Genomes and Genes
Experts and Doctors on enzyme inhibitors in Italy
Topic: enzyme inhibitors
Publications279 found, 100 shown here
- Matteoli G, Mazzini E, Iliev I, Mileti E, Fallarino F, Puccetti P, et al. Gut CD103+ dendritic cells express indoleamine 2,3-dioxygenase which influences T regulatory/T effector cell balance and oral tolerance induction. Gut. 2010;59:595-604 pubmed publisher..We identified a new IDO-dependent pathway leading to acquisition of tolerogenic functions in mucosal CD103-expressing DCs, indicating IDO as a possible therapeutic target for gut disorders. ..
- Ferrarini M, Ferrero E. Proteasome inhibitors and modulators of angiogenesis in multiple myeloma. Curr Med Chem. 2011;18:5185-95 pubmed..Finally, we summarize possible caveats and perspectives about antiangiogenic strategies that could be addressed to improve the efficacy of treatments for MM patients. ..
- Celetti A, Testa D, Staibano S, Merolla F, Guarino V, Castellone M, et al. Overexpression of the cytokine osteopontin identifies aggressive laryngeal squamous cell carcinomas and enhances carcinoma cell proliferation and invasiveness. Clin Cancer Res. 2005;11:8019-27 pubmed..These results identify osteopontin as a marker and a potential therapeutic target in cases of aggressive laryngeal squamous cell carcinomas. ..
- Deregibus M, Buttiglieri S, Russo S, Bussolati B, Camussi G. CD40-dependent activation of phosphatidylinositol 3-kinase/Akt pathway mediates endothelial cell survival and in vitro angiogenesis. J Biol Chem. 2003;278:18008-14 pubmed
- Muzio G, Maggiora M, Trombetta A, Martinasso G, Reffo P, Colombatto S, et al. Mechanisms involved in growth inhibition induced by clofibrate in hepatoma cells. Toxicology. 2003;187:149-59 pubmed..In light of these results, clofibrate, like conventional synthetic ligands of PPARgamma, may be regarded as a possible prototype anti-tumour drug...
- Trevisan A, Borella Venturini M, Di Marco L, Fabrello A, Giraldo M, Zanetti E, et al. Erythrocyte aminolevulinic acid dehydratase inhibition by cis-platin. Toxicol Lett. 2004;152:105-10 pubmed..This mechanism appears different from lead that prevalently inhibits ALAD removing zinc from the enzyme, other than interacting with sulfhydryl groups. ..
- Baldassarre G, Belletti B, Nicoloso M, Schiappacassi M, Vecchione A, Spessotto P, et al. p27(Kip1)-stathmin interaction influences sarcoma cell migration and invasion. Cancer Cell. 2005;7:51-63 pubmed..This study provides a functional link between proliferation and invasion of tumor cells based on diverse activities of p27(kip1) in different subcellular compartments. ..
- Krauskopf A, Eriksson O, Craigen W, Forte M, Bernardi P. Properties of the permeability transition in VDAC1(-/-) mitochondria. Biochim Biophys Acta. 2006;1757:590-5 pubmed..The labeled protein could be separated from all VDAC isoforms. While these results do not allow to exclude that VDAC is part of the PTP, they suggest that VDAC is not the target for PTP inhibition by Ro 68-3400. ..
- Bisogno T, Ortar G, Petrosino S, Morera E, Palazzo E, Nalli M, et al. Development of a potent inhibitor of 2-arachidonoylglycerol hydrolysis with antinociceptive activity in vivo. Biochim Biophys Acta. 2009;1791:53-60 pubmed publisher..p.). OMDM69 might represent a template for the development of selective and even more potent inhibitors of 2-AG hydrolysis. ..
- Ghigo A, Hirsch E. Isoform selective phosphoinositide 3-kinase gamma and delta inhibitors and their therapeutic potential. Recent Pat Inflamm Allergy Drug Discov. 2008;2:1-10 pubmed..Here, we describe recently published patent specifications disclosing new PI3K inhibitors, with a main focus on compounds displaying some selectivity for PI3Kdelta and gamma isoforms and their potential therapeutic applications. ..
- Minutoli L, Antonuccio P, Polito F, Bitto A, Squadrito F, Di Stefano V, et al. Mitogen-activated protein kinase 3/mitogen-activated protein kinase 1 activates apoptosis during testicular ischemia-reperfusion injury in a nuclear factor-kappaB-independent manner. Eur J Pharmacol. 2009;604:27-35 pubmed publisher..These findings should contribute to better understand testicular torsion-induced damage. ..
- Coletta A, Morozzo della Rocca B, Jaisankar P, Majumder H, Chillemi G, Sanna N, et al. Assignment of UV-vis spectrum of (3,3')-diindolylmethane, a Leishmania donovani topoisomerase IB inhibitor and a candidate DNA minor groove binder. J Phys Chem A. 2010;114:7121-6 pubmed publisher..The best docked DIM-DNA complexes display a binding energy pretty similar to the experimental energy and are all located in the DNA minor groove, strongly suggesting that DIM is a minor groove binder. ..
- Petrelli R, Felczak K, Cappellacci L. NMN/NaMN adenylyltransferase (NMNAT) and NAD kinase (NADK) inhibitors: chemistry and potential therapeutic applications. Curr Med Chem. 2011;18:1973-92 pubmed
- Ganassi S, Moretti A, Stornelli C, Fratello B, Pagliai A, Logrieco A, et al. Effect of Fusarium, Paecilomyces and Trichoderma formulations against aphid Schizaphis graminum. Mycopathologia. 2001;151:131-8 pubmed..As F. larvarum ITEM 2139 did not produce metabolites toxic to mammals, it might be a good candidate as a biocontrol agent of S. graminum in the field. ..
- Puliti M, von Hunolstein C, Bistoni F, Orefici G, Tissi L. Inhibition of nitric oxide synthase exacerbates group B streptococcus sepsis and arthritis in mice. Infect Immun. 2004;72:4891-4 pubmed..AG-treated mice displayed higher mortality rates and more frequent and severe arthritis than controls. Worsening of arthritis correlated with a higher number of GBS cells in the joints and local interleukin-1 beta production. ..
- Magnifico A, Albano L, Campaner S, Campiglio M, Pilotti S, Menard S, et al. Protein kinase Calpha determines HER2 fate in breast carcinoma cells with HER2 protein overexpression without gene amplification. Cancer Res. 2007;67:5308-17 pubmed..These data suggest that HER2 overexpression in HER2 2+ carcinomas is due to an accumulation of the recycled oncoprotein to the cell surface induced by activated PKCalpha. ..
- Saturnino C, Petrosino S, Ligresti A, Palladino C, De Martino G, Bisogno T, et al. Synthesis and biological evaluation of new potential inhibitors of N-acylethanolamine hydrolyzing acid amidase. Bioorg Med Chem Lett. 2010;20:1210-3 pubmed publisher..Cyclopentylhexadecanoate (13) exhibited the highest inhibitory activity on NAAA (IC(50)=10.0 microM), without inhibiting FAAH up to 50 microM. Compound 13 may become a useful template to design new NAAA inhibitors. ..
- Tundis R, Loizzo M, Menichini F. Natural products as alpha-amylase and alpha-glucosidase inhibitors and their hypoglycaemic potential in the treatment of diabetes: an update. Mini Rev Med Chem. 2010;10:315-31 pubmed..This article reviews recent data on plant extracts and isolated natural compounds that are being tested for their hypglycaemic activity, highlights ongoing research and considers the future persepctives. ..
- Angiolella L, Carradori S, Maccallini C, Giusiano G, Supuran C. Targeting Malassezia species for Novel Synthetic and Natural Antidandruff Agents. Curr Med Chem. 2017;24:2392-2412 pubmed publisher..related diseases, thus suggesting new opportunities to design innovative and alternative anti-dandruff drugs. ..
- Tod J, Hanley C, Morgan M, Rucka M, Mellows T, Lopez M, et al. Pro-migratory and TGF-β-activating functions of αvβ6 integrin in pancreatic cancer are differentially regulated via an Eps8-dependent GTPase switch. J Pathol. 2017;243:37-50 pubmed publisher..2017 The Authors. The Journal of Pathology published by John Wiley & Sons Ltd on behalf of Pathological Society of Great Britain and Ireland. ..
- Pellegrino D, Acierno R, Tota B. Control of cardiovascular function in the icefish Chionodraco hamatus: involvement of serotonin and nitric oxide. Comp Biochem Physiol A Mol Integr Physiol. 2003;134:471-80 pubmed..In contrast, SNP produced a notable relaxation of the bulbus wall with a marked increase of its stiffness, as indicated by the increase of systolic and diastolic dP/dt max (23 and 104%, respectively). ..
- Nobbio L, Sturla L, Fiorese F, Usai C, Basile G, Moreschi I, et al. P2X7-mediated increased intracellular calcium causes functional derangement in Schwann cells from rats with CMT1A neuropathy. J Biol Chem. 2009;284:23146-58 pubmed publisher..The development of P2X7 inhibitors is expected to provide a new therapeutic strategy for treatment of CMT1A neuropathy. ..
- D Angelo V, Ramaglia M, Iannotta A, Francese M, Pota E, Affinita M, et al. Influence of methylenetetrahydrofolate reductase gene polymorphisms on the outcome of pediatric patients with non-Hodgkin lymphoma treated with high-dose methotrexate. Leuk Lymphoma. 2013;54:2639-44 pubmed publisher..100%). Our data suggest a pharmacogenetic influence on the adverse effects of high-dose MTX in the 1 g/m(2) treatment group. ..
- Mazzocchi G, Rossi G, Rebuffat P, Malendowicz L, Markowska A, Nussdorfer G. Endothelins stimulate deoxyribonucleic acid synthesis and cell proliferation in rat adrenal zona glomerulosa, acting through an endothelin A receptor coupled with protein kinase C- and tyrosine kinase-dependent signaling pathways. Endocrinology. 1997;138:2333-7 pubmed
- Ricciardolo F, Rado V, Fabbri L, Sterk P, Di Maria G, Geppetti P. Bronchoconstriction induced by citric acid inhalation in guinea pigs: role of tachykinins, bradykinin, and nitric oxide. Am J Respir Crit Care Med. 1999;159:557-62 pubmed..Our study suggests a possible implication of these mechanisms in asthma associated with gastroesophageal acid reflux and a potential therapeutic role of tachykinin and bradykinin antagonists. ..
- Blanca G, Shevelev I, Ramadan K, Villani G, Spadari S, Hubscher U, et al. Human DNA polymerase lambda diverged in evolution from DNA polymerase beta toward specific Mn(++) dependence: a kinetic and thermodynamic study. Biochemistry. 2003;42:7467-76 pubmed
- Dugo L, Marzocco S, Mazzon E, Di Paola R, Genovese T, Caputi A, et al. Effects of GW274150, a novel and selective inhibitor of iNOS activity, in acute lung inflammation. Br J Pharmacol. 2004;141:979-87 pubmed..6. GW274150 may offer a novel therapeutic approach for the management of various inflammatory diseases where NO and related radicals have been postulated to play a role. ..
- Rosai J. Immunohistochemical markers of thyroid tumors: significance and diagnostic applications. Tumori. 2003;89:517-9 pubmed..At the practical level, cell type-related markers are much more useful than disease-related markers. Markers said to be of prognostic value in medullary carcinomas are calcitonin, bcl-2, and N-myc...
- Caccamo D, Campisi A, Currò M, Aguennouz M, Li Volti G, Avola R, et al. Nuclear factor-kappab activation is associated with glutamate-evoked tissue transglutaminase up-regulation in primary astrocyte cultures. J Neurosci Res. 2005;82:858-65 pubmed
- Pisani A, Martella G, Tscherter A, Costa C, Mercuri N, Bernardi G, et al. Enhanced sensitivity of DJ-1-deficient dopaminergic neurons to energy metabolism impairment: role of Na+/K+ ATPase. Neurobiol Dis. 2006;23:54-60 pubmed..These findings suggest that DJ-1 loss-of-function enhances vulnerability to energy metabolism alterations, and that nigral neurons are particularly sensitive to Na+/K+ ATPase impairment. ..
- Di Renzo F, Cappelletti G, Broccia M, Giavini E, Menegola E. Boric acid inhibits embryonic histone deacetylases: a suggested mechanism to explain boric acid-related teratogenicity. Toxicol Appl Pharmacol. 2007;220:178-85 pubmed..51 and maximum velocity by a factor beta=0.70. This work provides the first evidence for HDAC inhibition by BA and suggests such a molecular mechanism for the induction of BA-related malformations. ..
- Scarabel L, Locascio A, Furini A, Sattin M, Varotto S. Characterisation of ALS genes in the polyploid species Schoenoplectus mucronatus and implications for resistance management. Pest Manag Sci. 2010;66:337-44 pubmed publisher..At population level, the resistance pattern depends on the frequency of various resistant genotypes, and this influences the efficacy of various ALS-inhibiting herbicides. ..
- Barni S, Cabiddu M, Ghilardi M, Petrelli F. A novel perspective for an orphan problem: old and new drugs for the medical management of malignant ascites. Crit Rev Oncol Hematol. 2011;79:144-53 pubmed publisher..These agents have been developed for malignant ascites with the aim also to prolong the need for subsequent paracentesis. So patients with malignant ascites may look at the future with hope and growing optimism. ..
- Sanna F, Succu S, Melis M, Argiolas A. Dopamine agonist-induced penile erection and yawning: differential role of D?-like receptor subtypes and correlation with nitric oxide production in the paraventricular nucleus of the hypothalamus of male rats. Behav Brain Res. 2012;230:355-64 pubmed publisher..However, the stimulation of D? receptors by PD 168,077 also increases Ca²? influx/nitric oxide production leading to penile erection, but not yawning. ..
- Perotti V, Baldassari P, Bersani I, Molla A, Vegetti C, Tassi E, et al. NFATc2 is a potential therapeutic target in human melanoma. J Invest Dermatol. 2012;132:2652-60 pubmed publisher..These findings identify NFATc2 as a potential therapeutic target in melanoma. ..
- Zanassi P, Paolillo M, Schinelli S. Coexpression of phospholipase A2 isoforms in rat striatal astrocytes. Neurosci Lett. 1998;247:83-6 pubmed..These data suggest that the two PLA2 isoforms expressed in striatal astrocytes might play different roles in cellular processes mediated by astrocytes. ..
- Vincenzetti S, Cambi A, Neuhard J, Schnorr K, Grelloni M, Vita A. Cloning, expression, and purification of cytidine deaminase from Arabidopsis thaliana. Protein Expr Purif. 1999;15:8-15 pubmed..The kinetic properties of AT-CDA1 both toward the natural substrates and with analogs indicated that the catalytic mechanism of the plant enzyme is probably very similar to that of the human the E. coli enzymes. ..
- Bassi R, Anelli V, Giussani P, Tettamanti G, Viani P, Riboni L. Sphingosine-1-phosphate is released by cerebellar astrocytes in response to bFGF and induces astrocyte proliferation through Gi-protein-coupled receptors. Glia. 2006;53:621-30 pubmed..The results suggest that S1P and bFGF/S1P may play an important role in physiopathological glial proliferation, such as brain development, reactive gliosis and brain tumor formation. ..
- Aquila S, Giordano F, Guido C, Rago V, Carpino A. Nitric oxide involvement in the acrosome reaction triggered by leptin in pig sperm. Reprod Biol Endocrinol. 2011;9:133 pubmed publisher..Furthermore, the inhibitory effect of L-NAME and of Ab-ObR on the promotion of acrosome reaction triggered by leptin suggests a possible involvement of NO in the hormone action...
- Moschini E, Gualtieri M, Colombo M, Fascio U, Camatini M, Mantecca P. The modality of cell-particle interactions drives the toxicity of nanosized CuO and TiO? in human alveolar epithelial cells. Toxicol Lett. 2013;222:102-16 pubmed publisher..In conclusion, the so-called "Trojan horse" mechanism and autophagy, are involved in nCuO-induced cell death, even a further research is needed to explain the events occurring at early exposure time. ..
- Gull Y, Rasool N, Noreen M, Altaf A, Musharraf S, Zubair M, et al. Synthesis of N-(6-Arylbenzo[d]thiazole-2-acetamide Derivatives and Their Biological Activities: An Experimental and Computational Approach. Molecules. 2016;21:266 pubmed publisher..The in silico studies showed that these acetamide derivatives bind to the non-metallic active site of the urease enzyme. Structure-activity studies revealed that H-bonding of compounds with the enzyme is important for its inhibition. ..
- Di Stefano A, La Gaetana R, Bovalini L, Lusini P, Martelli P. Pertussis toxin reverses the inhibition of the adenylyl cyclase system by khellin in HeLa cells. Biochim Biophys Acta. 1996;1314:105-8 pubmed..Our results demonstrate, for the first time, that khellin is able to elicit an intracellular response by Gi alpha protein. ..
- Perilli M, Franceschini N, Bonfiglio G, Segatore B, Stefani S, Nicoletti G, et al. A kinetic study on the interaction between tazobactam (a penicillanic acid sulphone derivative) and active-site serine beta-lactamases. J Enzyme Inhib. 2000;15:1-10 pubmed..A detailed kinetic analysis permitted measurement of the acylation efficiency for some cephalosporinases and broad-spectrum beta-lactamases; the presence of a turn-over of acyl-enzyme complex was also evaluated...
- Angelucci F, Miele A, Boumis G, Brunori M, Dimastrogiovanni D, Bellelli A. Macromolecular bases of antischistosomal therapy. Curr Top Med Chem. 2011;11:2012-28 pubmed
- Beri S, Tonna N, Menozzi G, Bonaglia M, Sala C, Giorda R. DNA methylation regulates tissue-specific expression of Shank3. J Neurochem. 2007;101:1380-91 pubmed..Altogether, these data suggest the existence of a specific epigenetic control mechanism regulating SHANK3, but not SHANK1 and SHANK2, expression. ..
- Pastorello E, Farioli L, Conti A, Pravettoni V, Bonomi S, Iametti S, et al. Wheat IgE-mediated food allergy in European patients: alpha-amylase inhibitors, lipid transfer proteins and low-molecular-weight glutenins. Allergenic molecules recognized by double-blind, placebo-controlled food challenge. Int Arch Allergy Immunol. 2007;144:10-22 pubmed..The alpha-amylase inhibitor was confirmed to be the most important wheat allergen in food allergy and to play a role in wheat-dependent exercise-induced anaphylaxis, too. Other important allergens were LTP and the LMW glutenin subunits. ..
- Cuzzocrea S, Di Paola R, Genovese T, Mazzon E, Esposito E, Crisafulli C, et al. Anti-inflammatory and anti-apoptotic effects of fumonisin B1, an inhibitor of ceramide synthase, in a rodent model of splanchnic ischemia and reperfusion injury. J Pharmacol Exp Ther. 2008;327:45-57 pubmed publisher..The broader implications of our results provide a pharmacological rationale for the development of inhibitors of ceramide biosynthesis as novel therapeutics for ischemia and reperfusion-induced shock of several etiologies. ..
- Colizzi F, Perozzo R, Scapozza L, Recanatini M, Cavalli A. Single-molecule pulling simulations can discern active from inactive enzyme inhibitors. J Am Chem Soc. 2010;132:7361-71 pubmed publisher..A new compound was designed and its biological activity toward the PfFabZ enzyme predicted. Finally, the computational predictions were experimentally confirmed, highlighting the robustness of the drug design approach presented herein. ..
- Ubaldi M, Cannella N, Ciccocioppo R. Emerging targets for addiction neuropharmacology: From mechanisms to therapeutics. Prog Brain Res. 2016;224:251-84 pubmed publisher..This work is not exhaustive but rather it provides a few examples of how this research has advanced in recent years by virtue of studies carried out in our laboratory. ..
- Torcia M, De Chiara G, Nencioni L, Ammendola S, Labardi D, Lucibello M, et al. Nerve growth factor inhibits apoptosis in memory B lymphocytes via inactivation of p38 MAPK, prevention of Bcl-2 phosphorylation, and cytochrome c release. J Biol Chem. 2001;276:39027-36 pubmed..These data demonstrate that the molecular mechanisms underlying the survival factor function of NGF critically rely upon the continuous inactivation of p38 MAPK, a Bcl-2-modifying enzyme. ..
- Maestroni A, Ruggieri D, Dell Antonio G, Luzi L, Zerbini G. C-peptide increases the expression of vasopressin-activated calcium-mobilizing receptor gene through a G protein-dependent pathway. Eur J Endocrinol. 2005;152:135-41 pubmed..Further studies are needed to clarify whether VACM-1 is involved in the protective effect of C-peptide against the development of diabetic nephropathy. ..
- Oliverio S, Amendola A, Di Sano F, Farrace M, Fesus L, Nemes Z, et al. Tissue transglutaminase-dependent posttranslational modification of the retinoblastoma gene product in promonocytic cells undergoing apoptosis. Mol Cell Biol. 1997;17:6040-8 pubmed..Taken together, these data suggest that tTG, acting on the pRB protein, might play an important role in the cell progression through the death program. ..
- Sortino M, Battaglia A, Pamparana F, Carfagna N, Post C, Canonico P. Neuroprotective effects of nicergoline in immortalized neurons. Eur J Pharmacol. 1999;368:285-90 pubmed
- Atorino L, Di Meglio S, Farina B, Jones R, Quesada P. Rat germinal cells require PARP for repair of DNA damage induced by gamma-irradiation and H2O2 treatment. Eur J Cell Biol. 2001;80:222-9 pubmed..SNOG-induced SSBs were insensitive to both CAT and SOD. It is concluded that DNA in spermatocytes and spermatids is sensitive to damage by gamma-irradiation and H2O2 and that efficient repair of SSBs requires PARP activity. ..
- Marra F, Delogu W, Petrai I, Pastacaldi S, Bonacchi A, Efsen E, et al. Differential requirement of members of the MAPK family for CCL2 expression by hepatic stellate cells. Am J Physiol Gastrointest Liver Physiol. 2004;287:G18-26 pubmed..We conclude that members of the MAPK family differentially regulate cytokine-induced chemokine expression in human HSC. ..
- Pignatello R, Guccione S, Forte S, Di Giacomo C, Sorrenti V, Vicari L, et al. Lipophilic conjugates of methotrexate with short-chain alkylamino acids as DHFR inhibitors. Synthesis, biological evaluation, and molecular modeling. Bioorg Med Chem. 2004;12:2951-64 pubmed..Docking studies are in agreement with the proposed mode of interaction of these conjugates with the human DHFR. ..
- Ravasi S, Citro S, Viviani B, Capra V, Rovati G. CysLT1 receptor-induced human airway smooth muscle cells proliferation requires ROS generation, EGF receptor transactivation and ERK1/2 phosphorylation. Respir Res. 2006;7:42 pubmed..While PI3K and ROS involvement is an early event, the activation of Src occurs downstream of EGF-R activation and is followed by the classical Ras-ERK1/2 signaling pathway to control G1 progression and cell proliferation. ..
- Roviello G, Sigala S, Danesi R, Re M, Bonetta A, Cappelletti M, et al. Incidence and relative risk of adverse events of special interest in patients with castration resistant prostate cancer treated with CYP-17 inhibitors: A meta-analysis of published trials. Crit Rev Oncol Hematol. 2016;101:12-20 pubmed publisher..Strict monitoring of these side effects should be considered during CYP- 17 inhibitor therapy in prostate cancer patients. ..
- Morelli A, Chiozzi P, Chiesa A, Ferrari D, Sanz J, Falzoni S, et al. Extracellular ATP causes ROCK I-dependent bleb formation in P2X7-transfected HEK293 cells. Mol Biol Cell. 2003;14:2655-64 pubmed..These observations suggest that P2X7-dependent plasma membrane blebbing depends on the activation of the serine/threonine kinase ROCK I. ..
- Decleva E, Menegazzi R, Busetto S, Patriarca P, Dri P. Common methodology is inadequate for studies on the microbicidal activity of neutrophils. J Leukoc Biol. 2006;79:87-94 pubmed
- Mazzocchi G, Andreis P, De Caro R, Aragona F, Gottardo L, Nussdorfer G. Cerebellin enhances in vitro secretory activity of human adrenal gland. J Clin Endocrinol Metab. 1999;84:632-5 pubmed
- Falasca G, Franceschetti M, Bagni N, Altamura M, Biasi R. Polyamine biosynthesis and control of the development of functional pollen in kiwifruit. Plant Physiol Biochem. 2010;48:565-73 pubmed publisher..Gene expression preceded PA enzyme activity. The application of PA inhibitors in planta drastically reduced pollen germination. Thus, low free Spd can lead either to degeneration or loss of functionality of kiwifruit pollen grains. ..
- Madeddu P, Varoni M, Palomba D, Emanueli C, Demontis M, Glorioso N, et al. Cardiovascular phenotype of a mouse strain with disruption of bradykinin B2-receptor gene. Circulation. 1997;96:3570-8 pubmed..Dysfunction of the kallikrein-kinin system could contribute to increase blood pressure levels by leaving the activity of vasoconstrictor agents unbalanced. ..
- Maccarrone M, Piccirilli S, Battista N, Del Duca C, Nappi G, Corasaniti M, et al. Enhanced anandamide degradation is associated with neuronal apoptosis induced by the HIV-1 coat glycoprotein gp120 in the rat neocortex. J Neurochem. 2004;89:1293-300 pubmed..Taken together, these results suggest that gp120, by activating FAAH, decreases endogenous levels of AEA, and the latter effect seems instrumental in the execution of delayed neuronal apoptosis in the brain neocortex of rats. ..
- Di Pietro R, Mariggio M, Guarnieri S, Sancilio S, Giardinelli A, Di Silvestre S, et al. Tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) regulates endothelial nitric oxide synthase (eNOS) activity and its localization within the human vein endothelial cells (HUVEC) in culture. J Cell Biochem. 2006;97:782-94 pubmed
- Beretta G, Zuco V, De Cesare M, Perego P, Zaffaroni N. Namitecan: a hydrophilic camptothecin with a promising preclinical profile. Curr Med Chem. 2012;19:3488-501 pubmed..In this article, we review the relevant features of namitecan, with particular reference to its advantages compared with the two analogues (topotecan and irinotecan) approved for clinical use. ..
- Burlando B, Marchi B, Panfoli I, Viarengo A. Essential role of Ca2+ -dependent phospholipase A2 in estradiol-induced lysosome activation. Am J Physiol Cell Physiol. 2002;283:C1461-8 pubmed..This mechanism promotes lysosome fusion and catabolic activities and may mediate short-term estradiol effects. ..
- Di Santo R, Fermeglia M, Ferrone M, Paneni M, Costi R, Artico M, et al. Simple but highly effective three-dimensional chemical-feature-based pharmacophore model for diketo acid derivatives as hepatitis C virus RNA-dependent RNA polymerase inhibitors. J Med Chem. 2005;48:6304-14 pubmed..The results demonstrate that the hypothesis derived in this study can be considered to be a useful tool in designing new leads based on ADK scaffolds as HCV RdRp inhibitors. ..
- Mastrangelo E, Pezzullo M, Tarantino D, Petazzi R, Germani F, Kramer D, et al. Structure-based inhibition of Norovirus RNA-dependent RNA polymerases. J Mol Biol. 2012;419:198-210 pubmed publisher..e., Tyr41 to Ala) in hNV RdRp. Both NF023 and Suramin displayed reduced inhibitory potency versus the mutated hNV RdRp, thus hinting at a conserved inhibitor binding mode in the two polymerases. ..
- Pedrazzini E, Villa A, Longhi R, Bulbarelli A, Borgese N. Mechanism of residence of cytochrome b(5), a tail-anchored protein, in the endoplasmic reticulum. J Cell Biol. 2000;148:899-914 pubmed..These results suggest that b(5) slowly recycles between the ER and the cis-Golgi complex and that dynamic retrieval as well as retention are involved in sorting of tail-anchored proteins. ..
- Brussino L, Bucca C, Morello M, Scappaticci E, Mauro M, Rolla G. Effect on dyspnoea and hypoxaemia of inhaled N(G)-nitro-L-arginine methyl ester in hepatopulmonary syndrome. Lancet. 2003;362:43-4 pubmed..98 to 9.45 kPa). After L-NAME, the distance the patient could walk in 6 min rose by 92 m. Administration of L-NAME by aerosol might offer a new approach to treatment of hepatopulmonary syndrome. ..
- Mascarello A, Chiaradia Delatorre L, Mori M, Terenzi H, Botta B. Mycobacterium tuberculosis-Secreted Tyrosine Phosphatases as Targets Against Tuberculosis: Exploring Natural Sources in Searching for New Drugs. Curr Pharm Des. 2016;22:1561-9 pubmed
- Palmieri F, Passarella S, Stipani I, Quagliariello E. Mechanism of inhibition of the dicarboxylate carrier of mitochondria by thiol reagents. Biochim Biophys Acta. 1974;333:195-208 pubmed..As a result of this reaction these inhibitors prevent dicarboxylate binding directly and decrease the affinity for Pi by an indirect conformational change. ..
- Festuccia C, Muzi P, Gravina G, Millimaggi D, Speca S, Dolo V, et al. Tyrosine kinase inhibitor CEP-701 blocks the NTRK1/NGF receptor and limits the invasive capability of prostate cancer cells in vitro. Int J Oncol. 2007;30:193-200 pubmed..CEP-701 is a trademark of Cephalon Inc., West Chester, PA, USA. ..
- Temperini C, Winum J, Montero J, Scozzafava A, Supuran C. Carbonic anhydrase inhibitors: the X-ray crystal structure of the adduct of N-hydroxysulfamide with isozyme II explains why this new zinc binding function is effective in the design of potent inhibitors. Bioorg Med Chem Lett. 2007;17:2795-801 pubmed
- Panaro M, Acquafredda A, Cavallo P, Cianciulli A, Saponaro C, Mitolo V. Inflammatory responses in embryonal cardiomyocytes exposed to LPS challenge: an in vitro model of deciphering the effects of LPS on the heart. Curr Pharm Des. 2010;16:754-65 pubmed..The reflection of these experiments on human cardiac pathology will be discussed. ..
- Chiacchiera F, Grossi V, Cappellari M, Peserico A, Simonatto M, Germani A, et al. Blocking p38/ERK crosstalk affects colorectal cancer growth by inducing apoptosis in vitro and in preclinical mouse models. Cancer Lett. 2012;324:98-108 pubmed publisher..Current MEK1-directed pharmacological strategies could thus be exploited, in combination with p38? inhibition, to develop new approaches for CRC treatment. ..
- Franchetti P, Cappellacci L, Sheikha G, Jayaram H, Gurudutt V, Sint T, et al. Synthesis, structure, and antiproliferative activity of selenophenfurin, an inosine 5'-monophosphate dehydrogenase inhibitor analogue of selenazofurin. J Med Chem. 1997;40:1731-7 pubmed
- Rocchetti M, Besana A, Mostacciuolo G, Ferrari P, Micheletti R, Zaza A. Diverse toxicity associated with cardiac Na+/K+ pump inhibition: evaluation of electrophysiological mechanisms. J Pharmacol Exp Ther. 2003;305:765-71 pubmed..Indeed, the other differences observed concern quantitatively small effects; and 2) I(TI) suppression by PST2744 may be only partly accounted for by inhibition of the Na(+)/Ca(2+) exchanger. ..
- Riganti C, Orecchia S, Pescarmona G, Betta P, Ghigo D, Bosia A. Statins revert doxorubicin resistance via nitric oxide in malignant mesothelioma. Int J Cancer. 2006;119:17-27 pubmed..Simvastatin, Y27632 and toxin B elicited tyrosine nitration in the P-glycoprotein, thus providing a likely mechanism by which NO reverts the doxorubicin resistance in HMM cells. ..
- Capobianco M, Malucchi S, Ulisciani S, Fava C, Cambrin G, Avonto L, et al. Acute myeloid leukemia induced by mitoxantrone treatment for aggressive multiple sclerosis. Neurol Sci. 2008;29:185-7 pubmed publisher..The patient was treated by polychemotherapy and autologous bone marrow transplantation with complete recovery of t-AML and stabilization of the neurological disease. ..
- Mariani R, Maffioli S. Bacterial RNA polymerase inhibitors: an organized overview of their structure, derivatives, biological activity and current clinical development status. Curr Med Chem. 2009;16:430-54 pubmed
- Cuzzocrea S, McDonald M, Mazzon E, Siriwardena D, Calabro G, Britti D, et al. The tyrosine kinase inhibitor tyrphostin AG126 reduces the development of acute and chronic inflammation. Am J Pathol. 2000;157:145-58 pubmed
- Sparicio D, Landoni G, Pappalardo F, Crivellari M, Cerchierini E, Marino G, et al. Methylene blue for lithium-induced refractory hypotension in off-pump coronary artery bypass graft: report of two cases. J Thorac Cardiovasc Surg. 2004;127:592-3 pubmed