Zobrazeno 1 - 10
of 43
pro vyhledávání: '"Sing-Yuen Sit"'
Autor:
Brian McAuliffe, Paul Falk, Jie Chen, Yan Chen, Sing-Yuen Sit, Jacob Swidorski, Richard A. Hartz, Li Xu, Brian Venables, Ny Sin, Nicholas A. Meanwell, Alicia Regueiro-Ren, David Wensel, Umesh Hanumegowda, Mark Krystal
Publikováno v:
Viruses, Vol 16, Iss 10, p 1508 (2024)
The HIV-1 maturation inhibitor (MI) VH3739937 (VH-937) inhibits cleavage between capsid and spacer peptide 1 and exhibits an oral half-life in humans compatible with once-weekly dosing. Here, the antiviral properties of VH-937 are described. VH-937 e
Externí odkaz:
https://doaj.org/article/51872be0e27c430c8414ea5cea778b31
Autor:
Richard A. Hartz, Li Xu, Sing-Yuen Sit, Jie Chen, Brian L. Venables, Zeyu Lin, Sharon Zhang, Zhufang Li, Dawn Parker, Tara S. Simmons, Susan Jenkins, Umesh M. Hanumegowda, Ira Dicker, Mark Krystal, Nicholas A. Meanwell, Alicia Regueiro-Ren
Publikováno v:
Journal of Medicinal Chemistry. 65:15935-15966
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::50f57da166571042a230fdc9c14ab8fe
https://doi.org/10.1021/acs.jmedchem.2c01618
https://doi.org/10.1021/acs.jmedchem.2c01618
Autor:
Alicia Regueiro-Ren, Sing-Yuen Sit, Yan Chen, Jie Chen, Jacob J. Swidorski, Zheng Liu, Brian L. Venables, Ny Sin, Richard A. Hartz, Tricia Protack, Zeyu Lin, Sharon Zhang, Zhufang Li, Dauh-Rurng Wu, Peng Li, James Kempson, Xiaoping Hou, Anuradha Gupta, Richard Rampulla, Arvind Mathur, Hyunsoo Park, Amy Sarjeant, Yulia Benitex, Sandhya Rahematpura, Dawn Parker, Thomas Phillips, Roy Haskell, Susan Jenkins, Kenneth S. Santone, Mark Cockett, Umesh Hanumegowda, Ira Dicker, Nicholas A. Meanwell, Mark Krystal
Publikováno v:
Journal of medicinal chemistry. 65(18)
GSK3640254 is an HIV-1 maturation inhibitor (MI) that exhibits significantly improved antiviral activity toward a range of clinically relevant polymorphic variants with reduced sensitivity toward the second-generation MI GSK3532795 (BMS-955176). The
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cd326815d3682de3b91571d910517928
https://pubmed.ncbi.nlm.nih.gov/36044257
https://pubmed.ncbi.nlm.nih.gov/36044257
Autor:
Tricia Protack, Sing-Yuen Sit, Dieter M. Drexler, Alicia Regueiro-Ren, Mark I. Cockett, Yan Chen, Jerry Jeffrey, Nicholas A. Meanwell, Joseph L. Cantone, Ira B. Dicker, Martin Gartland, Mark Krystal, Zeyu Lin, Brian McAuliffe
Publikováno v:
Antimicrobial Agents and Chemotherapy
HIV-1 maturation inhibitors (MIs) offer a novel mechanism of action and potential for use in HIV-1 treatment. Prior MIs displayed clinical efficacy but were associated with the emergence of resistance and some gastrointestinal tolerability events. Tr
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::69ea10747ac645c2008b060f8062db2d
https://doi.org/10.1128/aac.01876-21
https://doi.org/10.1128/aac.01876-21
Autor:
Carolyn Diane Dzierba, Linda J. Bristow, Ramkumar Rajamani, Jie Chen, Rick L. Pieschl, Sing-Yuen Sit, Brian Lee Venables, Michele Matchett, Ronald J. Knox, Lorin A. Thompson, Nicholas A. Meanwell, Yong-Jin Wu, Jason M. Guernon, James Herrington
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 29:659-663
Screening of 100 acylsulfonamides from the Bristol-Myers Squibb compound collection identified the C3-cyclohexyl indole 6 as a potent Nav1.7 inhibitor. Replacement of the C2 furanyl ring of 6 with a heteroaryl moiety or truncation of this group led t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::2f347d20e2f2ebee9e7e423555c27787
https://doi.org/10.1016/j.bmcl.2018.12.013
https://doi.org/10.1016/j.bmcl.2018.12.013
Autor:
Umesh Hanumegowda, Sharon Zhang, Yan Chen, Zheng Liu, Ira B. Dicker, Zhufang Li, Sing-Yuen Sit, Ny Sin, Jacob Swidorski, Brian Terry, Himadri Samanta, Tricia Protack, Brian Lee Venables, Zeyu Lin, Yongnian Sun, Jie Chen, Beata Nowicka-Sans, Alicia Regueiro-Ren, Nicholas A. Meanwell, Matthew D. Healy, Mark Krystal, Mark I. Cockett
Publikováno v:
Antimicrobial Agents and Chemotherapy
BMS-955176 is a second-generation human immunodeficiency virus type 1 (HIV-1) maturation inhibitor (MI). A first-generation MI, bevirimat, showed clinical efficacy in early-phase studies, but ∼50% of subjects had viruses with reduced susceptibility
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::000fa48983f3b6ab685649499d7d0683
https://doi.org/10.1128/aac.02560-15
https://doi.org/10.1128/aac.02560-15
Autor:
Sing-Yuen Sit, Ny Sin, Umesh Hanumegowda, Dawn D. Parker, Zheng Liu, Alicia Regueiro-Ren, Xiaohua S. Huang, Brian Lee Venables, Brian Terry, Brett R. Beno, Sharon Zhang, Ira B. Dicker, Roy Haskell, Jacob Swidorski, Zhufang Li, Mark I. Cockett, Beata Nowicka-Sans, Zeyu Lin, Nicholas A. Meanwell, Tricia Protack, Sandhya Rahematpura, Juliang Zhu, Susan Jenkins, Himadri Samanta, Mark Krystal, Yan Chen, Kenneth S. Santone, Jie Chen
Publikováno v:
ACS Medicinal Chemistry Letters. 7:568-572
HIV-1 maturation inhibition (MI) has been clinically validated as an approach to the control of HIV-1 infection. However, identifying an MI with both broad polymorphic spectrum coverage and good oral exposure has been challenging. Herein, we describe
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::83c6472d1d93201556f25ce37013cceb
https://doi.org/10.1021/acsmedchemlett.6b00010
https://doi.org/10.1021/acsmedchemlett.6b00010
Autor:
Jacob Swidorski, Brian Lee Venables, Beata Nowicka-Sans, Sandhya Rahematpura, Zheng Liu, Ira B. Dicker, Jie Chen, Yan Chen, Brian Terry, Sing-Yuen Sit, Ny Sin, Umesh Hanumegowda, Tricia Protack, Susan Jenkins, Nicholas A. Meanwell, Dawn D. Parker, Alicia Regueiro-Ren, Mark Krystal
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:1925-1930
We have recently reported on the discovery of a C-3 benzoic acid (1) as a suitable replacement for the dimethyl succinate side chain of bevirimat (2), an HIV-1 maturation inhibitor that reached Phase II clinical trials before being discontinued. Rece
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a8197ac607d83b2abac46556d153b11e
https://doi.org/10.1016/j.bmcl.2016.03.019
https://doi.org/10.1016/j.bmcl.2016.03.019
Autor:
Yong-Jin, Wu, Brian, Venables, Jason, Guernon, Jie, Chen, Sing-Yuen, Sit, Ramkumar, Rajamani, Ronald J, Knox, Michele, Matchett, Rick L, Pieschl, James, Herrington, Linda J, Bristow, Nicholas A, Meanwell, Lorin A, Thompson, Carolyn, Dzierba
Publikováno v:
Bioorganicmedicinal chemistry letters. 29(4)
Screening of 100 acylsulfonamides from the Bristol-Myers Squibb compound collection identified the C3-cyclohexyl indole 6 as a potent Na
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::7e87a6b212eb6b55622d6c13aaa81742
https://pubmed.ncbi.nlm.nih.gov/30638874
https://pubmed.ncbi.nlm.nih.gov/30638874
Autor:
Alicia, Regueiro-Ren, Jacob J, Swidorski, Zheng, Liu, Yan, Chen, Ny, Sin, Sing-Yuen, Sit, Jie, Chen, Brian L, Venables, Juliang, Zhu, Beata, Nowicka-Sans, Tricia, Protack, Zeyu, Lin, Brian, Terry, Himadri, Samanta, Sharon, Zhang, Zhufang, Li, John, Easter, Brett R, Beno, Vinod, Arora, Xiaohua S, Huang, Sandhya, Rahematpura, Dawn D, Parker, Roy, Haskell, Kenneth S, Santone, Mark I, Cockett, Mark, Krystal, Nicholas A, Meanwell, Susan, Jenkins, Umesh, Hanumegowda, Ira B, Dicker
Publikováno v:
Journal of medicinal chemistry. 61(16)
GSK3532795, formerly known as BMS-955176 (1), is a potent, orally active, second-generation HIV-1 maturation inhibitor (MI) that advanced through phase IIb clinical trials. The careful design, selection, and evaluation of substituents appended to the
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::ec69348335bb02844efe70a17d779260
https://pubmed.ncbi.nlm.nih.gov/30067361
https://pubmed.ncbi.nlm.nih.gov/30067361