Zobrazeno 1 - 10
of 35
pro vyhledávání: '"Mike Randal"'
Autor:
Lars Karlsson, Neelakandha S. Mani, Todd K. Jones, Steven Nguyen, Pragnya J. Desai, Cheryl A. Grice, Kristen L. Arienti, Robin L. Thurmond, Frank U. Axe, James P. Edwards, Mike Randal, Siquan Sun, Danielle K. Wiener, Michael K. Ameriks, Jing Liu, Alice Lee-Dutra, Damara Gebauer
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:2370-2374
A series of pyrazole-based thioethers were prepared and found to be potent cathepsin S inhibitors. A crystal structure of 13 suggests that the thioether moiety may bind to the S3 pocket of the enzyme. Additional optimization led to the discovery of a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8c34a29a046072b572140132f3755f69
https://doi.org/10.1016/j.bmcl.2010.01.108
https://doi.org/10.1016/j.bmcl.2010.01.108
Autor:
Stig Hansen, Jenny Kung, Lisa Taylor, Kenneth J. Barr, Mike Randal, Daniel A. Erlanson, Robert S. McDowell, Christian Wiesmann, Min Zhong, Wang Shen, Jiang Zhu, Bruce Fahr
Publikováno v:
Nature Structural & Molecular Biology. 11:730-737
Obesity and type II diabetes are closely linked metabolic syndromes that afflict >100 million people worldwide. Although protein tyrosine phosphatase 1B (PTP1B) has emerged as a promising target for the treatment of both syndromes, the discovery of p
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b03d1388952a21ac3e1df66a605ff322
https://doi.org/10.1038/nsmb803
https://doi.org/10.1038/nsmb803
Autor:
Johan D. Oslob, Brian C. Raimundo, Michelle R. Arkin, Andrew C. Braisted, Robert S. McDowell, Jennifer Wilkinson, Nathan D. Waal, Jennifer Hyde, Chul Yu, Mike Randal
Publikováno v:
Journal of Medicinal Chemistry. 47:3111-3130
Fragment assembly has shown promise for discovering small-molecule antagonists for difficult targets, including protein-protein interactions. Here, we describe a process for identifying a 60 nM inhibitor of the interleukin-2 (IL-2)/IL-2 receptor (IL-
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::280dcde8d55a70338717c0d4881f5f0d
https://doi.org/10.1021/jm049967u
https://doi.org/10.1021/jm049967u
Autor:
Warren L. DeLano, Lisa Taylor, Robert S. McDowell, Jun Wang, Tinh N Luong, Andrew C. Braisted, Jennifer Hyde, Mike Randal, James A. Wells, Johan D. Oslob, Darren Raphael, Michelle R. Arkin
Publikováno v:
Proceedings of the National Academy of Sciences. 100:1603-1608
Understanding binding properties at protein–protein interfaces has been limited to structural and mutational analyses of natural binding partners or small peptides identified by phage display. Here, we present a high-resolution analysis of a nonpep
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c1d260904f2de849f83a397e70375648
https://doi.org/10.1073/pnas.252756299
https://doi.org/10.1073/pnas.252756299
Autor:
Lars Karlsson, Siquan Sun, Mike Randal, Jian Zhu, Robin L. Thurmond, Scott D. Bembenek, Frank U. Axe, James P. Edwards, Yin Gu, Michael K. Ameriks
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(21)
A crystal structure of 1 bound to a Cys25Ser mutant of cathepsin S helped to elucidate the binding mode of a previously disclosed series of pyrazole-based CatS inhibitors and facilitated the design of a new class of arylalkyne analogs. Optimization o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::99a5e8d553cddde76f9b9bd5bed2000a
https://pubmed.ncbi.nlm.nih.gov/19773165
https://pubmed.ncbi.nlm.nih.gov/19773165
Autor:
Douglas R. Cary, Jennifer Wilkinson, Yafan Lu, Robert S. McDowell, Phuongly Pham, Jeffrey W. Jacobs, Wanli Lu, Melissa B Lam, Michael J. Romanowski, Beth Pietrak, Marcus Ballinger, Raymond V. Fucini, Jian Sun, David M Penny, Wenjin Yang, Timothy J. Allison, Mike Randal, Dennis Colussi, Anila E Thomas, Bruce T. Fahr, Kenneth E Lind, Sanjeev Munshi
Publikováno v:
Biochemistry. 48(21)
BACE-1 (beta-site amyloid precursor protein cleaving enzyme), a prominent target in Alzheimer's disease drug discovery efforts, was surveyed using Tethering technology to discover small molecule fragment ligands that bind to the enzyme active site. S
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dad4f6a235db99ac7b282b393ed54e12
https://pubmed.ncbi.nlm.nih.gov/19284778
https://pubmed.ncbi.nlm.nih.gov/19284778
Autor:
Raymond V. Fucini, M. Lam, Wenjin Yang, Jeffrey W. Jacobs, A.E. Thomas, X.P. Shi, Jian Sun, Yafan Lu, Robert S. McDowell, Wanli Lu, Jennifer Wilkinson, Ballinger, Eric M Gordon, Min Zhong, Mike Randal
Publikováno v:
Journal of medicinal chemistry. 49(3)
A series of novel beta-site amyloid precursor protein cleaving enzyme (BACE-1) inhibitors containing an aminoethylene (AE) tetrahedral intermediate isostere were synthesized and evaluated in comparison to corresponding hydroxyethylene (HE) compounds.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::374e270770cc062ecb83c84a1abfaab6
https://pubmed.ncbi.nlm.nih.gov/16451048
https://pubmed.ncbi.nlm.nih.gov/16451048
Discovery and characterization of cooperative ligand binding in the adaptive region of interleukin-2
Publikováno v:
Biochemistry. 42(21)
The cytokine hormone interleukin-2 (IL-2) contains a highly adaptive region that binds small, druglike molecules. The binding properties of this adaptive region have been explored using a "tethering" method that relies on the formation of a disulfide
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9934e235f801431f638f038912faa03b
https://pubmed.ncbi.nlm.nih.gov/12767230
https://pubmed.ncbi.nlm.nih.gov/12767230
Autor:
Brian C. Raimundo, Mike Randal, Johan D. Oslob, Warren L DeLano, Michelle R. Arkin, James A. Wells, Andrew C. Braisted, B. McDowell
Publikováno v:
Small Molecule — Protein Interactions ISBN: 9783662053164
Protein-protein interfaces remain among the most challenging if not intractable targets for small-molecule drug discovery. Despite the wealth of structural information that has accumulated about these complexes and their tremendous value as biotherap
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::340881e258070e657f8b486c9de9cf42
https://doi.org/10.1007/978-3-662-05314-0_3
https://doi.org/10.1007/978-3-662-05314-0_3
Autor:
Eric M Gordon, Daniel A. Erlanson, Darren Raphael, James A. Wells, Mike Randal, Andrew C. Braisted, Robert M. Stroud
We report a strategy (called “tethering”) to discover low molecular weight ligands (≈250 Da) that bind weakly to targeted sites on proteins through an intermediary disulfide tether. A native or engineered cysteine in a protein is allowed to rea
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c64d7f66f66382959e7457c580eee567
https://europepmc.org/articles/PMC16870/
https://europepmc.org/articles/PMC16870/