Zobrazeno 1 - 10
of 26
pro vyhledávání: '"Valentine J. Klimkowski"'
Autor:
Abby Hillan, Emily Neal, Shelby Skaggs, Carson Middlebrook, Daniel Mulawa, R. Jeremy Johnson, Andrew Scheel, Alyssa Ritter, Emma Harris, Maxwell L. Todd, Jaelyn Voyles, Julia Pomeroy, Layla Wisser, Valentine J. Klimkowski, Grace Bassler, Madi Summers, Rieser Wells, Lizzy Ratz, Marisa Villarreal, Ryan Heumann, Sam Sullivan, Holly Rowe, Harrison Smith
Publikováno v:
Biochemistry and molecular biology education : a bimonthly publication of the International Union of Biochemistry and Molecular BiologyREFERENCE. 49(5)
Publikováno v:
Chirality. 31:301-311
Luminescent lanthanide (III) ions have been exploited for circularly polarized luminescence (CPL) for decades. However, very few of these studies have involved chiral samarium (III) complexes. Complexes are prepared by mixing axial chiral ligands (R/
Autor:
Timothy B. Durham, Jeffrey T. Dixon, James Lee Toth, Angela M. Siesky, Michael E. Christe, Valentine J. Klimkowski, Nathan A. Calvert, John F. Schindler, Dana Sindelar, Kyle W. Sloop, M. Dodson Michael, Jesline T. Alexander-Chacko, Julia X.C. Cao, Ginger Y. Wu, James E. McGee, Rachel N. Cavitt, Stefan Jon Thibodeaux, Sherry Y. Guo, Yong Wang, Michael J. Coghlan, Vladislav V. Kiselyov
Publikováno v:
Journal of Biological Chemistry. 290:20044-20059
Insulin-degrading enzyme (IDE, insulysin) is the best characterized catabolic enzyme implicated in proteolysis of insulin. Recently, a peptide inhibitor of IDE has been shown to affect levels of insulin, amylin, and glucagon in vivo. However, IDE(-/-
Autor:
C. Lin, Chin Liu, Valentine J. Klimkowski, Craig A. Swearingen, Lisa A. Adams, Stephanie L. Stout, Timothy B. Durham, Michael Robert Wiley, Kannan Thirunavukkarasu, Mark Chambers, Jim D. Durbin, Christopher John Rito, Jothirajah Marimuthu, James Lee Toth
Publikováno v:
Journal of Medicinal Chemistry. 57:10476-10485
A disintegrin and metalloproteinase with thrombospondin motifs-4 (ADAMTS-4) and ADAMTS-5 are zinc metalloproteases commonly referred to as aggrecanase-1 and aggrecanase-2, respectively. These enzymes are involved in the degradation of aggrecan, a key
Autor:
Michael A. Mohutsky, Valentine J. Klimkowski, Bhargav Patel, Prasad V. Bharatam, Nikhil Taxak, Prashant V. Desai, Vijay K. Gombar
Publikováno v:
Journal of Computational Chemistry. 33:1740-1747
Mechanism-based inhibition (MBI) of cytochrome P450 (CYP) can lead to drug-drug interactions and often to toxicity. Some aliphatic and aromatic amines can undergo biotransformation reactions to form reactive metabolites such as nitrosoalkanes, leadin
Autor:
Gerald F. Smith, Wayne W. Weber, John Walter Nr Macclesfield Liebeschuetz, Philip Sipes, Jeffry Bernard Franciskovich, Richard D. Towner, John Joseph Masters, Donetta S. Gifford-Moore, Trelia J. Craft, Ronald S. Foster, Jeffrey K. Smallwood, Michael L. Chouinard, Lea M. Johnson, Larry L. Froelich, Stephen C. Young, David W. Snyder, Marcia K. Chastain, Valentine J. Klimkowski, Christopher W. Murray
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:6910-6913
Several P4 domain derivatives of the general d-phenylglycinamide-based scaffold (2) were synthesized and evaluated for their ability to bind to the serine protease factor Xa. Some of the more potent compounds were evaluated for their anticoagulant ef
Autor:
Scott Martin Sheehan, Nikolay Y. Chirgadze, Gerald F. Smith, Jolie Anne Bastian, Michael Robert Wiley, Trelia J. Craft, Daniel Jon Sall, Jeffrey K. Smallwood, Jothirajah Marimuthu, John Walter Nr Macclesfield Liebeschuetz, Marcia K. Chastain, Philip Sipes, Jeffry Bernard Franciskovich, Brian Morgan Watson, Ronald S. Foster, Valentine J. Klimkowski
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:5801-5805
Analogs to a series of D-phenylglycinamide-derived factor Xa inhibitors were discovered. It was found that the S4 amide linkage can be replaced with an ether linkage to reduce the peptide character of the molecules and that this substitution leads to
Autor:
Stephanie L. Stout, Patrick C. May, Brian Morgan Watson, Pablo Garcia Losada, Valentine J. Klimkowski, Brian Michael Mathes, David E. Timm, Dustin J. Mergott, Scott A. Monk, Leonard L. Winneroski, Leonard N. Boggs, James P. Beck, James E. Audia, Matthew Allen Schiffler, Richard A. Brier, Anthony R. Borders, Jon A. Erickson, Robert D. Boyer, Kevin John Hudziak
Publikováno v:
Bioorganicmedicinal chemistry. 23(13)
The BACE1 enzyme is a key target for Alzheimer’s disease. During our BACE1 research efforts, fragment screening revealed that bicyclic thiazine 3 had low millimolar activity against BACE1. Analysis of the co-crystal structure of 3 suggested that po
Autor:
Linebarger Jh, Michael Robert Wiley, Leonard C. Weir, Trelia J. Craft, Goodson T, Donetta S. Gifford-Moore, Kyle Ja, Jason Scott Sawyer, Valentine J. Klimkowski, David K. Herron, Anne Louise Tebbe, Smith Gf, Douglas W. Beight, Ying Kwong Yee, Jennifer M. Tinsley, Richard D. Towner
Publikováno v:
Journal of Medicinal Chemistry. 43:873-882
Reversal of the A-ring amide link in 1,2-dibenzamidobenzene 1 (fXa K(ass) = 0.81 x 10(6) L/mol) led to a series of human factor Xa (hfXa) inhibitors based on N(2)-aroylanthranilamide 4. Expansion of the SAR around 4 showed that only small planar subs
Autor:
Sau-Chi B. Yan, Michael L. Denney, Valentine J. Klimkowski, Amy J. Smith, Lea M. Johnson, Michael Enrico Richett, Minsheng Zhang, Jefferson Ray Mccowan, Kumiko Takeuchi, Todd J. Kohn, Nickolay Y. Chirgadze, Jolie Anne Bastian, Dianna L. Bailey, Donetta S. Gifford-Moore, Barbara G. Utterback, Gerald F. Smith, Daniel Jon Sall, David K. Clawson, Richard Waltz Harper, David W. Snyder, Stephen L. Briggs, Ho-Shen Lin
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 9:775-780
Potent, subnanomolar thrombin inhibitors 4, 5, and 6 are developed through side chain optimization of novel, benzo[b]thiophene-based small organic entities 2 and 3 and through SAR additivity studies of the new structural elements identified. X-ray cr