Zobrazeno 1 - 10
of 49
pro vyhledávání: '"Paul Falk"'
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:
Kyle Parcella, Tao Wang, Kyle Eastman, Zhongxing Zhang, Zhiwei Yin, Manoj Patel, Yong Tu, Barbara Zhizhen Zheng, Michael A. Walker, Mark G. Saulnier, David Frennesson, Michael Bowsher, Eric Gillis, Kevin Peese, Makonen Belema, Christopher Cianci, Ira B. Dicker, Brian McAuliffe, Bo Ding, Paul Falk, Jean Simmermacher, Dawn D. Parker, Prasanna Sivaprakasam, Kevin Kish, Hal Lewis, Umesh Hanumegowda, Susan Jenkins, John F. Kadow, Mark Krystal, Nicholas A. Meanwell, B. Narasimhulu Naidu
Publikováno v:
ACS Med Chem Lett
[Image: see text] Allosteric HIV-1 integrase inhibitors (ALLINIs) have been of interest recently because of their novel mechanism of action. Strategic modifications to the C5 moiety of a class of 4-(4,4-dimethylpiperidinyl)-2,6-dimethylpyridinyl ALLI
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1ef219ff3295f925d0de0c18dbd1bec7
https://europepmc.org/articles/PMC9190037/
https://europepmc.org/articles/PMC9190037/
Autor:
Nicholas A. Meanwell, Ravi Kumar Trivedi, Tatyana Zvyaga, Richard Rampulla, Sarkunam Kandhasamy, Debarati Mazumder Tagore, Sureshbabu Vishwakrishnan, Arvind Mathur, Sunitha Puttaswamy, Abhijith Rao, Hua Fang, Sankar Sivaprasad, Susan Jenkins, Eric Mull, Kathy Mosure, Kaushik Ghosh, Barbara Zheng, Subba Reddy, Fiona McPhee, Chaoqun Chen, Bowsher Michael S, James Loy, Ying-Kai Wang, Amit Kumar, Ramkumar Rajamani, Kishore Rendunchintala, Paul Michael Scola, Gillis Eric P, Salil D. Desai, Li-Qiang Sun, Rushith Kumar Anumula, Nagalakshmi Pulicharla, Sheldon Hiebert, Venkata Rao Baratam, Paul Falk, Sarmistha Sinha, Stanley D'andrea
Publikováno v:
Journal of Medicinal Chemistry. 63:14740-14760
The discovery of a pan-genotypic hepatitis C virus (HCV) NS3/4A protease inhibitor based on a P1–P3 macrocyclic tripeptide motif is described. The all-carbon tether linking the P1–P3 subsites of 21...
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f9fae1c3f9b157cd2f44f9613c2d3455
https://doi.org/10.1021/acs.jmedchem.0c01296
https://doi.org/10.1021/acs.jmedchem.0c01296
Autor:
Kyle Parcella, Manoj Patel, Yong Tu, Kyle Eastman, Kevin Peese, Eric Gillis, Ira Dicker, Brian McAuliffe, Bo Ding, Paul Falk, Jean Simmermacher, Dawn Parker, Prasanna Sivaprakasam, Javed Khan, Kevin Kish, Hal Lewis, Umesh Hanumegowda, Susan Jenkins, John Kadow, Mark Krystal, Nicholas Meanwell, B. Narasimhulu Naidu
Publikováno v:
SSRN Electronic Journal.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::fb46a6a57e400e71e40d1517de5ec5cd
https://doi.org/10.2139/ssrn.4063473
https://doi.org/10.2139/ssrn.4063473
Autor:
Kyle Parcella, Manoj Patel, Yong Tu, Kyle Eastman, Kevin Peese, Eric Gillis, Makonen Belema, Ira B. Dicker, Brian McAuliffe, Bo Ding, Paul Falk, Jean Simmermacher, Dawn D. Parker, Prasanna Sivaprakasam, Javed A. Khan, Kevin Kish, Hal Lewis, Umesh Hanumegowda, Susan Jenkins, John F. Kadow, Mark Krystal, Nicholas A. Meanwell, B. Narasimhulu Naidu
Publikováno v:
Bioorganic & Medicinal Chemistry. 67:116833
Allosteric integrase inhibitors (ALLINIs) of HIV-1 may hold promise as a novel mechanism for HIV therapeutics and cure. Scaffold modifications to the 4-(4,4-dimethylpiperidinyl) 2,6-dimethylpyridinyl class of ALLINIs provided a series of potent compo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3e022b9484eaf5af0acf5fbe2eef0aed
https://doi.org/10.1016/j.bmc.2022.116833
https://doi.org/10.1016/j.bmc.2022.116833
Autor:
Paul Falk, Alexandra Thiry, Fiona McPhee, Ronald E. Rose, Karen Ericson, Dennis Hernandez, Nannan Zhou
Publikováno v:
Hepatology Communications
Hepatology Communications, Vol 2, Iss 9, Pp 1123-1135 (2018)
Hepatology Communications, Vol 2, Iss 9, Pp 1123-1135 (2018)
Entecavir (ETV) is a first‐line therapy for chronic hepatitis B virus (HBV), demonstrating potent suppression of HBV DNA and a high barrier to viral resistance. Previous studies revealed that ETV‐resistant (ETVr) HBV DNA resulted from substitutio
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6439e4a8688ba3c64c928457bdd80a8d
https://doi.org/10.1002/hep4.1231
https://doi.org/10.1002/hep4.1231
Autor:
Alan Xiangdong Wang, Andrew C. Good, Fei Yu, Peter Hrnciar, Herbert E. Klei, Manjula Paruchuri, Fiona McPhee, Dennis Hernandez, Paul Falk, Jeffrey Tredup, Amy K. Sheaffer, Qi Gao, Barbara Zheng, Kevin Kish, Kathy Mosure, Stanley D'andrea, Ramkumar Rajamani, Alicia Ng, Jay O. Knipe, Yan Chen, Li-Qiang Sun, Jacques Friborg, Paul Michael Scola, Arvind Mathur, Nicholas A. Meanwell, Richard Rampulla
The design and synthesis of potent, tripeptidic acylsulfonamide inhibitors of HCV NS3 protease that contain a difluoromethyl cyclopropyl amino acid at P1 are described. A cocrystal structure of 18 with a NS3/4A protease complex suggests the presence
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::deb2005e8a0764575ac7a4f49607aedd
https://europepmc.org/articles/PMC5807875/
https://europepmc.org/articles/PMC5807875/
Autor:
Danshi Li, Herbert E. Klei, Sing-Yuen Sit, Piyasena Hewawasam, Ny Sin, Brian Lee Venables, Paul Levesque, Qi Gao, Bilder Donna M, Dennis M. Grasela, Dennis Hernandez, Anthony J. Cocuzza, Amy K. Sheaffer, Richard J. Colonno, Jeffrey Tredup, Kathy Mosure, Stanley D'andrea, Jialong Zhu, Lucy Sun, Fei Yu, Paul Falk, Alan Xiangdong Wang, Steven Levine, Fiona McPhee, Andrew C. Good, Huabin Sun, Jay O. Knipe, Barbara Zheng, Richard Schartman, Nicholas A. Meanwell, Jie Chen, Maria Donoso, James Loy, Guangzhi Zhai, Ramkumar Rajamani, Li-Qiang Sun, Stephen P. Adams, Luciano Mueller, Tatyana Zvyaga, Yong Tu, Hong Shi, Paul Michael Scola, Chaoqun Chen, William Warner, Yan Chen, Yong-Hae Han, Diana Barry, Jacques Friborg, Kevin Kish, Michael Sinz
Publikováno v:
Journal of Medicinal Chemistry. 57:1730-1752
The discovery of asunaprevir (BMS-650032, 24) is described. This tripeptidic acylsulfonamide inhibitor of the NS3/4A enzyme is currently in phase III clinical trials for the treatment of hepatitis C virus infection. The discovery of 24 was enabled by
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2de12395392456b92810af925e724113
https://doi.org/10.1021/jm500297k
https://doi.org/10.1021/jm500297k
Autor:
Alan Xiangdong Wang, Barbara Zheng, Min S. Lee, Dennis Hernandez, Andrew C. Good, Stanley D'andrea, Amy K. Sheaffer, Fiona McPhee, Christoph Gesenberg, Sing-Yuen Sit, Ny Sin, Paul Falk, Danshi Li, Piyasena Hewawasam, Yan Chen, Yong-Hae Han, Paul Levesque, Brian Lee Venables, Nicholas A. Meanwell, Michael Sinz, Wenying Li, Qi Gao, Li-Qiang Sun, Jay O. Knipe, Chaoqun Chen, Caly Chien, Diana Barry, Guangzhi Zhai, Anthony J. Cocuzza, Tatyana Zvyaga, Stephen P. Adams, Jialong Zhu, Fei Yu, Dennis M. Grasela, Richard J. Colonno, Yong Tu, Ramkumar Rajamani, Herbert E. Klei, Jianqing Li, Min Ding, Jan Willem Thuring, Jie Chen, Susan Jenkins, Keith D. Combrink, Jeffrey Allen Campbell, Kenneth S. Santone, Paul Michael Scola, Eric Hughes, Bilder Donna M
Publikováno v:
Journal of Medicinal Chemistry. 57:1708-1729
The discovery of BMS-605339 (35), a tripeptidic inhibitor of the NS3/4A enzyme, is described. This compound incorporates a cyclopropylacylsulfonamide moiety that was designed to improve the potency of carboxylic acid prototypes through the introducti
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4bf8154b804898acc5dffe118ba07d84
https://doi.org/10.1021/jm401840s
https://doi.org/10.1021/jm401840s
Autor:
Dennis Hernandez, Arlene Carifa, Timothy Eley, Robert A. Fridell, Nannan Zhou, Aaron Monikowski, Paul Falk, Fei Yu, Chunfu Wang, Fiona McPhee, David F. Gardiner, Joseph Ueland
Publikováno v:
Hepatology. 58:902-911
In a sentinel cohort, hepatitis C virus (HCV) patients (primarily genotype [GT] 1a) were treated with daclatasvir (NS5A inhibitor) and asunaprevir (NS3 protease inhibitor). Preexistence, emergence, and persistence of resistance variants in patients w
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b455879e98f3cbdffc5838b07ead987b
https://doi.org/10.1002/hep.26388
https://doi.org/10.1002/hep.26388