimento di Scienze Anatomiche Umane e Fisiopatologia dell Apparato Locomotore, Universita di Bologna, Bologna, Italy
Leukemia 22:147-60. 2008..Our findings indicate that perifosine, either alone or in combination with existing drugs, might be a promising therapeutic agent for the treatment of those AML cases characterized by upregulation of the PI3K-Akt survival pathway...
Visceral leishmaniasis: elimination with existing interventionsGreg Matlashewski
Special Programme for Research and Training in Tropical Diseases, WHO, Geneva, Switzerland
Lancet Infect Dis 11:322-5. 2011....
Transition from octahedral to tetrahedral geometry causes the activation or inhibition by Znf2+ of Pseudomonas aeruginosa phosphorylcholine phosphataseLisandro H Otero
Departamento de Biologia Molecular, Universidad Nacional de Rio Cuarto, 5800 Rio Cuarto, Cordoba, Argentina
Biometals 23:307-14. 2010Pseudomonas aeruginosa phosphorylcholine phosphatase (PchP) catalyzes the hydrolysis of phosphorylcholine, which is produced by the action of hemolytic phospholipase C on phosphatidylcholine or sphyngomielin, to generate choline and ..
Quantification of the response to miltefosine treatment for visceral leishmaniasis by QT-NASBAP J de Vries
Academic Medical Center, Division of Infectious Diseases, Tropical Medicine and AIDS, Meibergdreef 9, Amsterdam, The Netherlands
Trans R Soc Trop Med Hyg 100:1183-6. 2006..QT-NASBA values declined exponentially and were negative after 6 weeks. Miltefosine plasma concentrations continued to accumulate during the 4 weeks of treatment. The terminal elimination half-life was 14.8 days...
Sphingosylphosphorylcholine inhibits melanin synthesis via pertussis toxin-sensitive MITF degradationDong Seok Kim
Department of Biochemistry, Chung Ang University College of Medicine, Seoul, Republic of Korea
J Pharm Pharmacol 62:181-7. 2010..In this study we aimed to examine sphingosylphosphorylcholine-mediated signalling pathways related to melanogenesis...
The acute-phase reactant C-reactive protein binds to phosphorylcholine-expressing Neisseria meningitidis and increases uptake by human phagocytesRosalyn Casey
Division of Microbial Sciences, Faculty of Health and Medical Sciences, University of Surrey, Stag Hill, Guildford, Surrey GU2 7XH, United Kingdom
Infect Immun 76:1298-304. 2008..has been shown to help protect the host from several bacterial pathogens, which it recognizes by binding to phosphorylcholine (PC) on their surfaces...
Anti-acanthamoeba efficacy and toxicity of miltefosine in an organotypic skin equivalentJulia Walochnik
Department of Medical Parasitology, Institute of Hygiene, Medical University of Vienna, 1095 Vienna, Austria
J Antimicrob Chemother 64:539-45. 2009..in vitro. The aim of the current study was to evaluate the suitability of miltefosine for the topical treatment of Acanthamoeba infections...
Comparison of miltefosine and meglumine antimoniate for the treatment of zoonotic cutaneous leishmaniasis (ZCL) by a randomized clinical trial in IranM Mohebali
School of Public Health and Institute of Public Health Research, Medical Sciences University of Tehran, P O Box 14155 6446, Tehran, Iran
Acta Trop 103:33-40. 2007..major in Iran, based on parasitological as well as clinical criteria two weeks, three months, and six months after end of treatment...
Miltefosine induces apoptosis-like death in Leishmania donovani promastigotesCaroline Paris
UMR 8076 CNRS, , France
Antimicrob Agents Chemother 48:852-9. 2004..Identification of the death-signaling pathways activated in HePC-sensitive parasites appears to be essential for a better understanding of the molecular mechanisms of action and resistance in these parasites...
Rationale and clinical application of alkylphospholipid analogues in combination with radiotherapyStefan R Vink
Division of Experimental Therapy Department of Radiation Oncology, The Netherlands Cancer Institute, Plesmanlaan 121, 1066 CX Amsterdam, The Netherlands
Cancer Treat Rev 33:191-202. 2007..The preclinical results on molecular targeting underlying this approach will be reviewed, concluded with first clinical data on combined treatment of radiotherapy with perifosine...
Akt inhibitors as an HIV-1 infected macrophage-specific anti-viral therapyPauline Chugh
Department of Microbiology and Immunology, School of Medicine, University of Rochester Medical Center 601 Elmwood Avenue Box 672 Rochester, New York 14742 USA
Retrovirology 5:11. 2008..Unlike CD4+ T cells, HIV-1 infected macrophages exhibit extended life span even upon stress, consistent with their in vivo role as long-lived HIV-1 reservoirs...
New treatment approach in Indian visceral leishmaniasis: single-dose liposomal amphotericin B followed by short-course oral miltefosineShyam Sundar
Kala azar Medical Research Center, Department of Medicine, Banaras Hindu University, Institute of Medical Sciences, Varanasi, India
Clin Infect Dis 47:1000-6. 2008....
Duplicate copies of lic1 direct the addition of multiple phosphocholine residues in the lipopolysaccharide of Haemophilus influenzaeKate L Fox
Molecular Infectious Diseases Group, University of Oxford Department of Paediatrics, Weatherall Institute of Molecular Medicine, John Radcliffe Hospital, Headington, Oxford, United Kingdom
Infect Immun 76:588-600. 2008..When bound, C-reactive protein leads to complement-mediated killing, indicating the potential biological significance of multiple PCho residues...
Miltefosine--discovery of the antileishmanial activity of phospholipid derivativesSimon L Croft
Drugs for Neglected Diseases Initiative DNDi, 1 Place St Gervais, CH 1201 Geneva, Switzerland
Trans R Soc Trop Med Hyg 100:S4-8. 2006..Miltefosine is active against most Leishmania species, including those that cause cutaneous disease...
Involvement of miltefosine-mediated ERK activation in glioma cell apoptosis through Fas regulationRicha Tewari
National Brain Research Centre, Manesar, Haryana, India
J Neurochem 107:616-27. 2008..Taken together, our findings suggest the involvement of ERK activation in miltefosine-induced glioma cell apoptosis...
Lem3p is essential for the uptake and potency of alkylphosphocholine drugs, edelfosine and miltefosinePamela K Hanson
Department of Physiology, Emory University School of Medicine, Atlanta, Georgia 30322, USA
J Biol Chem 278:36041-50. 2003..These data demonstrate a requirement for Lem3p expression for normal phosphatidylcholine and alkylphosphocholine drug transport across the plasma membrane of yeast...
Low levels of IgM antibodies to phosphorylcholine predict cardiovascular disease in 60-year old men: effects on uptake of oxidized LDL in macrophages as a potential mechanismUlf de Faire
Division of Cardiovascular Epidemiology, Institute of Environmental Medicine, Karolinska Institutet, S 171 77 Stockholm, Sweden
J Autoimmun 34:73-9. 2010We here determine the role of IgM antibodies against phosphorylcholine (anti-PC) in prediction of cardiovascular disease (CVD) and on macrophage uptake of Oxidized LDL (OxLDL).
In vitro combination treatment with perifosine and UCN-01 demonstrates synergism against prostate (PC-3) and lung (A549) epithelial adenocarcinoma cell linesGirija P Dasmahapatra
Clinical Trials Unit, Developmental Therapeutics Program, National Cancer Institute, Bethesda, Maryland 20892, USA
Clin Cancer Res 10:5242-52. 2004..CONCLUSIONS: As the concentrations of UCN-01 and perifosine causing synergistic inhibition of cell growth are clinically achievable without prominent toxicity, these data support the development of clinical studies with this combination...
Oral miltefosine for the treatment of Indian visceral leishmaniasisShyam Sundar
Kala azar Medical Research Center, Banaras Hindu University, Varanasi, India
Trans R Soc Trop Med Hyg 100:S26-33. 2006..5 mg/kg daily for 28 days) was established with a cure rate (94%) similar to that seen in adults. Miltefosine is the first oral antileishmanial drug with a high degree of safety and efficacy for the treatment of VL...
N-glycans of the porcine nematode parasite Ascaris suum are modified with phosphorylcholine and core fucose residuesGerald Pöltl
Department für Chemie, Universität für Bodenkultur, Vienna, Austria
FEBS J 274:714-26. 2007..parasite Ascaris suum have focused on its glycosphingolipids, which were found, in part, to be modified by phosphorylcholine. Using mass spectrometry and western blotting, we have now analyzed the peptide N-glycosidase A-released N-..
Low plasma membrane expression of the miltefosine transport complex renders Leishmania braziliensis refractory to the drugMaría P Sánchez-Cañete
Instituto de Parasitologia y Biomedicina Lopez Neyra, CSIC, Parque Tecnológico de Ciencias de la Salud, Armilla, Granada, Spain
Antimicrob Agents Chemother 53:1305-13. 2009..braziliensis might be prevalent...
Low levels of IgM antibodies against phosphorylcholine-A potential risk marker for ischemic stroke in menBeatrice G Sjöberg
Department of Medicine, Karolinska University Hospital Huddinge, Karolinska Institutet, Stockholm, Sweden
Atherosclerosis 203:528-32. 2009Natural antibodies specific for phosphorylcholine (anti-PC) have been implicated as protective factors in atherosclerosis. We herein determined the relationship between IgM anti-PC and incidence of cardiovascular disease (CVD).
Thermodynamics of phosphorylcholine and lysophosphatidylcholine binding to the major protein of bovine seminal plasma, PDC-109V Anbazhagan
School of Chemistry, University of Hyderabad, India
FEBS Lett 579:2933-8. 2005..The binding of phosphorylcholine (PrC) and lysophosphatidylcholine (Lyso-PC) with PDC-109 was investigated by monitoring the ligand-induced ..
Phosphorylcholine expression by nontypeable Haemophilus influenzae correlates with maturation of biofilm communities in vitro and in vivoWenzhou Hong
Department of Microbiology and Immunology, Wake Forest University Health Sciences, 5101A Gray Building, Medical Center Boulevard, Winston Salem, NC 27157, USA
J Bacteriol 189:8300-7. 2007..NTHI variants within biofilms have on their surfaces lipooligosaccharides containing sialic acid (NeuAc) and phosphorylcholine (PCho)...
Radiosensitization of squamous cell carcinoma by the alkylphospholipid perifosine in cell culture and xenograftsStefan R Vink
Division of Experimental Therapy and Cellular Biochemistry, The Netherlands Cancer Institute/Antoni van Leeuwenhoek Hospital, Amsterdam, The Netherlands
Clin Cancer Res 12:1615-22. 2006..These data provide strong support for further development of this combination in clinical studies...
Enzyme-degradable phosphorylcholine porous hydrogels cross-linked with polyphosphoesters for cell matricesChookaet Wachiralarpphaithoon
Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University, 2 3 10 Kanda surugadai, Chiyoda ku, Tokyo 101 0062, Japan
Biomaterials 28:984-93. 2007Biodegradable highly porous hydrogels composed of poly [2-methacryloyloxyethyl phosphorylcholine (MPC)] cross-linked with polyphosphoesters have been prepared as novel cellular matrices...
Preclinical evaluation of radiation and perifosine in a genetically and histologically accurate model of brainstem gliomaOren J Becher
Departments of Cancer Biology and Genetics, Brain Tumor Center, Memorial Sloan Kettering Cancer Center, New York, New York 10021, USA
Cancer Res 70:2548-57. 2010..92). Perifosine + 10 Gy did not result in a significantly increased survival relative to 10 Gy alone (P = 0.23). This PDGF-induced BSG model can serve as a preclinical tool for the testing of novel agents...
Using a molecular model and kinetic experiments in the presence of divalent cations to study the active site and catalysis of Pseudomonas aeruginosa phosphorylcholine phosphatasePaola R Beassoni
Departamento de Biologia Molecular, Universidad Nacional de Rio Cuarto, 5800 Rio Cuarto, Cordoba, Argentina
Biochim Biophys Acta 1784:2038-44. 2008b>Phosphorylcholine phosphatase (PchP) of Pseudomonas aeruginosa, a product of the PA5292 gene, catalyzes the hydrolysis of phosphocholine to choline and inorganic phosphate (Pi)...
A phase II study of perifosine in androgen independent prostate cancerEdwin M Posadas
Medical Oncology Clinical Research Unit, Center for Cancer Research, National Cancer Institute, Bethesda, Maryland, USA
Cancer Biol Ther 4:1133-7. 2005..No significant clinical activity against prostate cancer was observed. This agent does not merit further study in the setting of monotherapy in this population...
Crossreactivity of human anti-dsDNA antibodies to phosphorylcholine: clues to their originA Sharma
Bloomsbury Rheumatology Unit/Centre for Rheumatology, Dept of Medicine, University College London, Arthur Stanley House, London, W1P 9PG, UK
J Autoimmun 16:479-84. 2001..In particular, anti-DNA antibodies have been shown to crossreact with phosphorylcholine (PC), a dominant epitope on pneumococcal cell wall polysaccharide...
Development and validation of a quantitative assay for the measurement of miltefosine in human plasma by liquid chromatography-tandem mass spectrometryThomas P C Dorlo
Department of Pharmacy and Pharmacology, Slotervaart Hospital The Netherlands Cancer Institute, Louwesweg 6, 1066 EC Amsterdam, The Netherlands
J Chromatogr B Analyt Technol Biomed Life Sci 865:55-62. 2008..At the lowest level, the intra-assay precision was lower than 10.7%, the inter-assay precision was 10.6% and accuracies were between 95.1 and 109%. This assay is successfully used in a clinical pharmacokinetic study with miltefosine...
Site-directed mutations and kinetic studies show key residues involved in alkylammonium interactions and reveal two sites for phosphorylcholine in Pseudomonas aeruginosa phosphorylcholine phosphatasePaola R Beassoni
Departamento de Biologia Molecular, Universidad Nacional de Rio Cuarto, X5800BYA Río Cuarto, Cordoba, Argentina
Biochim Biophys Acta 1814:858-63. 2011Pseudomonas aeruginosa phosphorylcholine phosphatase (PchP) catalyzes the hydrolysis of phosphorylcholine (Pcho) to produce choline and inorganic phosphate...
Rapid development of hydrophilicity and protein adsorption resistance by polymer surfaces bearing phosphorylcholine and naphthalene groupsKoji Futamura
Department of Materials Engineering, Department of Bioengineering, School of Engineering, Center for NanoBio Integration, The University of Tokyo, 7 3 1 Hongo, Bunkyo ku, Tokyo, Japan
Langmuir 24:10340-4. 2008..protein solution under completely dry conditions, a new phospholipid copolymer, poly (2-methacryloyloxyethyl phosphorylcholine (MPC)- co-2-vinylnaphthalene (vN)) (PMvN), was synthesized...
Identification, cloning, and expression of Pseudomonas aeruginosa phosphorylcholine phosphatase geneMaria J Massimelli
Departamento de Biologia Molecular, Facultad de Ciencias Exactas, Fisicoquímicas y Naturales, Universidad Nacional de Rio Cuarto, 5800, Rio Cuarto, Cordoba, Argentina
Curr Microbiol 50:251-6. 2005Pseudomonas aeruginosa phosphorylcholine phosphatase (PChP) is a periplasmic enzyme produced simultaneously with the hemolytic phospholipase C (PLc-H) when the bacteria are grown in the presence of choline, betaine, dimethylglycine or ..
Sphingosylphosphorylcholine is a Melanogenic Stimulator for Human MelanocytesKazuhiko Higuchi
Department of Dermatology, Tokyo Women's Medical University, Tokyo, Japan
Pigment Cell Res 16:670-8. 2003..These results suggest that SPC may be a melanogenic stimulator of human melanocytes inducing the coordinated upregulated expression of various melanogenic molecules, including c-kit...
Glucantime-resistant Leishmania tropica isolated from Iranian patients with cutaneous leishmaniasis are sensitive to alternative antileishmania drugsR Hadighi
Department of Parasitology, Faculty of Medicine, Iran University of Medical Sciences, 14496, Tehran, Iran
Parasitol Res 101:1319-22. 2007..However, these resistant isolates were shown to be sensitive to miltefosine and paromomycin. The latter two drugs could thus be useful alternatives for the treatment of leishmaniasis in Iran even for SbV-resistant isolates...
Evaluation of 2-methacryloyloxyethyl phosphorylcholine polymeric nanoparticle for immunoassay of C-reactive protein detectionJongwon Park
Department of Materials Engineering, School of Engineering, The University of Tokyo, Tokyo, Japan
Anal Chem 76:2649-55. 2004To prepare novel 2-methacryloyloxyethyl phosphorylcholine (MPC)-polymeric nanoparticle (MPC-PNP), water-soluble amphiphilic phospholipid polymer, poly [MPC-co-n-butyl methacrylate (BMA)-co-p-nitrophenyloxycarbonyl poly(ethylene glycol) ..
Choline catabolism, σ⁵⁴ factor and NtrC are required for the full expression of the Pseudomonas aeruginosa phosphorylcholine phosphatase geneMaria J Massimelli
Departamento de Biologia Molecular, FCEFQN, Universidad Nacional de Rio Cuarto, Ruta 36 Km 601, 5800 Rio Cuarto, Cordoba, Argentina
Microbiol Res 166:380-90. 2011Choline favors the pathogenesis of Pseudomonas aeruginosa because hemolytic phospholipase C and phosphorylcholine phosphatase (PchP) are synthesized as a consequence of its catabolism...
How do nematodes transfer phosphorylcholine to carbohydrates?William Harnett
Strathclyde Institute of Pharmacy and Biomedical Sciences, Glasgow, UK
Trends Parasitol 26:114-8. 2010An unusual aspect of the biology of nematodes is the attachment of phosphorylcholine (PC) to carbohydrate. The attachment appears to play an important role in nematode development and, in some parasitic species, in immunomodulation...
Controlled delivery of antisense oligodeoxynucleotide from cationically modified phosphorylcholine polymer filmsZhuoQi Zhang
Biological Physics Group, School of Physics and Astronomy, The University of Manchester, Sackville Street Building, Sackville Street, Manchester M60 1QD, UK
Biomacromolecules 7:784-91. 2006..In this study, phosphorylcholine (PC) polymer films bearing different cationic charge densities were deposited onto smooth silicon substrates...
Isolation and characterization of heparin- and phosphorylcholine-binding proteins of boar and stallion seminal plasma. Primary structure of porcine pB1J J Calvete
Institut für Reproduktionsmedizin, Tierarztliche Hochschule Hannover, Hannover Kirchrode, Germany
FEBS Lett 407:201-6. 1997In the bovine, seminal plasma heparin-binding proteins bind to sperm lipids containing the phosphorylcholine group and mediate the capacitating effects of heparin-like glycosaminoglycans during sperm residence in the female genital tract...
Sphingosylphosphorylcholine-induced ERK activation inhibits melanin synthesis in human melanocytesDong Seok Kim
Research Division for Human Life Sciences, Seoul National University, 28 Yongon Dong, Chongno Gu, Seoul 110 744, South Korea
Pigment Cell Res 19:146-53. 2006..These results suggest that the ERK pathway is involved in the melanogenic signaling cascade, and that ERK activation by SPC reduces melanin synthesis via MITF downregulation...
Low level natural antibodies against phosphorylcholine: a novel risk marker and potential mechanism in atherosclerosis and cardiovascular diseaseJohan Frostegard
Department of Medicine, Karolinska University Hospital, Huddinge, Karolinska Institutet, Stockholm, Sweden
Clin Immunol 134:47-54. 2010..A common denominator is phosphorylcholine (PC), a hapten-like epitope which is exposed on OxLDL and some microorganisms...
Regeneration of functional nerves within full thickness collagen-phosphorylcholine corneal substitute implants in guinea pigsChristopher R McLaughlin
University of Ottawa Eye Institute, The Ottawa Hospital, General Campus, 501 Smyth Road, Ottawa, ONK1H 8L6, Canada
Biomaterials 31:2770-8. 2010..Porcine type I collagen and 2-methacryloyloxyethyl phosphorylcholine (MPC) were crosslinked using 1-ethyl-3-(3-dimethyl aminopropyl) carbodiimide (EDC) and N-hydroxysuccinimide (..
Collagen-phosphorylcholine interpenetrating network hydrogels as corneal substitutesWenguang Liu
Department of Cellular and Molecular Medicine, University of Ottawa, Ottawa, Ontario, Canada
Biomaterials 30:1551-9. 2009..crosslinked porcine atelocollagen, and poly(ethylene glycol) diacrylate crosslinked 2-methacryloyloxyethyl phosphorylcholine (MPC)...
Development of miltefosine for the leishmaniasesJ D Berman
National Center for Complementary and Alternative Medicine, National Institutes of Health, 6707 Democracy Blvd, Suite 401, Bethesda MD, 20892 USA
Mini Rev Med Chem 6:145-51. 2006..Miltefosine (hexadecylephosphocholine) is the first oral agent that is effective and tolerated for both visceral and cutaneous disease in several endemic regions, and represents a major advance in the treatment of these diseases...
Preparation and biophysical characterization of recombinant Pseudomonas aeruginosa phosphorylcholine phosphatasePaola R Beassoni
Departamento de Biologia Molecular, Universidad Nacional de Rio Cuarto, Rio Cuarto, Cordoba, Argentina
Protein Expr Purif 71:153-9. 2010..aeruginosa infections constitute a widespread health problem with high economical and social impact, and the phosphorylcholine phosphatase (PchP) of this bacterium is a potential target for antimicrobial treatment...
The M603 idiotype is lost in the response to phosphocholine in terminal deoxynucleotidyl transferase-deficient miceQing Sheng Mi
Laboratory of Immunology, Gerontology Research Center, National Institute on Aging, National Institutes of Health, Baltimore 21224, USA
Eur J Immunol 32:1139-46. 2002..These data indicate that production of M603-id antibody is TdT dependent, while generation of M167-id antibody is TdT independent, and that in the absence of competition from M603-like B cells, T15-id B cells can respond to PC-PM...
Construction of viscoelastic biocompatible films via the layer-by-layer assembly of hyaluronan and phosphorylcholine-modified chitosanPiotr Kujawa
Faculté de Pharmacie and Département de Chimie, Universite de Montreal, C P 6128 Succursale Centre Ville, Montreal, Quebec, Canada
Biomacromolecules 8:3169-76. 2007Films of hyaluronan (HA) and a phosphorylcholine-modified chitosan (PC-CH) were constructed by the polyelectrolyte multilayer (PEM) deposition technique and their buildup in 0...
In vitro activity of hexadecylphosphocholine (miltefosine) against metronidazole-resistant and -susceptible strains of Trichomonas vaginalisC Blaha
Department of Medical Parasitology, Clinical Institute of Hygiene and Medical Microbiology, Medical University of Vienna, Kinderspitalgasse 15, 1095 Vienna, Austria
J Antimicrob Chemother 57:273-8. 2006..Treatment of trichomonads with HePC resulted in rounding up and, at concentrations of >or=40 microM, in subsequent total lysis of the organisms. CONCLUSIONS: HePC may be a promising new candidate for the treatment of trichomoniasis...
A new class of anticancer alkylphospholipids uses lipid rafts as membrane gateways to induce apoptosis in lymphoma cellsArnold H van der Luit
Division of Cellular Biochemistry, The Netherlands Cancer Institute, Plesmanlaan 121, 1066 CX Amsterdam, The Netherlands
Mol Cancer Ther 6:2337-45. 2007..Overall, our results suggest that lipid rafts are critical membrane portals for cellular entry of alkylphospholipids depending on SMS1 activity and, therefore, are potential targets for alkylphospholipid anticancer therapy...
In vitro bactericidal activity of the antiprotozoal drug miltefosine against Streptococcus pneumoniae and other pathogenic streptococciDaniel Llull
Departamento de Microbiologia Molecular, Centro de Investigaciones Biologicas, CSIC, Ramiro de Maeztu 9, 28040 Madrid, Spain
Antimicrob Agents Chemother 51:1844-8. 2007..5 microM. Bactericidal activity was also observed in cultures of other streptococci, although these failed to undergo lysis. The autolysis elicited by miltefosine can be attributed to triggering of the pneumococcal autolysin LytA...
A phase II trial of perifosine in locally advanced, unresectable, or metastatic pancreatic adenocarcinomaRobert de W Marsh
University of Florida, Department of Medicine, Division of Hematology Oncology, Gainesville, Florida 32610 0277, USA
Am J Clin Oncol 30:26-31. 2007..Perifosine, a heterocyclic alkylphosphocholine signal transduction inhibitor, has activity against multiple cell types in vitro. This is a phase II study to determine activity and toxicity of perifosine in pancreatic adenocarcinoma...
Antibodies of IgM subclass to phosphorylcholine and oxidized LDL are protective factors for atherosclerosis in patients with hypertensionJun Su
Center of Infectious Medicine and Unit of Rheumatology, F 59 Department of Medicine, Karolinska University Hospital, Huddinge, Stockholm 141 86, Sweden
Atherosclerosis 188:160-6. 2006OBJECTIVE: To determine the importance of antibodies against phosphorylcholine (PC) and oxidized low density lipoprotein (OxLDL) for development of atherosclerosis...
Noninvasive detection of lentiviral-mediated choline kinase targeting in a human breast cancer xenograftBalaji Krishnamachary
Johns Hopkins University In Vivo Cellular Molecular Imaging Center Program, The Russell H Morgan Department of Radiology and Radiological Science, Johns Hopkins University School of Medicine, Baltimore, Maryland 21205, USA
Cancer Res 69:3464-71. 2009..This study shows the use of lentiviral vectors to target chk in a human breast cancer xenograft and noninvasive MRS detection of this targeting...
Novel biomimetic surfactant: synthesis and micellar characteristicsJian-Ping Xu
Department of Polymer Science and Engineering, Zhejiang University, Hangzhou 310027, P. R. China
Macromol Biosci 5:164-71. 2005..Novel biomimetic surfactants based on cholesterol as the hydrophobic segment and poly[2-(methacryloyloxy)ethyl phosphorylcholine] (pMPC) as the hydrophilic segment were synthesized in the present study by atom transfer radical ..
Synthesis and characterization of biocompatible thermo-responsive gelators based on ABA triblock copolymersChengming Li
Department of Chemistry, University of Sheffield, Brook Hill, Sheffield, South Yorkshire S3 7HF, United Kingdom
Biomacromolecules 6:994-9. 2005..outer A blocks comprise poly(N-isopropylacrylamide) and the central B block is poly(2-methacryloyloxyethyl phosphorylcholine) is achieved using atom transfer radical polymerization with a commercially available bifunctional initiator...
Progress in the treatment of a neglected infectious disease: visceral leishmaniasisHenry W Murray
Department of Medicine, Weill Medical College of Cornell University, 1300 York Avenue, New York, NY 10021, USA
Expert Rev Anti Infect Ther 2:279-92. 2004....
Novel biomimetic polymersomes as polymer therapeutics for drug deliveryJian-Ping Xu
Department of Polymer Science and Engineering, Zhejiang University, Hangzhou 310027, P.R. China
J Control Release 107:502-12. 2005Novel amphiphilic diblock copolymers, cholesterol-end-capped poly(2-methacryloyloxyethyl phosphorylcholine) (CMPC), which have poly(2-methacryloyloxyethyl phosphorylcholine) (poly(MPC)) as hydrophilic segment and cholesterol as ..
A new class of biochemically degradable, stimulus-responsive triblock copolymer gelatorsChengming Li
Dainton Building, Department of Chemistry, University of Sheffield, Brook Hill, Sheffield, South Yorkshire, S3 7HF, UK
Angew Chem Int Ed Engl 45:3510-3. 2006
Cell adhesion and morphology in porous scaffold based on enantiomeric poly(lactic acid) graft-type phospholipid polymersJunji Watanabe
Department of Materials Engineering, School of Engineering, The University of Tokyo, 7-3-1, Hongo, Bunkyo-ku, Tokyo 113-8656, Japan
Biomacromolecules 3:1375-83. 2002..The cytocompatible polymer was composed of 2-methacryloyloxyethyl phosphorylcholine (MPC), n-butyl methacrylate (BMA), and the enantiomeric PLLA (or PDLA) macromonomer...
Phosphorylcholine-based pH-responsive diblock copolymer micelles as drug delivery vehicles: light scattering, electron microscopy, and fluorescence experimentsCristiano Giacomelli
, LCPO-ENSCPB, , 16 Av. Pey Berland, 33607 Pessac Cedex, France
Biomacromolecules 7:817-28. 2006..of a diblock copolymer comprising a highly hydrophilic and biocompatible poly(2-methacryloyloxyethyl phosphorylcholine) (PMPC) corona-forming block and a pH-sensitive poly(2-(diisopropylamino)ethyl methacrylate) (PDPA) core-..
Synthesis and characterization of biocompatible, thermoresponsive ABC and ABA triblock copolymer gelatorsChengming Li
Department of Chemistry, Dainton Building, University of Sheffield, Brook Hill, Sheffield, South Yorkshire, S3 7HF, UK
Langmuir 21:11026-33. 2005..This is consistent with intramicelle collapse of the outer PNIPAM blocks prior to the development of the intermicelle hydrophobic interactions that are a prerequisite for macroscopic gelation...
Synthesis of biocompatible, stimuli-responsive, physical gels based on ABA triblock copolymersYinghua Ma
School of Chemistry, Physics and Environmental Science, University of Sussex, Falmer, Brighton BN1 9QJ, U.K
Biomacromolecules 4:864-8. 2003..methacrylate), DPA or 2-(diethylamino)ethyl methacrylate), DEA; B = 2-methacryloyloxyethyl phosphorylcholine, MPC] prepared using atom transfer radical polymerization dissolve in acidic solution but form biocompatible ..
Research Grants
- BACTERIAL PHOSPHORYLCHOLINE AND PATHOGENESISJeffrey Weiser; Fiscal Year: 2003..An exception to this rule is the expression of phosphorylcholine (ChoP)...
- Deregulated lipid metabolism in strokeRAO M ADIBHATLA; Fiscal Year: 2010..The long-range thrust of this research is to develop strategies to minimize disabilities due to stroke. ..
- Development of Chemical Receptors for ProteinsSanku Mallik; Fiscal Year: 2005..Testing of the synthetic receptors for possible applications in detection of metastatic cancer, imaging and delivery of anti- cancer drugs. ..
- CDP-choline: Mechanisms in Cerebral IschemiaRAO ADIBHATLA; Fiscal Year: 2006..Arachidonic acid activates neutral sphingomyelinase, resulting in membrane disintegration. PCCT activity was stimulated by exogenous CDP-choline. Aim 2 will be tested in gerbil transient forebrain ischemia. ..
- Bacterial biofilms in otitis mediaWILLIAM SWORDS; Fiscal Year: 2009..influenzae biofilms contain sialic acid and phosphorylcholine that contribute to the progression of otitis in a chinchilla middle-ear infection model system...
- Bacterial biofilms in otitis mediaWILLIAM SWORDS; Fiscal Year: 2007..influenzae biofilms contain sialic acid and phosphorylcholine that contribute to the progression of otitis in a chinchilla middle-ear infection model system...
- BIOACTIVITIES OF PNEUMOCOCCAL CELL WALL IN MENINGITISElaine I Tuomanen; Fiscal Year: 2011..blood brain barrier (CbpA on the cell wall ligates laminin receptor LR) and then penetrates into the CNS (phosphorylcholine PCho on the cell wall ligates platelet activating factor receptor PAFr) and have shown that these steps are ..
- Structure-Function Relationships of C-Reactive ProteinAlok Agrawal; Fiscal Year: 2006..These studies will provide substantial insight into the mechanisms by which this ancient protein may contribute to host defense, or alternatively, to pathogenesis of disease. ..
- GENETICS & VIRULENCE OF PNEUMOCOCCAL CAPSULAR TYPESJanet Yother; Fiscal Year: 1993....
- Genetic Control of Phospholipid Biosynthesis and Muscular DystrophyGregory Cox; Fiscal Year: 2007..The rmd mouse offers the first demonstration of a defect in a phospholipid biosynthetic enzyme causing muscular dystrophy and may reveal unique entry points in which to intervene in the disease process. ..
- Bacterial host mimicry and chronic airway infectionWILLIAM SWORDS; Fiscal Year: 2009..that share certain structural modifications, including the addition of host structures like sialic acid and phosphorylcholine. Data included in this application show that the addition of phosphorylcholine to these endotoxins decreases ..
- Genetic Control of Phospholipid Biosynthesis and Muscular DystrophyGregory A Cox; Fiscal Year: 2010..The rmd mouse offers the first demonstration of a defect in a phospholipid biosynthetic enzyme causing muscular dystrophy and may reveal unique entry points in which to intervene in the disease process. ..
- MR Based Molecular Imaging of Prostate CancerJohn Kurhanewicz; Fiscal Year: 2009....
- Control of lung permeability by oxidized phospholipidsKonstantin Birukov; Fiscal Year: 2007..Oxidation of a natural phospholipid component, 1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphorylcholine (OxPAPC) reproduces a wide spectrum of physiological effects exerted by oxidized phospholipids...
- Competition Among Bacterial Resiratory PathogensJeffrey Weiser; Fiscal Year: 2004..Both organisms express cell-surface phosphorylcholine (ChoP), an unusual bacterial structure that allows for binding to epithelial cells expressing the receptor ..
- C-Reactive Protein in Human Mucosal ImmunityJane Gould; Fiscal Year: 2005..It's function in the serum includes binding to phosphorylcholine (ChoP) on the cell wall of Streptococcus pneumoniae, which leads to activation of the complement pathway and ..
