Experts and Doctors on humans in Kenilworth, England, United Kingdom


Locale: Kenilworth, England, United Kingdom
Topic: humans

Top Publications

  1. Baselga J, Morales S, Awada A, Blum J, Tan A, Ewertz M, et al. A phase II study of combined ridaforolimus and dalotuzumab compared with exemestane in patients with estrogen receptor-positive breast cancer. Breast Cancer Res Treat. 2017;163:535-544 pubmed publisher
    ..Therefore, the combination is not being further pursued. ..
  2. Maloney J, Berman G, Gagnon R, Bernstein D, Nelson H, Kleine Tebbe J, et al. Sequential Treatment Initiation with Timothy Grass and Ragweed Sublingual Immunotherapy Tablets Followed by Simultaneous Treatment Is Well Tolerated. J Allergy Clin Immunol Pract. 2016;4:301-9.e2 pubmed publisher
    ..In this trial, a 4-week sequential SLIT-tablet dosing schedule followed by simultaneous intake of timothy grass and ragweed tablets was well tolerated. ..
  3. Yáñez J, Wang S, Knemeyer I, Wirth M, Alton K. Intestinal lymphatic transport for drug delivery. Adv Drug Deliv Rev. 2011;63:923-42 pubmed publisher
  4. Phelps P, Anthes J, Correll C. Cloning and functional characterization of dog transient receptor potential vanilloid receptor-1 (TRPV1). Eur J Pharmacol. 2005;513:57-66 pubmed
    ..Taken together, these data constitute the first study of the cloning, expression and pharmacological characterization of dog TRPV1. ..
  5. Hodgson R, Higgins G, Guthrie D, Lu S, Pond A, Mullins D, et al. Comparison of the V1b antagonist, SSR149415, and the CRF1 antagonist, CP-154,526, in rodent models of anxiety and depression. Pharmacol Biochem Behav. 2007;86:431-40 pubmed
    ..This work demonstrates the different profiles of V1b and CRF1 receptor antagonists and supports both approaches in the treatment of affective disorders. ..
  6. Cornely O, Duarte R, Haider S, Chandrasekar P, Helfgott D, Jiménez J, et al. Phase 3 pharmacokinetics and safety study of a posaconazole tablet formulation in patients at risk for invasive fungal disease. J Antimicrob Chemother. 2016;71:718-26 pubmed publisher
  7. Chackalamannil S, Wang Y, Greenlee W, Hu Z, Xia Y, Ahn H, et al. Discovery of a novel, orally active himbacine-based thrombin receptor antagonist (SCH 530348) with potent antiplatelet activity. J Med Chem. 2008;51:3061-4 pubmed publisher
  8. Ghosal A, Yuan Y, Tong W, Su A, Gu C, Chowdhury S, et al. Characterization of human liver enzymes involved in the biotransformation of boceprevir, a hepatitis C virus protease inhibitor. Drug Metab Dispos. 2011;39:510-21 pubmed publisher
  9. Gupta S, Kantesaria B, Glue P. Pharmacokinetics, safety, and tolerability of ribavirin in hemodialysis-dependent patients. Eur J Clin Pharmacol. 2012;68:415-8 pubmed publisher
    ..4% of the dose. Ribavirin hemodialysis clearance (CLhd = 74.5 ml/min) represented approximately 50% of the renal clearance (CLr) measured in subjects with normal renal function (CLr = 129 ml/min). ..

More Information

Publications168 found, 100 shown here

  1. Wang S, He C, Maguire M, Clemmons A, Burrier R, Guzzi M, et al. Genomic organization and functional characterization of the mouse GalR1 galanin receptor. FEBS Lett. 1997;411:225-30 pubmed
    ..Functional analysis of the encoded cDNA revealed active ligand binding and intracellular signaling. The expression is detected in brain, spinal cord, heart and skeletal muscle. ..
  2. Wu B, Li Y, Ong K, Sun Y, Shrestha S, Hou L, et al. Reduction of In-Stent Restenosis by Cholesteryl Ester Transfer Protein Inhibition. Arterioscler Thromb Vasc Biol. 2017;37:2333-2341 pubmed publisher
  3. Krishna G, Sansone Parsons A, Martinho M, Kantesaria B, Pedicone L. Posaconazole plasma concentrations in juvenile patients with invasive fungal infection. Antimicrob Agents Chemother. 2007;51:812-8 pubmed
    ..In conclusion, posaconazole concentrations in plasma were similar for juvenile and adult patients, suggesting that clinical outcomes are expected to be similar in adults and children with refractory invasive fungal infection. ..
  4. Basso A, Doll R. Inhibition of cyclin-dependent kinases - a review of the recent patent literature. Recent Pat Anticancer Drug Discov. 2006;1:357-67 pubmed
    ..This review discusses the rationale for inhibiting Cdks as an approach to cancer therapy and the status of Cdk inhibitors in clinical trials. Compounds resulting from a patent literature search from 2003 to July, 2005 are discussed. ..
  5. Basso A, Liu M, Dai C, Gray K, Nale L, Tevar S, et al. SCH 2047069, a novel oral kinesin spindle protein inhibitor, shows single-agent antitumor activity and enhances the efficacy of chemotherapeutics. Mol Cancer Ther. 2010;9:2993-3002 pubmed publisher
    ..SCH 2047069 showed antitumor activity in a variety of preclinical models as a single agent and in combination with paclitaxel, gemcitabine, or vincristine. ..
  6. Nicoll Griffith D. Use of cysteine-reactive small molecules in drug discovery for trypanosomal disease. Expert Opin Drug Discov. 2012;7:353-66 pubmed publisher
  7. Elbasha E, Chhatwal J. Myths and Misconceptions of Within-Cycle Correction: A Guide for Modelers and Decision Makers. Pharmacoeconomics. 2016;34:13-22 pubmed publisher
    ..We also demonstrate that both the trapezoidal and Simpson's rules can easily be implemented in commonly used software. ..
  8. Krishna G, Ma L, Prasad P, Moton A, Martinho M, O Mara E. Effect of posaconazole on the pharmacokinetics of simvastatin and midazolam in healthy volunteers. Expert Opin Drug Metab Toxicol. 2012;8:1-10 pubmed publisher
    ..Other statins, whose metabolism/elimination is not affected by CYP3A4 inhibition, should be considered for co-administration. ..
  9. McComas C, Palani A, Chang W, Holloway M, Lesburg C, Li P, et al. Development of a New Structural Class of Broadly Acting HCV Non-Nucleoside Inhibitors Leading to the Discovery of MK-8876. ChemMedChem. 2017;12:1436-1448 pubmed publisher
  10. Krishna G, Sansone Parsons A, Kantesaria B. Drug interaction assessment following concomitant administration of posaconazole and phenytoin in healthy men. Curr Med Res Opin. 2007;23:1415-22 pubmed
  11. Mann P, McNicholas P, Chau A, Patel R, Mendrick C, Ullmann A, et al. Impact of antifungal prophylaxis on colonization and azole susceptibility of Candida species. Antimicrob Agents Chemother. 2009;53:5026-34 pubmed publisher
    ..Overall breakthrough infections by Candida species were very rare (approximately 1%), and C. glabrata was the colonizing species that was the most frequently associated with breakthrough infections. ..
  12. Chien A, Cockerill A, Fancourt C, Schmidt E, Moasser M, Rugo H, et al. A phase 1b study of the Akt-inhibitor MK-2206 in combination with weekly paclitaxel and trastuzumab in patients with advanced HER2-amplified solid tumor malignancies. Breast Cancer Res Treat. 2016;155:521-30 pubmed publisher
    ..Preliminary data indicate significant clinical activity in patients with HER2+ tumors despite prior HER2-directed therapy. ..
  13. Sun H, Palcza J, Card D, Gipson A, Rosenberg R, Kryger M, et al. Effects of Suvorexant, an Orexin Receptor Antagonist, on Respiration during Sleep In Patients with Obstructive Sleep Apnea. J Clin Sleep Med. 2016;12:9-17 pubmed publisher
    ..Due to inter- and intra-individual variability in respiratory effects, suvorexant should be used with caution in patients with compromised respiratory function, and at the lowest effective dose., NCT01300455. ..
  14. Cosman F, Gilchrist N, McClung M, Foldes J, de Villiers T, Santora A, et al. A phase 2 study of MK-5442, a calcium-sensing receptor antagonist, in postmenopausal women with osteoporosis after long-term use of oral bisphosphonates. Osteoporos Int. 2016;27:377-86 pubmed publisher
    ..Switching from ALN to MK-5442 resulted in a pulsatile increase in PTH and increases in BTMs, but a decline in BMD compared with continued ALN. MK-5442 is not a viable option for the treatment of osteoporosis. ..
  15. Bautista O, Luxembourg A. Deconstructing the measure of vaccine efficacy against disease irrespective of HPV in HPV vaccine clinical trials. Contemp Clin Trials. 2016;47:254-8 pubmed publisher
    ..Without such understanding, comparing studies and drawing conclusions from such comparison are highly misleading. Approaches are proposed to divide this endpoint in components that are easier to interpret. ..
  16. Li X, Brown N, Chau A, Lopez Ribot J, Ruesga M, Quindos G, et al. Changes in susceptibility to posaconazole in clinical isolates of Candida albicans. J Antimicrob Chemother. 2004;53:74-80 pubmed
    ..Multiple mutations in ERG11 are required to confer decreased susceptibility to posaconazole. ..
  17. Sabatelli F, Patel R, Mann P, Mendrick C, Norris C, Hare R, et al. In vitro activities of posaconazole, fluconazole, itraconazole, voriconazole, and amphotericin B against a large collection of clinically important molds and yeasts. Antimicrob Agents Chemother. 2006;50:2009-15 pubmed
    ..Posaconazole exhibited potent antifungal activity against a wide variety of clinically important fungal pathogens and was frequently more active than other azoles and amphotericin B. ..
  18. Krishna G, Parsons A, Kantesaria B, Mant T. Evaluation of the pharmacokinetics of posaconazole and rifabutin following co-administration to healthy men. Curr Med Res Opin. 2007;23:545-52 pubmed
  19. Aki C, Chao J, Ferreira J, Dwyer M, Yu Y, Chao J, et al. Diaminocyclobutenediones as potent and orally bioavailable CXCR2 receptor antagonists: SAR in the phenolic amide region. Bioorg Med Chem Lett. 2009;19:4446-9 pubmed publisher
  20. Tang H, Mayersohn M. Controversies in allometric scaling for predicting human drug clearance: an historical problem and reflections on what works and what does not. Curr Top Med Chem. 2011;11:340-50 pubmed
  21. Cumming J, Smith E, Wang L, Misiaszek J, Durkin J, Pan J, et al. Structure based design of iminohydantoin BACE1 inhibitors: identification of an orally available, centrally active BACE1 inhibitor. Bioorg Med Chem Lett. 2012;22:2444-9 pubmed publisher
    ..Herein we report SAR development in the S3 and F' subsites of BACE1 for this series, the synthetic approaches employed in this effort, and in vivo data for the optimized compound. ..
  22. Rothofsky M, Lin S. CROC-1 encodes a protein which mediates transcriptional activation of the human FOS promoter. Gene. 1997;195:141-9 pubmed
    ..Results suggest that CROC-1 participates in intracellular signalling pathways involved in induction of the human FOS promoter. ..
  23. Banfield C, Gupta S, Marino M, Lim J, Affrime M. Grapefruit juice reduces the oral bioavailability of fexofenadine but not desloratadine. Clin Pharmacokinet. 2002;41:311-8 pubmed
    ..The bioavailability of drugs that do not undergo significant intestinal or hepatic metabolism, such as fexofenadine, may be altered when administered with agents that influence drug transport mechanisms. ..
  24. Anthes J, Chapman R, Richard C, Eckel S, Corboz M, Hey J, et al. SCH 206272: a potent, orally active tachykinin NK(1), NK(2), and NK(3) receptor antagonist. Eur J Pharmacol. 2002;450:191-202 pubmed
    ..This compound may have beneficial effects in diseases thought to be mediated by tachykinins, such as cough, asthma, and chronic obstructive pulmonary disease. ..
  25. Song X, Zhang J, Chen X, Palyha O, Chung C, Sonatore L, et al. Identification of DGAT2 Inhibitors Using Mass Spectrometry. J Biomol Screen. 2016;21:117-26 pubmed publisher
    ..Additional profiling of one chemotype in particular identified two promising reversible and selective compounds (compound 15 and compound 16) that effectively inhibit TG production in mouse primary hepatocytes. ..
  26. Garland S, Cheung T, McNeill S, Petersen L, Romaguera J, Vazquez Narvaez J, et al. Safety and immunogenicity of a 9-valent HPV vaccine in females 12-26 years of age who previously received the quadrivalent HPV vaccine. Vaccine. 2015;33:6855-64 pubmed publisher
  27. Hussain M, Fantuzzo R, Mercorelli S, Cullen C. A direct droplet digital PCR method for quantification of residual DNA in protein drugs produced in yeast cells. J Pharm Biomed Anal. 2016;123:128-31 pubmed publisher
    ..This method simplifies the residual DNA quantification protocol by eliminating DNA extraction or protease digestion and eliminates use of DNA standards in day-to-day running of the method. ..
  28. Corman S, Elbasha E, Michalopoulos S, Nwankwo C. Cost-Utility of Elbasvir/Grazoprevir in Patients with Chronic Hepatitis C Genotype 1 Infection. Value Health. 2017;20:1110-1120 pubmed publisher
    ..Compared with other oral direct-acting antiviral agents, EBR/GZR ± RBV was the economically dominant regimen for treating GT1a noncirrhotic and GT1b TN cirrhotic patients, and was cost saving in all other populations. ..
  29. Wang P, Wu P, Egan R, Billah M. Human phosphodiesterase 8A splice variants: cloning, gene organization, and tissue distribution. Gene. 2001;280:183-94 pubmed
    ..Compared to PDE8A1, PDE8As 2-5 appear to be expressed in much lower abundance. Among various tissues and organs, PDE8A1 and PDE8A2 are expressed at various levels. ..
  30. Alley E, Lopez J, Santoro A, Morosky A, Saraf S, Piperdi B, et al. Clinical safety and activity of pembrolizumab in patients with malignant pleural mesothelioma (KEYNOTE-028): preliminary results from a non-randomised, open-label, phase 1b trial. Lancet Oncol. 2017;18:623-630 pubmed publisher
    ..Response durability and efficacy in this patient population warrants further investigation. Merck. ..
  31. Shah U. GPR119 agonists: a promising new approach for the treatment of type 2 diabetes and related metabolic disorders. Curr Opin Drug Discov Devel. 2009;12:519-32 pubmed
    ..In addition, an overview of the recent progress made in the discovery of orally active GPR119 agonists is provided. ..
  32. Chandorkar G, Zhan Q, Donovan J, Rege S, Patino H. Pharmacokinetics of surotomycin from phase 1 single and multiple ascending dose studies in healthy volunteers. BMC Pharmacol Toxicol. 2017;18:24 pubmed publisher
    ..Results of these phase 1 studies support the continued clinical development of surotomycin for the treatment of Clostridium difficile-associated diarrhea. NCT02835118 and NCT02835105 . Retrospectively registered, July 13 2016. ..
  33. Tong L, Kim S, Rosner K, Yu W, Shankar B, Chen L, et al. Fused bi-heteroaryl substituted hydantoin compounds as TACE inhibitors. Bioorg Med Chem Lett. 2017;27:3037-3042 pubmed publisher
  34. Ho G, Yang S, Smotryski J, Bercovici A, Nechuta T, Smith E, et al. The discovery of potent, selective, and orally active pyrazoloquinolines as PDE10A inhibitors for the treatment of Schizophrenia. Bioorg Med Chem Lett. 2012;22:1019-22 pubmed publisher
    ..Compound 27 inhibits MK-801 induced hyperactivity at 3mg/kg with an ED(50) of 4mg/kg and displays a ?6-fold separation between the ED(50) for inhibition of MK-801 induced hyperactivity and hypolocomotion in rats. ..
  35. Jaime Ramirez A, McMichael E, Kondadasula S, Skinner C, Mundy Bosse B, Luedke E, et al. NK Cell-Mediated Antitumor Effects of a Folate-Conjugated Immunoglobulin Are Enhanced by Cytokines. Cancer Immunol Res. 2016;4:323-336 pubmed publisher
  36. Cheng K, Gupta S, Wang H, Uss A, Njoroge G, Hughes E. Current drug discovery strategies for treatment of hepatitis C virus infection. J Pharm Pharmacol. 2011;63:883-92 pubmed publisher
    ..Additional issues, including genotype coverage, resistant mutations, and combination therapy represent major challenges for future drug discovery efforts. ..
  37. Deng Y, Shipps G, Zhao L, Siddiqui M, Popovici Muller J, Curran P, et al. Modulating the interaction between CDK2 and cyclin A with a quinoline-based inhibitor. Bioorg Med Chem Lett. 2014;24:199-203 pubmed publisher
    ..Through a series of chemical modifications the affinity (Kd) of the original hit improved from 1 to 0.005?M. ..
  38. Kosoglou T, Salfi M, Lim J, Batra V, Cayen M, Affrime M. Evaluation of the pharmacokinetics and electrocardiographic pharmacodynamics of loratadine with concomitant administration of ketoconazole or cimetidine. Br J Clin Pharmacol. 2000;50:581-9 pubmed
    ..It is concluded that, although there was a significant pharmacokinetic drug interaction between ketoconazole or cimetidine and loratadine, this effect was not accompanied by a change in the QTc interval in healthy adult volunteers. ..
  39. Ma S, Subramanian R, Xu Y, Schrag M, Shou M. Structural characterization of novel adenine dinucleotide phosphate conjugates of imatinib in incubations with rat and human liver microsomes. Drug Metab Dispos. 2008;36:2414-8 pubmed publisher
    ..Imatinib-ADP+ adducts have been observed only in in vitro studies to date. The physiological role of these adducts is not clear, nor is their in vivo relevance...
  40. Weiss T, Zhang D, Borse N, Walter E. Initiation & completion rates of hepatitis A vaccination among US pediatric populations born between 2005 and 2009. Vaccine. 2015;33:6871-7 pubmed publisher
    ..It is important for providers to identify every opportunity for hepatitis A vaccination and to assure that children get protection from this vaccine-preventable disease. ..
  41. Oehninger S, Nelson S, Verweij P, Stegmann B. Predictive factors for ovarian response in a corifollitropin alfa/GnRH antagonist protocol for controlled ovarian stimulation in IVF/ICSI cycles. Reprod Biol Endocrinol. 2015;13:117 pubmed publisher
    ..NCT01144416 , Protocol P06029. ..
  42. Kullar R, Sakoulas G, Deresinski S, van Hal S. When sepsis persists: a review of MRSA bacteraemia salvage therapy. J Antimicrob Chemother. 2016;71:576-86 pubmed publisher
    ..We recommend that combination antibiotic therapy be considered for use in MRSAB salvage treatment. ..
  43. Chackalamannil S, Doller D, McQuade R, Ruperto V. Himbacine analogs as muscarinic receptor antagonists--effects of tether and heterocyclic variations. Bioorg Med Chem Lett. 2004;14:3967-70 pubmed
    ..The structural and stereochemical requirements of the heterocyclic unit for muscarinic binding are discussed in the light of these data. ..
  44. Ogawa Y, Ogura M, Tobinai K, Ando K, Suzuki T, Watanabe T, et al. A phase I study of vorinostat combined with bortezomib in Japanese patients with relapsed or refractory multiple myeloma. Int J Hematol. 2016;103:25-33 pubmed publisher
    ..Vorinostat 400 mg plus bortezomib 1.3 mg/m(2) was safe and well-tolerated in Japanese patients with relapsed or refractory MM not considered bortezomib refractory (NCT00858234). ..
  45. Graham T. Prolylcarboxypeptidase (PrCP) inhibitors and the therapeutic uses thereof: a patent review. Expert Opin Ther Pat. 2017;27:1077-1088 pubmed publisher
    ..Additional fundamental research into the signaling pathways is likely required before the true therapeutic potential of PrCP inhibition will be realized. ..
  46. Zhang Q, Qiu P, Arreaza M, Simon J, Golovko A, Laverty M, et al. P518/Qrfp sequence polymorphisms in SAMP6 osteopenic mouse. Genomics. 2007;90:629-35 pubmed
    ..Tissue distribution of human, mouse, and rat P518/Qrfp and its receptors showed expression in bone and spinal cord. A direct role for P518/Qrfp function in maintaining bone mineral density is suggested. ..
  47. Zhu H, Cooper A, Desai J, Njoroge G, Kirschmeier P, Bishop W, et al. Discovery of C-imidazole azaheptapyridine FPT inhibitors. Bioorg Med Chem Lett. 2010;20:1134-6 pubmed publisher
    ..This series also has reduced hERG activity versus previous N-linked imidazole series. X-ray of compound 10a bound to FTase revealed strong interaction between bridgehead imidazole 3N with catalytic zinc atom. ..
  48. Heppner D, Kemp T, Martin B, Ramsey W, Nichols R, Dasen E, et al. Safety and immunogenicity of the rVSV?G-ZEBOV-GP Ebola virus vaccine candidate in healthy adults: a phase 1b randomised, multicentre, double-blind, placebo-controlled, dose-response study. Lancet Infect Dis. 2017;17:854-866 pubmed publisher
    ..The immunogenicity results support selection of the 2?×?107 PFU dose. Biomedical Advanced Research and Development Authority, US Department of Health and Human Services. ..
  49. Gonsiorek W, Fan X, Hesk D, Fossetta J, Qiu H, Jakway J, et al. Pharmacological characterization of Sch527123, a potent allosteric CXCR1/CXCR2 antagonist. J Pharmacol Exp Ther. 2007;322:477-85 pubmed
    ..049 +/- 0.004 nM). Taken together, our data show that Sch527123 represents a novel, potent, and specific CXCR2 antagonist with potential therapeutic utility in a variety of inflammatory conditions. ..
  50. Parker E, van Heek M, Stamford A. Neuropeptide Y receptors as targets for anti-obesity drug development: perspective and current status. Eur J Pharmacol. 2002;440:173-87 pubmed
  51. Cheng K, Li C, Hsieh Y, Montgomery D, Liu T, White R. Development of a high-throughput in vitro assay using a novel Caco-2/rat hepatocyte system for the prediction of oral plasma area under the concentration versus time curve (AUC) in rats. J Pharmacol Toxicol Methods. 2006;53:215-8 pubmed
    ..The results presented in this study suggest that the Caco-2/rat hepatocyte system may be used as a high-throughput screen in drug discovery for pharmacokinetic behaviors of compounds in rats. ..
  52. Wang W, Prosise W, Chen J, Taremi S, Le H, Madison V, et al. Construction and characterization of a fully active PXR/SRC-1 tethered protein with increased stability. Protein Eng Des Sel. 2008;21:425-33 pubmed publisher
  53. Liu R, Tewari M, Kong R, Zhang R, Ingravallo P, Ralston R. A peptide derived from hepatitis C virus E2 envelope protein inhibits a post-binding step in HCV entry. Antiviral Res. 2010;86:172-9 pubmed publisher
    ..These data suggest that interactions involving the C terminal region of E2 may play an important role in the HCV entry process. ..
  54. O Mara E, Kasserra C, Huddlestone J, Wan Y, Soni P, Caceres M, et al. Effect of vicriviroc on the QT/corrected QT interval and central nervous system in healthy subjects. Antimicrob Agents Chemother. 2010;54:2448-54 pubmed publisher
  55. Wickwire E, Williams S, Roth T, Capaldi V, Jaffe M, Moline M, et al. Sleep, Sleep Disorders, and Mild Traumatic Brain Injury. What We Know and What We Need to Know: Findings from a National Working Group. Neurotherapeutics. 2016;13:403-17 pubmed publisher
    ..Next, essential empirical and clinical questions and knowledge gaps are addressed. Finally, actionable recommendations are offered to guide active and efficient collaboration between academic, industry, and governmental stakeholders. ..
  56. Cumming J, Le T, Babu S, Carroll C, Chen X, Favreau L, et al. Rational design of novel, potent piperazinone and imidazolidinone BACE1 inhibitors. Bioorg Med Chem Lett. 2008;18:3236-41 pubmed publisher
    ..The key feature of both series is a cyclic amine motif specifically crafted to achieve interactions with both the flap and with the S2' pocket. ..
  57. Berlin M. Recent advances in the development of novel glucocorticoid receptor modulators. Expert Opin Ther Pat. 2010;20:855-73 pubmed publisher
  58. Sharman Moser S, Yu J, Goldshtein I, Ish Shalom S, Rouach V, Shalev V, et al. Cost and Consequences of Nonadherence With Oral Bisphosphonate Therapy: Findings From a Real-World Data Analysis. Ann Pharmacother. 2016;50:262-9 pubmed publisher
    ..002). In patients 75 years and older, nonadherence with oral bisphosphonates can be associated with significantly greater short-term risk of osteoporotic fractures and higher utilization of health care services. ..
  59. Chang M, Chang M, Reed J, Milward D, Xu J, Cornell W. Developing timely insights into comparative effectiveness research with a text-mining pipeline. Drug Discov Today. 2016;21:473-80 pubmed publisher
    ..The timely information alerts generated by this system provide the earliest and most complete picture of emerging clinical research. ..
  60. Chao J, Taveras A, Chao J, Aki C, Dwyer M, Yu Y, et al. C(4)-alkyl substituted furanyl cyclobutenediones as potent, orally bioavailable CXCR2 and CXCR1 receptor antagonists. Bioorg Med Chem Lett. 2007;17:3778-83 pubmed
    ..5 nM, CXCR1 IC(50)=37 nM). In addition, 16 has shown good oral pharmacokinetic profiles in rat, mouse, monkey, and dog. ..
  61. McBriar M. Melanin concentrating hormone receptor antagonists as antiobesity agents: from M2 to MCHR-1. Curr Top Med Chem. 2007;7:1440-54 pubmed
    ..Several challenges such as selectivity over other receptors, toxicity of a potential metabolite and determining receptor occupancy via a medium throughput assay will be reviewed. ..
  62. Hsieh Y, Cheng K, Wang Y, Chackalamannil S, Xia Y, Korfmacher W, et al. The role of exploratory drug metabolism and pharmacokinetics in new drug research: case study-selection of a thrombin receptor antagonist for development. Curr Pharm Des. 2009;15:2262-9 pubmed
    ..This screening paradigm followed by the extensive lead optimization process culminated in the selection of SCH 530348, a potent, selective and orally active thrombin receptor antagonist for the treatment of thrombosis. ..
  63. Chavez Eng C, Lutz R, Li H, Goykhman D, Bateman K, Woolf E. Quantitation of anacetrapib, stable-isotope labeled-anacetrapib (microdose), and four metabolites in human plasma using liquid chromatography tandem mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci. 2016;1011:204-14 pubmed publisher
    ..1% formic acid (A) and acetonitrile with 0.1% formic acid (B). The assays were utilized to support a clinical study in which a microdosing approach was used to determine the pharmacokinetics of anacetrapib and its metabolites. ..
  64. Anthes J, Gilchrest H, Richard C, Eckel S, Hesk D, West R, et al. Biochemical characterization of desloratadine, a potent antagonist of the human histamine H(1) receptor. Eur J Pharmacol. 2002;449:229-37 pubmed
    ..The mechanism of desloratadine antagonism of the human histamine H(1) receptor may help to explain the high potency and 24-h duration of action observed in clinical studies. ..
  65. Wan Y, Jakway J, Qiu H, Shah H, Garlisi C, Tian F, et al. Identification of full, partial and inverse CC chemokine receptor 3 agonists using [35S]GTPgammaS binding. Eur J Pharmacol. 2002;456:1-10 pubmed
  66. Brown W, Foody J, Zieve F, Tomassini J, Shah A, Tershakovec A. Inverse relationship between high-density lipoprotein cholesterol raising and high-sensitivity C-reactive protein reduction in older patients treated with lipid-lowering therapy. J Clin Lipidol. 2016;10:116-23 pubmed publisher
    ..HDL-C was inversely and consistently correlated with baseline and 12-week on-treatment hsCRP and with therapy-induced changes in HDL-C and hsCRP. ..
  67. Krishna G, Moton A, Ma L, Martinho M, Seiberling M, McLeod J. Effects of oral posaconazole on the pharmacokinetics of atazanavir alone and with ritonavir or with efavirenz in healthy adult volunteers. J Acquir Immune Defic Syndr. 2009;51:437-44 pubmed
    ..In addition, because of decreased posaconazole exposure, coadministration with efavirenz should be avoided unless the benefit to patients outweighs the risk. ..
  68. Shah V, Castro Perez J, McLaren D, Herath K, Previs S, Roddy T. Enhanced data-independent analysis of lipids using ion mobility-TOFMSE to unravel quantitative and qualitative information in human plasma. Rapid Commun Mass Spectrom. 2013;27:2195-200 pubmed publisher
  69. Niu X, Umland S, Ingram R, Beyer B, Liu Y, Sun J, et al. IK682, a tight binding inhibitor of TACE. Arch Biochem Biophys. 2006;451:43-50 pubmed
    ..The conformational changes of TACE may contribute significantly to the high affinity binding as a result of a more stable TACE-inhibitor complex. ..
  70. Zhao J, Liu Y, Reichert P, Pflanz S, Pramanik B. Glycosylation analysis of interleukin-23 receptor: elucidation of glycosylation sites and characterization of attached glycan structures. J Mass Spectrom. 2010;45:1416-25 pubmed publisher
    ..High mannose and hybrid type glycans were only observed on Asn157. The structural characterization on IL-23r glycosylation provides useful information for better understanding of the biological function of IL-23r. ..
  71. McNicholas P, Mann P, Wojcik L, Qiu P, Lee E, McCarthy M, et al. Mapping and characterization of vicriviroc resistance mutations from HIV-1 isolated from treatment-experienced subjects enrolled in a phase II study (VICTOR-E1). J Acquir Immune Defic Syndr. 2011;56:222-9 pubmed publisher
    ..These data suggest that genotypic tests for VCV susceptibility may require larger training sets and additional information beyond V3 sequences. ..
  72. Amin M, Minton S, LoRusso P, Krishnamurthi S, Pickett C, Lunceford J, et al. A phase I study of MK-5108, an oral aurora a kinase inhibitor, administered both as monotherapy and in combination with docetaxel, in patients with advanced or refractory solid tumors. Invest New Drugs. 2016;34:84-95 pubmed publisher
    ..The MTD for MK-5108 + docetaxel (CT) was established at 300 mg/day, below the exposure target. Use of pharmacodynamic gene expression assays to determine target engagement was validated. ..
  73. Nunes A, Yang J, Radican L, Engel S, Kurtyka K, Tunceli K, et al. Assessing occurrence of hypoglycemia and its severity from electronic health records of patients with type 2 diabetes mellitus. Diabetes Res Clin Pract. 2016;121:192-203 pubmed publisher
    ..The structured data and clinical notes are complementary within the EHR, and both need to be considered in order to fully assess the occurrence of hypoglycemia. ..
  74. Korfmacher W. Principles and applications of LC-MS in new drug discovery. Drug Discov Today. 2005;10:1357-67 pubmed
    ..The strategies for optimizing the use of this technique and also the potential problems and how to avoid them will be highlighted. ..
  75. Duong L, Leung A, Langdahl B. Cathepsin K Inhibition: A New Mechanism for the Treatment of Osteoporosis. Calcif Tissue Int. 2016;98:381-97 pubmed publisher
    ..ODN is currently in a worldwide Phase 3 fracture outcome trial for the treatment of postmenopausal osteoporosis with interim results supporting its anti-fracture efficacy at the spine, hip and non-vertebral sites. ..
  76. Ogert R, Hou Y, Ba L, Wojcik L, Qiu P, Murgolo N, et al. Clinical resistance to vicriviroc through adaptive V3 loop mutations in HIV-1 subtype D gp120 that alter interactions with the N-terminus and ECL2 of CCR5. Virology. 2010;400:145-55 pubmed publisher
    ..Collectively, these amino acid changes influenced the interaction of gp120 with both the N-terminus and ECL2 region of CCR5. ..
  77. Zhang S, Hughes J, Murgolo N, Levitan D, Chen J, Liu Z, et al. Mutation Detection in an Antibody-Producing Chinese Hamster Ovary Cell Line by Targeted RNA Sequencing. Biomed Res Int. 2016;2016:8356435 pubmed publisher
    ..The effect of an extended culturing period to mimic the scale of cell expansion in a manufacturing process and varying selection pressure in the cell culture were also closely examined. ..
  78. Jia Y, Wang X, Varty L, Rizzo C, Yang R, Correll C, et al. Functional TRPV4 channels are expressed in human airway smooth muscle cells. Am J Physiol Lung Cell Mol Physiol. 2004;287:L272-8 pubmed
    ..We conclude that functional TRPV4 is expressed in human airway smooth muscle cells and may act as an osmolarity sensor in the airway. ..
  79. Wu R, Anthes J, Kreutner W, Harris A, West R. Desloratadine inhibits constitutive and histamine-stimulated nuclear factor-kappaB activity consistent with inverse agonism at the histamine H1 Receptor. Int Arch Allergy Immunol. 2004;135:313-8 pubmed
    ..Inhibition of basal and histamine-stimulated NF-kappaB activity may help to explain previously reported inhibitory effects of desloratadine on allergic inflammatory mediators. ..
  80. Gluchowski N, Chitraju C, Picoraro J, Mejhert N, Pinto S, Xin W, et al. Identification and characterization of a novel DGAT1 missense mutation associated with congenital diarrhea. J Lipid Res. 2017;58:1230-1237 pubmed publisher
    ..Our findings add to the growing recognition of DGAT1 deficiency as a cause of congenital diarrhea with protein-losing enteropathy and indicate that DGAT1 mutations result in a spectrum of diseases. ..
  81. Wang P, Zhang J, Bian H, Wu P, Kuvelkar R, Kung T, et al. Induction of lysosomal and plasma membrane-bound sialidases in human T-cells via T-cell receptor. Biochem J. 2004;380:425-33 pubmed
    ..Taken together, these results suggest an important immunoregulatory role for both Neu-1 and Neu-3 in humans. ..
  82. Hsieh Y, Korfmacher W. The role of hyphenated chromatography-mass spectrometry techniques in exploratory drug metabolism and pharmacokinetics. Curr Pharm Des. 2009;15:2251-61 pubmed
    ..This review describes the major hyphenated chromatography-mass spectrometry techniques and their applications in supporting exploratory DMPK studies including various in vitro and in vivo PK and metabolite identification profiles. ..
  83. Anilkumar G, Selyutin O, Rosenblum S, Zeng Q, Jiang Y, Chan T, et al. II. Novel HCV NS5B polymerase inhibitors: discovery of indole C2 acyl sulfonamides. Bioorg Med Chem Lett. 2012;22:713-7 pubmed publisher
    ..Further SAR investigation resulted in identification of acyl sufonamide analog 7q (NS5B IC(50)=0.039?M, replicon EC(50)=0.011?M) with >100-fold improved replicon activity. ..
  84. Parker E, Babij C, Balasubramaniam A, Burrier R, Guzzi M, Hamud F, et al. GR231118 (1229U91) and other analogues of the C-terminus of neuropeptide Y are potent neuropeptide Y Y1 receptor antagonists and neuropeptide Y Y4 receptor agonists. Eur J Pharmacol. 1998;349:97-105 pubmed
  85. Huang H, Nguyen T, Pickett C. Regulation of the antioxidant response element by protein kinase C-mediated phosphorylation of NF-E2-related factor 2. Proc Natl Acad Sci U S A. 2000;97:12475-80 pubmed
  86. Varty G, Lu S, Morgan C, Cohen Williams M, Hodgson R, Smith Torhan A, et al. The anxiolytic-like effects of the novel, orally active nociceptin opioid receptor agonist 8-[bis(2-methylphenyl)methyl]-3-phenyl-8-azabicyclo[3.2.1]octan-3-ol (SCH 221510). J Pharmacol Exp Ther. 2008;326:672-82 pubmed publisher
    ..Collectively, these data suggest that NOP agonists such as SCH 221510 may have an anxiolytic-like profile similar to benzodiazepines, with a reduced side-effect liability. ..
  87. Moton A, Krishna G, Wang Z. Tolerability and safety profile of posaconazole: evaluation of 18 controlled studies in healthy volunteers. J Clin Pharm Ther. 2009;34:301-11 pubmed publisher
    ..Posaconazole also demonstrated minimal potential to prolong corrected QT interval. The safety profile analysis found posaconazole to be well tolerated, and results were similar across sex, age and race. ..
  88. Buontempo P, Wojcik L, Buontempo C, Ogert R, Strizki J, Howe J, et al. Quantifying the relationship between HIV-1 susceptibility to CCR5 antagonists and virus affinity for antagonist-occupied co-receptor. Virology. 2009;395:268-79 pubmed publisher
  89. Zeng Q, Nair A, Rosenblum S, Huang H, Lesburg C, Jiang Y, et al. Discovery of an irreversible HCV NS5B polymerase inhibitor. Bioorg Med Chem Lett. 2013;23:6585-7 pubmed publisher
    ..The results of distribution, metabolism and pharmacokinetics were reported. Compound 2e was demonstrated to be potent (replicon GT-1b EC50 = 0.003 ?M), highly selective, and safe in in vitro and in vivo assays. ..
  90. Davidson M, Tomassini J, Jensen E, Neff D, Polis A, Tershakovec A. Changing characteristics of statin-related cIMT trials from 1988 to 2006. Atherosclerosis. 2016;246:121-9 pubmed publisher
    ..These trends are consistent with increased treatment and control of high LDL-C levels over recent years in clinical practice, and may influence the results of cIMT studies. ..
  91. Gilchrest H, Cheewatrakoolpong B, Billah M, Egan R, Anthes J, Greenfeder S. Human cord blood-derived mast cells synthesize and release I-309 in response to IgE. Life Sci. 2003;73:2571-81 pubmed
    ..These results suggest that IgE, through the production and release of cytokines such as I-309, GM-CSF and MIP-1alpha could promote an inflammatory reaction in the absence of antigen stimulation of mast cells. ..
  92. Chen J, Tran C, Xiao L, Palamanda J, Klapmuts T, Kumari P, et al. Co-induction of CYP3A12 and 3A26 in dog liver slices by xenobiotics: species difference between human and dog CYP3A induction. Drug Metab Lett. 2009;3:61-6 pubmed
    ..This finding suggests that these two amino acids may play a role in the binding specificity of ligands. ..