Zobrazeno 1 - 10
of 37
pro vyhledávání: '"Akbar Nayeem"'
Autor:
Andrea Olga Andrea Olga Shorts, Aaron P. Yamniuk, Keith S. Bahjat, Radha Ramakrishnan, Gaëlle Martin, Sanjib Dutta, David A Critton, Hua Fang, Dibella Rose A, Kader Thiam, Lynne Campbell, Arathi Krishnakumar, Burce Ergel, Martin J. Corbett, Haibin Chen, Robert J. Johnston, Richard Y.-C. Huang, Alan J. Korman, Joseph M. Rizzo, Thomas Cayton, Zheng Yang, Michael Quigley, Jason Pinckney, Ying-Kai Wang, Ginger Rakestraw, Justine Ngo, Paul O. Sheppard, Linhui Julie Su, Andrew Rankin, Jim Holloway, Xiaodi Deng, Akbar Nayeem, Arvind Rajpal, Eric Boyer, Hadia Lemar, Alexander T. Kozhich
Publikováno v:
Nature. 574:565-570
Co-inhibitory immune receptors can contribute to T cell dysfunction in patients with cancer1,2. Blocking antibodies against cytotoxic T-lymphocyte-associated protein 4 (CTLA-4) and programmed cell death 1 (PD-1) partially reverse this effect and are
Autor:
Neil T. Burford, Marta Dabros, Mujing Yan, Michael C. Myers, Robert Langish, Cullen L. Cavallaro, R. Michael Lawrence, Shun Su, Ruth R. Wexler, Akbar Nayeem, Yi-Xin Li, Anne Rose, Chao Hannguang J, Peter S. Gargalovic, Kamelia Behnia, Bilder Donna M, Tao Wang, Joelle M. Onorato
Publikováno v:
Bioorganicmedicinal chemistry letters. 30(7)
This article describes the discovery of aryl hydroxy pyrimidinones and the medicinal chemistry efforts to optimize this chemotype for potent APJ agonism. APJ is a G-protein coupled receptor whose natural agonist peptide, apelin, displays hemodynamic
Autor:
Giridhar S. Tirucherai, Sean M. Crawford, Binodh DeSilva, Renuka Pillutla, Akbar Nayeem, Lora Hamuro, Craig J. Thalhauser, Tarek A. Leil
Publikováno v:
The AAPS journal. 21(5)
A mechanistic model of the immune response was evaluated for its ability to predict anti-drug antibody (ADA) and their impact on pharmacokinetics (PK) and pharmacodynamics (PD) for a biotherapeutic in a phase 1 clinical trial. Observed ADA incidence
Autor:
Paul E. Morin, Haixia Wang, Lawrence J. Kennedy, Stephen P. O'connor, James J. Li, Akbar Nayeem, Vidhyashankar Ramamurthy, Steven Sheriff, Nathan Morgan, Steven J. Walker, Xiang-Yang Ye, Frederick Moulin, Brad D. Maxwell, Thomas Harrity, Jeffrey A. Robl, Stephanie Y. Chen, Timothy W. Harper, Rachel Zebo, Jun Li, Zhenqiu Hong, Shung Wu, Mengmeng Wang, Randolph P. Ponticiello, David A. Gordon, Rajasree Golla, Ramakrishna Seethala, Daniel M. Camac, Joseph R. Taylor, David S. Yoon
[Image: see text] BMS-823778 (2), a 1,2,4-triazolopyridinyl-methanol derived analog, was identified as a potent and selective inhibitor of human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD-1) enzyme (IC(50) = 2.3 nM) with >10,000-fold selectiv
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::537bf023154f9aff48423a9bc7df61b2
https://europepmc.org/articles/PMC6295842/
https://europepmc.org/articles/PMC6295842/
Autor:
Steven J. Walker, Vidyhashankar Ramamurthy, Jun Li, Shung Wu, David K. Leahy, John D. Dimarco, Brad D. Maxwell, Daniel M. Camac, Joseph R. Taylor, Akbar Nayeem, Zhiwei Guo, James J. Li, Xiang-Yang Ye, Frederick Moulin, Paul E. Morin, Stepen P O’Connor, Haixia Wang, Jeffrey A. Robl, Rachel Zebo, Mark S. Kirby, Thomas Harrity, Joel C. Barrish, Timothy W. Harper, Lawrence L Kennedy, Rajasree Golla, Atsu Apedo, Bogdan Sleczka, Yi-Xin Li, David S. Yoon, Bin He, Steven Sheriff, Ramakrishna Seethala, Nathan Morgan, Mengmeng Wang, Randolph P. Ponticiello, Raymond P. Scaringe, Stephanie Y. Chen, Jianqing Li, Zhenqiu Hong, Ronald L. Hanson, David A. Gordon
Publikováno v:
Journal of medicinal chemistry. 60(12)
BMS-816336 (6n-2), a hydroxy-substituted adamantyl acetamide, has been identified as a novel, potent inhibitor against human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzyme (IC50 3.0 nM) with >10000-fold selectivity over human 11β-hydrox
Autor:
Ramakrishna Seethala, Steven J. Walker, Jun Li, Stephen P. O'connor, Lawrence J. Kennedy, Steven Sheriff, Rachel Zebo, Daniel M. Camac, Paul E. Morin, Jeffrey A. Robl, Joseph R. Taylor, James J. Li, Haixia Wang, Thomas Harrity, David A. Gordon, Akbar Nayeem, Timothy W. Harper, Zhenqiu Hong, Mengmeng Wang, Randolph P. Ponticiello, Rajasree Golla, Nathan Morgan
Publikováno v:
ACS Medicinal Chemistry Letters. 5:803-808
Small alkyl groups and spirocyclic-aromatic rings directly attached to the left side and right side of the 1,2,4-triazolopyridines (TZP), respectively, were found to be potent and selective inhibitors of human 11β-hydroxysteroid dehydrogenase-type 1
Autor:
Mengmeng Wang, Akbar Nayeem, Ramakrishna Seethala, Stephanie Y. Chen, Rajasree Golla, Jeffrey A. Robl, Bin He, Yi-Xin Li, Bogdan Sleczka, David A. Gordon, Xiang-Yang Ye, Timothy W. Harper, Mark S. Kirby
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:6699-6704
Starting from high throughput screening hit 2-adamantyl acetic acid 3, a series of polycyclic acids have been designed and synthesized as novel, potent, and selective inhibitors of human 11β-HSD-1. Structure-activity relationships of two different r
Publikováno v:
Journal of Computer-Aided Molecular Design. 23:411-418
The success of structure-based drug design relies on accurate protein modeling where one of the key issues is the modeling and refinement of loops. This study takes a critical look at modeled loops, determining the effect of re-sampling side-chains a
Publikováno v:
Protein Engineering Design and Selection. 22:257-266
Epothilone F, 21-hydroxyl-epothilone B, is an intermediate in the synthesis of BMS-310705, an antitumor compound that has been evaluated in Phase I clinical trials. A bioconversion process utilizing the Gram-positive bacterium Amycolatopsis orientali
Autor:
Rajasree Golla, Zhengping Ma, David A. Gordon, Haixia Wang, Yuval Blat, Shung C. Wu, Bhavana Sahni-Arya, Mary Ellen K. Salyan, Donna L. Pedicord, Michael J. Flynn, James J. Li, Cynthia Gates, Laurie Bergeron, Ramakrishna Seethala, Lawrence G. Hamann, Akbar Nayeem
Publikováno v:
Biochimica et Biophysica Acta (BBA) - Proteins and Proteomics. 1774:1184-1191
11beta-hydroxysteroid dehydrogenase 1 regulates the tissue availability of cortisol by interconverting cortisone and cortisol. It is capable of functioning as both a reductase and a dehydrogenase depending upon the surrounding milieu. In this work, w