Zobrazeno 1 - 10
of 21
pro vyhledávání: '"Gerry Everlof"'
Autor:
Yan Shi, Ying Wang, Wei Meng, Robert P. Brigance, Denis E. Ryono, Scott Bolton, Hao Zhang, Sean Chen, Rebecca Smirk, Shiwei Tao, Joseph A. Tino, Kristin N. Williams, Richard Sulsky, Laura Nielsen, Bruce Ellsworth, Michael K. Y. Wong, Jung-Hui Sun, Leslie W. Leith, Dawn Sun, Dauh-Rurng Wu, Anuradha Gupta, Richard Rampulla, Arvind Mathur, Bang-Chi Chen, Aiying Wang, Helen G. Fuentes-Catanio, Lori Kunselman, Michael Cap, Jacob Zalaznick, Xiaohui Ma, Heng Liu, Joseph R. Taylor, Rachel Zebo, Beverly Jones, Stephen Kalinowski, Joann Swartz, Ada Staal, Kevin O’Malley, Lisa Kopcho, Jodi K. Muckelbauer, Stanley R. Krystek, Steven A. Spronk, Jovita Marcinkeviciene, Gerry Everlof, Xue-Qing Chen, Carrie Xu, Yi-Xin Li, Robert A. Langish, Yanou Yang, Qi Wang, Kamelia Behnia, Aberra Fura, Evan B. Janovitz, Nicola Pannacciulli, Steven Griffen, Bradley A. Zinker, John Krupinski, Mark Kirby, Jean Whaley, Robert Zahler, Joel C. Barrish, Jeffrey A. Robl, Peter T. W. Cheng
Publikováno v:
Journal of Medicinal Chemistry. 65:4291-4317
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::cc68196d2f5ecc2fc360366195341ffb
https://doi.org/10.1021/acs.jmedchem.1c02110
https://doi.org/10.1021/acs.jmedchem.1c02110
Autor:
Brian J. Murphy, Daniel Smith, Julia Sapuppo, Giridhar S. Tirucherai, Lawrence J. Kennedy, Ching-Hsuen Chu, Anthony V. Azzara, Shiwei Tao, Glenn D. Rosen, Subramaniam Krishnananthan, Jun Li, Victor R. Guarino, Lisa Burns, Joseph R. Taylor, Milinda Ziegler, Lakshmi Sivaraman, Bruce A. Ellsworth, Selvakumar Kumaravel, Hao Zhang, Tao Wang, Jun Shi, Atsu Apedo, Dhanusu Suresh, Kathy Mosure, Gerry Everlof, David A. Gordon, Lisa Zhang, Michael Gill, Chen-Pin Hung, Jianqing Li, Peter T. W. Cheng, Robert F. Kaltenbach, Sutjano Jusuf, Ying Wang, Stephanie Boehm, Mary Ellen Cvijic, Matthew G. Soars, Chi Shing Sum, Yan Shi, Jeffrey A. Robl, Reddigunta Ramesh Babu, Bradley A. Zinker, Yanou Yang, Stephen S. Kalinowski, Carrie Xu, Steven J. Walker, Sarah C. Traeger, Rebekah Heiry, Kimberley A. Lentz, Qian Ruan
Publikováno v:
Journal of Medicinal Chemistry. 64:15549-15581
The oxycyclohexyl acid BMS-986278 (33) is a potent lysophosphatidic acid receptor 1 (LPA1) antagonist, with a human LPA1 Kb of 6.9 nM. The structure-activity relationship (SAR) studies starting from the LPA1 antagonist clinical compound BMS-986020 (1
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::c00ce908946d21bafba2486eb2e08c90
https://doi.org/10.1021/acs.jmedchem.1c01256
https://doi.org/10.1021/acs.jmedchem.1c01256
Autor:
Ching Kim Tye, Chunhong Yan, Sarah C. Traeger, Wayne Vaccaro, Yingru Zhang, Gerry Everlof, Jianqing Li, Henry Yip, Peng Li, John T. Hunt, Michael A. Poss, Gregory D. Vite, Mussari Christopher P, Steven Sheriff, Asoka Ranasinghe, Haiying Zhang, Richard A. Westhouse, Dharmpal S. Dodd, Richard Rampulla, Zheng Yang, Frank Marsilio, Derek J. Norris, Wen-Ching Han, Tram N. Huynh, Yufen Zhao, Patrice Gill, Nirmala Raghavan, Lalgudi S. Harikrishnan, Ashvinikumar V. Gavai, Susan Wee, John S. Tokarski, Dauh-Rurng Wu, Arvind Mathur, Mei-Li Wen, Huiping Zhang, David R. Tortolani, George V. Delucca, Krista Menard, Francis Y. Lee, Claude A. Quesnelle, Dawn Sun, Vijay T. Ahuja, Daniel O'malley, Christine Huang, Muthoni G. Kamau
Publikováno v:
Journal of Medicinal Chemistry. 64:14247-14265
Inhibition of the bromodomain and extra-terminal (BET) family of adaptor proteins is an attractive strategy for targeting transcriptional regulation of key oncogenes, such as c-MYC. Starting with the screening hit 1, a combination of structure-activi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e6552024d7da4fe4ccaa968fbe1cf079
https://doi.org/10.1021/acs.jmedchem.1c00625
https://doi.org/10.1021/acs.jmedchem.1c00625
Autor:
Vidya Perera, Jennifer Raftis, Samira Garonzik, Ronald Aronson, Joseph Luettgen, David E. Newby, Simon Wilson, Mohammed N. Meah, J. Gerry Everlof, Bindu Murthy
Publikováno v:
Arteriosclerosis, Thrombosis, and Vascular Biology
Supplemental Digital Content is available in the text.
Objective: PAR (protease-activated receptor)-4 antagonism has antiplatelet effects under conditions of high shear stress. We aimed to establish whether PAR4 antagonism had additive antithrom
Objective: PAR (protease-activated receptor)-4 antagonism has antiplatelet effects under conditions of high shear stress. We aimed to establish whether PAR4 antagonism had additive antithrom
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::108909ff31c635f45cba7acd1922fd02
https://doi.org/10.1161/atvbaha.120.314960
https://doi.org/10.1161/atvbaha.120.314960
Autor:
Peter T W, Cheng, Robert F, Kaltenbach, Hao, Zhang, Jun, Shi, Shiwei, Tao, Jun, Li, Lawrence J, Kennedy, Steven J, Walker, Yan, Shi, Ying, Wang, Suresh, Dhanusu, Ramesh, Reddigunta, Selvakumar, Kumaravel, Sutjano, Jusuf, Daniel, Smith, Subramaniam, Krishnananthan, Jianqing, Li, Tao, Wang, Rebekah, Heiry, Chi Shing, Sum, Stephen S, Kalinowski, Chen-Pin, Hung, Ching-Hsuen, Chu, Anthony V, Azzara, Milinda, Ziegler, Lisa, Burns, Bradley A, Zinker, Stephanie, Boehm, Joseph, Taylor, Julia, Sapuppo, Kathy, Mosure, Gerry, Everlof, Victor, Guarino, Lisa, Zhang, Yanou, Yang, Qian, Ruan, Carrie, Xu, Atsu, Apedo, Sarah C, Traeger, Mary Ellen, Cvijic, Kimberley A, Lentz, Giridhar, Tirucherai, Lakshmi, Sivaraman, Jeffrey, Robl, Bruce A, Ellsworth, Glenn, Rosen, David A, Gordon, Matthew G, Soars, Michael, Gill, Brian J, Murphy
Publikováno v:
Journal of medicinal chemistry. 64(21)
The oxycyclohexyl acid BMS-986278 (
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::80069106f38ceb56aa2828cf9bc68357
https://pubmed.ncbi.nlm.nih.gov/34709814
https://pubmed.ncbi.nlm.nih.gov/34709814
Autor:
Andrew P. Degnan, Haiquan Fang, Tatyana Zvyaga, Zuzana Haarhoff, Claude A. Quesnelle, Melissa Kramer, Frank Marsilio, Richard A. Westhouse, John S. Tokarski, Shilpa Madari, Jiuqiao Zhao, Amy Wiebesiek, Chunhong Yan, Francis Y. Lee, Michael Sinz, John Morrison, Jean Simmermacher-Mayer, Carolynn Fanslau, Steven Sheriff, Lisa Huang, Ashvinikumar V. Gavai, Chunshan Xie, Matthew D. Hill, Gerry Everlof
Publikováno v:
Bioorganicmedicinal chemistry letters. 51
We describe our efforts to introduce structural diversity to a previously described triazole-containing N1-carboline series of bromodomain and extra-terminal (BET) inhibitors. N9 carbolines were designed to retain favorable binding interactions that
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ada735600c02c9c410a77e52ab96e515
https://pubmed.ncbi.nlm.nih.gov/34560263
https://pubmed.ncbi.nlm.nih.gov/34560263
Autor:
Chunhong Yan, Francis Y. Lee, Ashvinikumar V. Gavai, Melissa Kramer, Frank Marsilio, Eric Shields, Laura Monereau, Zuzana Haarhoff, Richard A. Westhouse, Lisa Zhang, Gerry Everlof, John S. Tokarski, Matthew D. Hill, Tatyana Zvyaga, Asoka Ranasinghe, Carolynn Fanslau, Ching Kim Tye, Steven Sheriff, Christine Huang, Andrew P. Degnan, Krista Menard, John Morrison, Haiquan Fang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 44:128108
We describe our efforts to identify structurally diverse leads in the triazole-containing N1-carboline series of bromodomain and extra-terminal inhibitors. Replacement of the N5 “cap” phenyl moiety with various heteroaryls, coupled with additiona
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6dd1b9be7f6bf8d56a691226fab9f262
https://doi.org/10.1016/j.bmcl.2021.128108
https://doi.org/10.1016/j.bmcl.2021.128108
Autor:
Ivar M. McDonald, Wang Nenghui, Victor R. Guarino, Kimberley A. Lentz, Richard E. Olson, Wendy Clarke, Roy Haskell, J. Gerry Everlof
Publikováno v:
Bioorganicmedicinal chemistry letters. 30(3)
The objective of this Letter is to report the first (to our knowledge) in vivo proof of concept for a sulfenamide prodrug to orally deliver a poorly soluble drug containing a weakly-acidic NH–acid from a conventional solid dosage formulation. This
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::07dd39c1805268048faa33aa27a7d547
https://pubmed.ncbi.nlm.nih.gov/31870650
https://pubmed.ncbi.nlm.nih.gov/31870650
Autor:
Hong Wu, Gary L. Schieven, Joel C. Barrish, Bei Wang, Bang Chi Chen, Sam T. Chao, Gerry Everlof, Jung Hui Sun, Chunjian Liu, John H. Dodd, Murray McKinnon, Kathleen M. Gillooly, Katerina Leftheris, John Hynes, Tracy L. Taylor, Vivekananda M. Vrudhula, T. G. Murali Dhar, Stephen T. Wrobleski, Hongjian Zhang, David J. Shuster, Shuqun Lin, Kim W. McIntyre, Rulin Zhao, Christoph Gesenberg, James Lin, Punit Marathe
Publikováno v:
Journal of Medicinal Chemistry. 58:7775-7784
In search for prodrugs to address the issue of pH-dependent solubility and exposure associated with 1 (BMS-582949), a previously disclosed phase II clinical p38α MAP kinase inhibitor, a structurally novel clinical prodrug, 2 (BMS-751324), featuring
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9c8e794014371379532fed83f3d8fff5
https://doi.org/10.1021/acs.jmedchem.5b00839
https://doi.org/10.1021/acs.jmedchem.5b00839
Autor:
Claude A. Quesnelle, Patrice Gill, Richard Rampulla, Ching Su, Gerry Everlof, George L. Trainor, Ke Chen, Vinod Arora, Richard A. Westhouse, Celia D’Arienzo, Andrew J. Tebben, Weifang Shan, John T. Hunt, Derek J. Norris, Louis J. Lombardo, Zheng Yang, Arvind Mathur, Mei-Li Wen, Yingru Zhang, Dauh-Rurng Wu, Wen-Ching Han, Krista Menard, Victor R. Guarino, Asoka Ranasinghe, Richard E. Olson, Ashvinikumar V. Gavai, Bruce S. Fischer, Phil S. Baran, Anne Rose, Lan Xiao, Ronald E. White, Mary Ellen Cvijic, Gregory D. Vite, Ding Ren Shen, Jere E. Meredith, Haiqing Wang, Francis Y. Lee, Aaron Balog
Publikováno v:
ACS Medicinal Chemistry Letters. 6:523-527
Structure-activity relationships in a series of (2-oxo-1,4-benzodiazepin-3-yl)-succinamides identified highly potent inhibitors of γ-secretase mediated signaling of Notch1/2/3/4 receptors. On the basis of its robust in vivo efficacy at tolerated dos
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0c3995231a45ba8104a424851cf0a94b
https://doi.org/10.1021/acsmedchemlett.5b00001
https://doi.org/10.1021/acsmedchemlett.5b00001