Zobrazeno 1 - 10
of 41
pro vyhledávání: '"Douglas C. Beshore"'
Autor:
Victoria A. Kleiner, Thierry O. Fischmann, John A. Howe, Douglas C. Beshore, Michael J. Eddins, Yan Hou, Todd Mayhood, Daniel Klein, Debbie D. Nahas, Bob J. Lucas, He Xi, Edward Murray, Daphne Y. Ma, Krista Getty, Rachel Fearns
Publikováno v:
Communications Biology, Vol 6, Iss 1, Pp 1-12 (2023)
Abstract Respiratory syncytial virus (RSV) and human metapneumovirus (HMPV) are related RNA viruses responsible for severe respiratory infections and resulting disease in infants, elderly, and immunocompromised adults1–3. Therapeutic small molecule
Externí odkaz:
https://doaj.org/article/b774cd14df994f13b41ff196588a5489
Autor:
Scott E. Wolkenberg, Richard J. O. Barnard, Steven N. Gallicchio, Michael A. Plotkin, Douglas C. Beshore, Christine Burlein, Robert W. Myers, M. Katharine Holloway, Daniel J. Klein, Vanessa L. Rada, Christopher D. Cox, David A. Powell, Daniel Krosky, Paul J. Coleman, Gregory C. Adam, Sangita B. Patel, Wei Lemaire
Publikováno v:
ACS Medicinal Chemistry Letters
A novel series of histone deacetylase (HDAC) inhibitors lacking a zinc-binding moiety has been developed and described herein. HDAC isozyme profiling and kinetic studies indicate that these inhibitors display a selectivity preference for HDACs 1, 2,
Autor:
Douglas C. Beshore, Andrew M. Haidle, Ashok Arasappan, Yeon-Hee Lim, Izzat Raheem, Anthony J. Roecker, Samantha E. Shockley, Vladimir Simov
Publikováno v:
Journal of medicinal chemistry. 65(5)
Increasing the efficiency of the drug discovery process is a challenge faced by drug hunters everywhere. One strategy medicinal chemists employ to meet this challenge is learning from knowledge sources within and beyond their organization. In this Pe
Autor:
William J. Ray, Mark T. Bilodeau, Matthew A. Seager, Marion Wittmann, Thomas J. Greshock, Scott D. Kuduk, Joy Fuerst, Lei Ma, Douglas C. Beshore, Kenneth A. Koeplinger, Christina N. Di Marco, Charles D. Thompson, George D. Hartman, Ronald K. Chang
Publikováno v:
ACS Medicinal Chemistry Letters. 9:652-656
Identification of ligands that selectively activate the M1 muscarinic signaling pathway has been sought for decades to treat a range of neurological and cognitive disorders. Herein, we describe the optimization efforts focused on addressing key physi
Autor:
Steven V. Fox, Kate Mostoller, Steve Warrington, Chris Min, Caroline Cilissen, Marion Wittmann, Douglas C. Beshore, Dawn Harris, Henry S. Lange, Natasa Pajkovic, Jason M. Uslaner, Chantal Mahon, Scott D. Kuduk
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 365:556-566
The current standard of care for treating Alzheimer's disease is acetylcholinesterase inhibitors, which nonselectively increase cholinergic signaling by indirectly enhancing activity of nicotinic and muscarinic receptors. These drugs improve cognitiv
Autor:
Douglas C. Beshore, Stephen Day, Jason Cassaday, Michelle F. Homsher, Brian Squadroni, David Pechter, Michelle Smith, Lei Ma, Jeffrey D. Hermes, Elizabeth Mohammed, Michelle Hartnett, Paul Zuck, Michael F.A. Finley, Victor N. Uebele, Fredrick Monsma
Publikováno v:
SLAS Discovery. 22:1060-1066
Agonist shift assays feature cross-titrations of allosteric modulators and orthosteric ligands. Information generated in agonist shift assays can include a modulator's effect on the orthosteric agonist's potency (alpha) and efficacy (beta), as well a
Autor:
James I. Fells, John M. Sanders, Jason E. Imbriglio, Suen Linda M, Andrew M. Haidle, Abbas Walji, Elizabeth Joshi, William D. Shipe, Nunzio Sciammetta, Hakan Gunaydin, Tjerk Bueters, Andreas Verras, Robert P. Sheridan, J. Christopher Culberson, Brian E. Mattioni, Marc A. Labroli, Douglas C. Beshore
Publikováno v:
Journal of Medicinal Chemistry. 60:6771-6780
High-throughput screening (HTS) has enabled millions of compounds to be assessed for biological activity, but challenges remain in the prioritization of hit series. While biological, absorption, distribution, metabolism, excretion, and toxicity (ADME
Autor:
Daniel R. Pitts, Victoria Cofre, Adam W. Johnson, Douglas C. Beshore, Scott D. Kuduk, Robert M. DiPardo
Publikováno v:
Journal of Heterocyclic Chemistry. 54:1558-1571
Complementary strategies to 2,5-disubstituted pyrazolo[4,3-c]cinnolin-3-ones are reported herein, providing late stage substituent introduction at either the 2- or the 5-position. Treating a readily prepared 4-thiocinnoline ester with substituted hyd
Autor:
Jonathan Steele, Yong Liu, Liam Evans, Ronald de Vries, Richard Phipps, Cheri M Maciolek, Roy Helmy, Steven L. Colletti, Iain Martin, Gary E. Martin, Douglas C. Beshore, Natasa Pajkovic, Headley Williams, Rhys Salter, Yong Gong, James H. Small
Publikováno v:
Xenobiotica; the fate of foreign compounds in biological systems. 49(8)
Metabolite identification is an integral part of both preclinical and clinical drug discovery and development. Synthesis of drug metabolites is often required to support definitive identification, preclinical safety studies and clinical trials. Here
Autor:
Douglas C, Beshore, Christina, N Di Marco, Ronald K, Chang, Thomas J, Greshock, Lei, Ma, Marion, Wittmann, Matthew A, Seager, Kenneth A, Koeplinger, Charles D, Thompson, Joy, Fuerst, George D, Hartman, Mark T, Bilodeau, William J, Ray, Scott D, Kuduk
Publikováno v:
ACS medicinal chemistry letters. 9(7)
[Image: see text] Identification of ligands that selectively activate the M(1) muscarinic signaling pathway has been sought for decades to treat a range of neurological and cognitive disorders. Herein, we describe the optimization efforts focused on