Zobrazeno 1 - 10
of 26
pro vyhledávání: '"David G. Harden"'
Autor:
Shu Chang, Anthony V. Azzara, Yi-Xin Li, Marta Dabros, James Kempson, Reshma Panemangelor, Huji Turdi, Kimberly A. Foster, William J. Keim, Jean M. Whaley, Jeffrey A. Robl, Fang Moore, Luping Chen, Mary Jane Cullen, Xiaoping Hou, Atsu Apedo, R. Michael Lawrence, Arvind Mathur, David G. Harden, Wei Meng, Kevin O'Malley, Mary Ann Pelleymounter, Hannguang Chao, Pratik Devasthale, Jon J. Hangeland, Zhengping Ma, Dauh-Rurng Wu, Robert Paul Brigance, Guohua Zhao, Lynn M. Abell, Qi Gao, Susan Harvey, Lisa M. Kopcho, Dong Cheng, Elizabeth A. Dierks, Ching-Hsuen Chu, Suzanne Rooney, Xiang-Yang Ye, Saleem Ahmad, Wei Wang
Publikováno v:
Journal of Medicinal Chemistry. 64:14773-14792
MGAT2 inhibition is a potential therapeutic approach for the treatment of metabolic disorders. High-throughput screening of the BMS internal compound collection identified the aryl dihydropyridinone compound 1 (hMGAT2 IC50 = 175 nM) as a hit. Compoun
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::40e90999a2854f1a395c0459b5cd876d
https://doi.org/10.1021/acs.jmedchem.1c01356
https://doi.org/10.1021/acs.jmedchem.1c01356
Autor:
Neha Surti, Jonathan Lippy, Samuel Gerritz, David G. Harden, Peter Chase, Jefferson Chin, Julia M. Nielsen, Harold N. Weller, R. Michael Lawrence, Wilson Z. Shou, Darshani Weerakoon
Publikováno v:
SLAS discovery : advancing life sciences RD. 26(2)
Hits from high-throughput screening (HTS) assays are typically evaluated using cheminformatics and/or empirical approaches before a decision for follow-up (activity confirmation and/or sample resynthesis) is made. However, the compound integrity (i.e
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0c60028ac212de1108d34666138b183b
https://pubmed.ncbi.nlm.nih.gov/32400264
https://pubmed.ncbi.nlm.nih.gov/32400264
Autor:
Matt Soars, Lisa M. Kopcho, Carolyn A. Weigelt, Shilpa Demes, Gregory D. Vite, Mary J. Harner, Rohit Malik, Guo Li, David G. Harden, Charles F. Voliva, Kevin O’Malley, Zheming Ruan, Lan-Ying Qin, Brian J. Arey, Peter K. Park, Jennifer Price, Steven Sheriff, Gerald J. Duke, Ashvinikumar V. Gavai, JIngjing Deng, Brian E. Fink, Christopher M. Barbieri, Max Ruzanov, Muge Celiktas, Mark R. Witmer, Yuval Blat, William D. Schmitz, Joseph G. Naglich, Iyoncy Rodrigo
Publikováno v:
Cancer Research. 81:1140-1140
The chromosome 9p21 (chr9p21) locus is deleted in almost 10% of all cancer types. This locus includes the CDKN2A gene that encodes the critical tumor suppressors p19-ARF and p16-INK4a. Methylthioadenosine phosphorylase (MTAP), a gene proximal to CDKN
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::769a298e5dedd6469a5cf85008a3a619
https://doi.org/10.1158/1538-7445.am2021-1140
https://doi.org/10.1158/1538-7445.am2021-1140
Autor:
Jean-François Lavallée, Yanou Yang, Carol A. Watson, Karen S. Hartl, Victor R. Guarino, Mark Gagnon, Timothy W. Harper, E. Scott Priestley, Jing Yang, Anne Marinier, Ruediger Edward H, Alain Martel, Dietmar A. Seiffert, Michel Bouvier, Ruth R. Wexler, Jacques Banville, Todd J. Friends, Roger Remillard, Michael M. Miller, Pancras C. Wong, Shana L. Posy, Ge Zhang, David G. Harden, Jonathan L. Josephs, Jon J. Hangeland, Harold R. O'Grady, R. Michael Lawrence, Sarah E. Malmstrom, Nick J. Allegretto, François Tremblay
Publikováno v:
Journal of medicinal chemistry. 62(16)
In an effort to identify novel antithrombotics, we have investigated protease-activated receptor 4 (PAR4) antagonism by developing and evaluating a tool compound, UDM-001651, in a monkey thrombosis model. Beginning with a high-throughput screening hi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cf314765253f0852affa327de9bc38c5
https://pubmed.ncbi.nlm.nih.gov/31246024
https://pubmed.ncbi.nlm.nih.gov/31246024
Autor:
Lynn M. Abell, Scott A. Shaw, David G. Harden, Meriah Neissel Valente, Sylwia Stachura, Xiaoqin Liu, Kristen Pike, Ellen K. Kick, Kimberly Nowak, Benjamin P. Vokits, Andrew Quoc Viet, Nicholas R. Wurtz, Ji Gao, Javed Khan, Gayani Fernando, Gerald J. Duke, Ruth R. Wexler, Franck Duclos, Gregory A. Locke, Lei Zhao, Ashok Dongre, Paul G. Sleph, David A. Gordon
Publikováno v:
MedChemComm. 8(11)
Myeloperoxidase, a mammalian peroxidase involved in the immune system as an anti-microbial first responder, can produce hypochlorous acid in response to invading pathogens. Myeloperoxidase has been implicated in several chronic pathological diseases
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6938309a24e135aae00aaf681ec2a84d
https://pubmed.ncbi.nlm.nih.gov/30108726
https://pubmed.ncbi.nlm.nih.gov/30108726
Autor:
Vincenzo Calandra, Steven I. Dworetzky, Yong-Jin Wu, Ronald J. Knox, William Fitzpatrick, Huan He, JoAnne E Natale, David G. Harden, Li-Qiang Sun, Carl D. Davis, David Weaver, Frederic Machet, Joseph Polino, John E. Starrett, Karen Heman, Ping Chen, Valentin K. Gribkoff, Christopher G. Boissard, Clotilde Bourin, Charles M. Conway, Jie Chen, Mark W. Thompson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:6188-6191
Acrylamide (S)-6, a potent and efficacious KCNQ2 (Kv7.2) opener, demonstrated significant activity in two models of neuropathic pain and in the formalin test, suggesting that KCNQ2 openers may be useful in the treatment of neuropathic pain including
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4c81071ad17f712c14b9149ad6dfe150
https://doi.org/10.1016/j.bmcl.2013.08.092
https://doi.org/10.1016/j.bmcl.2013.08.092
Autor:
Ivar M. McDonald, Robert A. Mate, Debra J. Post-Munson, Meredith Ferrante, David G. Harden, Lizbeth Gallagher, Richard E. Olson, F. Christopher Zusi, Barbara J. Robertson, Steven I. Dworetzky, Daniel G. Morgan, Hong Huang, Ronald J. Knox, Nicholas J. Lodge, John E. Macor, Robert L. Bertekap
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:1684-1688
High throughput screening led to the identification of a novel series of quinolone α7 nicotinic acetylcholine receptor (nAChR) agonists. Optimization of an HTS hit (1) led to 4-phenyl-1-(quinuclidin-3-ylmethyl)quinolin-2(1H)-one, which was found to
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9746d0f86cd20debcb9cc92ebb146599
https://doi.org/10.1016/j.bmcl.2013.01.070
https://doi.org/10.1016/j.bmcl.2013.01.070
Autor:
William A. Schumacher, Jocelyne Guay, J.Eileen Bird, David A. Gordon, Mary Giancarli, Ruth R. Wexler, Pancras C. Wong, Mario Callejo, Michael M. Miller, Carol A. Watson, Julia Guy, Anne Marinier, Brad D. Maxwell, Ji Hua, E. Scott Priestley, Dietmar A. Seiffert, David G. Harden, Michel Bouvier, R. Michael Lawrence, Jacques Banville, Jing Yang, Nick J. Allegretto, Jeffrey S. Bostwick
Publikováno v:
Science translational medicine. 9(371)
Antiplatelet agents are proven efficacious treatments for cardiovascular and cerebrovascular diseases. However, the existing drugs are compromised by unwanted and sometimes life-threatening bleeding that limits drug usage or dosage. There is a substa
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b8d427e379afff9473a9e5e545b39ec1
https://pubmed.ncbi.nlm.nih.gov/29610748
https://pubmed.ncbi.nlm.nih.gov/29610748
Autor:
Robert G. Gentles, Michael A. Poss, Tracey Fiedler, Ronald J. Knox, David G. Harden, Shuanghua Hu, Yazhong Huang, C. J. Andres, Nicholas J. Lodge, C. David Weaver, Katherine A. Grant-Young
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:5694-5697
An exploratory SAR study on a series of potent, non-apamin-displacing 4-(aminomethylaryl)pyrazolopyrimidine KCa channel blockers is described and their selectivity against KCa channel subtypes is reported. The most potent analog, 5-chloro-N-(thiophen
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7bea31396fd449f218df9992fbb861d4
https://doi.org/10.1016/j.bmcl.2008.08.026
https://doi.org/10.1016/j.bmcl.2008.08.026
Publikováno v:
SLAS Discovery. 13:486-493
Fluorescent detection of calcium mobilization has been used successfully to identify modulators of G-protein-coupled receptors (GPCRs); however, inherent issues with fluorescence may limit its potential for high-throughput screening miniaturization.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7b221ef1f14396924a9f0accb37da054
https://doi.org/10.1177/1087057108319212
https://doi.org/10.1177/1087057108319212