Margarita Garcia Calvo
Affiliation: Merck Research Laboratories
- The target of ezetimibe is Niemann-Pick C1-Like 1 (NPC1L1)Margarita Garcia-Calvo
Department of Metabolic Disorders, Merck Research Laboratories, Rahway, NJ 07065, USA
Proc Natl Acad Sci U S A 102:8132-7. 2005..These results unequivocally establish NPC1L1 as the direct target of ezetimibe and should facilitate efforts to identify the molecular mechanism of cholesterol transport...
- Discovery of novel aspartyl ketone dipeptides as potent and selective caspase-3 inhibitorsYongxin Han
Department of Medicinal Chemistry, Merck Frosst Centre for Therapeutic Research, Merck Frosst Canada and Co, PO Box 1005, Pointe Claire Dorval, Quebec, Canada H9R 4P8
Bioorg Med Chem Lett 14:805-8. 2004..The iterative discovery process of using combinatorial chemistry, parallel synthesis, moleculare modelling and structural biology will be discussed...
- Discovery of potent, selective human granzyme B inhibitors that inhibit CTL mediated apoptosisChristopher A Willoughby
Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA
Bioorg Med Chem Lett 12:2197-200. 2002..A novel class of small molecule human granzyme B inhibitors is reported. Compound 20 has a K(i) of 7 nM against human granzyme B and blocks CTL mediated apoptosis with an IC(50) of 3 micromolar...
- The caspase-like sites of proteasomes, their substrate specificity, new inhibitors and substrates, and allosteric interactions with the trypsin-like sitesAlexei F Kisselev
Department of Cell Biology, Harvard Medical School, Boston, Massachusetts 02115, USA
J Biol Chem 278:35869-77. 2003..Thus, occupancy of the caspase-like sites stimulates the trypsin-like activity of proteasomes, but substrates of the caspase-like sites inhibit the chymotrypsin-like activity by binding to a distinct noncatalytic site...
- Mouse and human granzyme B have distinct tetrapeptide specificities and abilities to recruit the bid pathwayLivia Casciola-Rosen
Departments of Medicine, Cell Biology, and Pathology, Johns Hopkins University School of Medicine, Baltimore, Maryland 21224, USA
J Biol Chem 282:4545-52. 2007....