Research Topics
Species | Bennett MaSummaryAffiliation: Merck Research Laboratories Country: USA Publications
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Detail Information
Publications
Non-peptide alpha(v)beta(3) antagonists. Part 3: identification of potent RGD mimetics incorporating novel beta-amino acids as aspartic acid replacementsPaul J Coleman
Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA
Bioorg Med Chem Lett 12:31-4. 2002..Modification of the beta-alanine 3-substituents alters the potency and physicochemical properties of these receptor antagonists and in some cases provides orally bioavailable alpha(v)beta(3) inhibitors...
Cytotoxicity of a Quinone-containing Cockroach Sex Pheromone in Human Lung Adenocarcinoma CellsBennett Ma
Department of Drug Metabolism, Merck Research Laboratories, West Point, Pennsylvania 19486, USA
Chem Res Toxicol 20:72-8. 2007..Future experiments may be needed to evaluate the overall safety of BTQ before the commercialization of the compound as a cockroach attractant...
Purification and cloning of a Delta class glutathione S-transferase displaying high peroxidase activity isolated from the German cockroach Blattella germanicaBennett Ma
Department of Drug Metabolism, Merck Research Laboratories, West Point, PA 19486, USA
FEBS J 274:1793-1803. 2007..ELISA showed that BgGSTD1 bound to serum IgE obtained from patients with cockroach allergy, indicating that the protein may be a cockroach allergen...
Cytochrome P450 2C8 (CYP2C8)-mediated hydroxylation of an endothelin ETA receptor antagonist in human liver microsomesBennett Ma
Department of Drug Metabolism, WP 75A 203, Merck Research Laboratories, West Point, PA 19486, USA
Drug Metab Dispos 32:473-8. 2004..It is concluded that the hydroxylation of compound A is mainly catalyzed by CYP2C8, and thus the reaction can possibly serve as an alternative marker assay for CYP2C8 in human liver microsomes...
Cytochrome P450 3A-dependent metabolism of a potent and selective gamma-aminobutyric acid Aalpha2/3 receptor agonist in vitro: involvement of cytochrome P450 3A5 displaying biphasic kineticsBennett Ma
Department of Drug Metabolism, Merck Research Laboratories, West Point, PA 19486, USA
Drug Metab Dispos 35:1301-7. 2007..It is concluded that CYP3A4 plays a major role in TPA023 metabolism, and CYP3A5 may also contribute at higher concentrations of the compound...
Mechanistic studies on metabolic interactions between gemfibrozil and statinsThomayant Prueksaritanont
Department of Drug Metabolism, WP75 100, Merck Research Laboratories, West Point, PA 19486, USA
J Pharmacol Exp Ther 301:1042-51. 2002..Collectively, the results of these studies provide metabolic insight into the nature of drug-drug interaction between GFZ and statins, and a possible explanation for the enhanced susceptibility of CVA to interactions with GFZ...
CYP2C75-involved autoinduction of metabolism in rhesus monkeys of methyl 3-chloro-3'-fluoro-4'-{(1R)-1-[({1-[(trifluoroacetyl)amino]cyclopropyl}carbonyl)amino]ethyl}-1,1'-biphenyl-2-carboxylate (MK-0686), a bradykinin B1 receptor antagonistCuyue Tang
Department of Drug Metabolism and Pharmacokinetics, Merck Research Laboratories, WP75A 203, Merck and Co, Inc, West Point, PA 19486, USA
J Pharmacol Exp Ther 325:935-46. 2008..Therefore, MK-0686, both a substrate and inducer for CYP2C75, caused autoinduction of its own metabolism in rhesus monkeys by increasing the expression of this enzyme...
Acyl glucuronidation and glucosidation of a new and selective endothelin ET(A) receptor antagonist in human liver microsomesCuyue Tang
Department of Drug Metabolism, West Point, Pennsylvania 19486 0004, USA
Drug Metab Dispos 31:37-45. 2003....
Sulfotransferase 1E1 is a low km isoform mediating the 3-O-sulfation of ethinyl estradiolMichael L Schrag
Drug Metabolism Department, Merck Research Laboratories, West Point, Pennsylvania, USA
Drug Metab Dispos 32:1299-303. 2004..Collectively, these data are consistent with SULT1E1 as the primary sulfotransferase involved in EE sulfation at clinically relevant concentrations (<10 nM)...
Glycosidation of an endothelin ET(A) receptor antagonist and diclofenac in human liver microsomes: aglycone-dependent UDP-sugar selectivityCuyue Tang
Department of Drug Metabolism, Merck Research Laboratories, Sumneytown Pike, P O Box 4, WP75 100, West Point, Pennsylvania 19486 0004, USA
Drug Metab Dispos 33:1796-802. 2005..The mechanism may involve enzyme conformational changes associated with Compound A binding to the enzyme...
The human hepatic metabolism of simvastatin hydroxy acid is mediated primarily by CYP3A, and not CYP2D6Thomayant Prueksaritanont
Department of Drug Metabolism, Merck Research Laboratories, West Point, PA 19486, USA
Br J Clin Pharmacol 56:120-4. 2003..To identify the cytochrome P450 (CYP) isoforms responsible for the metabolism of simvastatin hydroxy acid (SVA), the most potent metabolite of simvastatin (SV)...
Glucuronidation of statins in animals and humans: a novel mechanism of statin lactonizationThomayant Prueksaritanont
Department of Drug Metabolism, Merck Research Laboratories, West Point, Pennsylvania 19486, USA
Drug Metab Dispos 30:505-12. 2002....
Solvent effect on cDNA-expressed human sulfotransferase (SULT) activities in vitroBennett Ma
Department of Drug Metabolism, WP 75A-203, Merck Research Laboratories, West Point, PA 19486, USA
Drug Metab Dispos 31:1300-5. 2003..4%, v/v) was reduced to <15% for all solvents examined. Thus, it is recommended that ethanol is used as the preferred solvent vehicle and that incubations with expressed enzyme contain >12 microg/ml total protein...
Discovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophreniaIzzat T Raheem
Discovery Chemistry, Merck Research Laboratories, West Point, PA 19486, USA
Bioorg Med Chem Lett 22:5903-8. 2012..Further, THPP-1 displays significantly fewer preclinical adverse events in assays measuring prolactin secretion, catalepsy, and weight gain, in contrast to the typical and atypical antipsychotics haloperidol and olanzapine...
Novel cytochrome P450-mediated ring opening of the 1,3,4-oxadiazole in setileuton, a 5-lipoxygenase inhibitorCheri M Maciolek
Department of Drug Metabolism and Pharmacokinetics, Merck Research Laboratories, WP75A 203, P O Box 4, West Point, PA 19486, USA
Drug Metab Dispos 39:763-70. 2011..An alternative, comparatively slow pathway of chemical hydrolysis also was identified and described. Three potential mechanisms for the two-step metabolic ring opening of the 1,3,4-oxadizole are proposed...
