Zobrazeno 1 - 10
of 34
pro vyhledávání: '"Brian E Schultz"'
Autor:
Weimei Xing, Ona Barauskas, Thorsten Kirschberg, Anita Niedziela-Majka, Michael Clarke, Gabriel Birkus, Perry Weissburg, Xiaohong Liu, Brian E Schultz, Roman Sakowicz, HyockJoo Kwon, Joy Y Feng
Publikováno v:
PLoS ONE, Vol 12, Iss 8, p e0181969 (2017)
Influenza polymerase is a heterotrimer composed of polymerase acidic protein A (PA) and basic proteins 1 (PB1) and 2 (PB2). The endonuclease active site, located in the PA subunit, cleaves host mRNA to prime viral mRNA transcription, and is essential
Externí odkaz:
https://doaj.org/article/214d6c14bef247f8a2cf1c7bae8f111c
Autor:
Ona Barauskas, Weimei Xing, Esmeralda Aguayo, Madeleine Willkom, Annapurna Sapre, Michael Clarke, Gabriel Birkus, Brian E Schultz, Roman Sakowicz, HyockJoo Kwon, Joy Y Feng
Publikováno v:
PLoS ONE, Vol 12, Iss 10, p e0185998 (2017)
Influenza polymerase is a heterotrimer protein with both endonuclease and RNA-dependent RNA polymerase (RdRp) activity. It plays a critical role in viral RNA replication and transcription and has been targeted for antiviral drug development. In this
Externí odkaz:
https://doaj.org/article/8ed1d422bf5149b8833aef2a4805c888
Autor:
Yili Xu, Brian E. Schultz, Daniel Soohoo, Raju Subramanian, John P. Bilello, Ruidong Li, Darius Babusis, Jingyu Zhang, Cynthia Kim, Eisuke Murakami, Bill J. Smith, Jing Zou, Qin Yue, Roman Sakowicz, Congrong Niu, Joy Y. Feng, Jared Pitts, Li Li, Bin Ma, Xiaofeng Zhao, Xuping Xie, Bernard P. Murray, Albert Liclican, Pei Yong Shi
Publikováno v:
Antimicrobial Agents and Chemotherapy
Remdesivir (RDV; GS-5734, Veklury), the first FDA-approved antiviral to treat COVID-19, is a single-diastereomer monophosphoramidate prodrug of an adenosine analogue. RDV is taken up in the target cells and metabolized in multiple steps to form the a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5e65d9cff18affdae94d721eea0e4267
https://doi.org/10.1128/aac.00602-21
https://doi.org/10.1128/aac.00602-21
Autor:
Kyla Ramey, Katana Ashley Anne, Kato Darryl, Tran Chinh Viet, Cheng Y. Yang, Link John O, Debi Jin, Yujin Wang, Kobayashi Tetsuya, Karki Kapil Kumar, Armando G. Villaseñor, Todd C. Appleby, Kelly Wang, Sangi Michael, Jeff Zablocki, Randy Vivian, Brian E. Schultz, Yang Zheng-Yu, Guofeng Cheng, Dustin Siegel, Zipfel Sheila, Ona Barauskas, James G. Taylor, Martinez Ruben, Katie Chan, Adam J. Schrier
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 29:2428-2436
Treatment of hepatitis C virus (HCV) infection has been historically challenging due the high viral genetic complexity wherein there are eight distinct genotypes and at least 86 viral subtypes. While HCV NS3/4A protease inhibitors are an established
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::210d14a9952795cbbb25c9ee4809cc66
https://doi.org/10.1016/j.bmcl.2019.03.037
https://doi.org/10.1016/j.bmcl.2019.03.037
Autor:
Jiri Vlach, Alexandra B. Samal, Anita Niedziela-Majka, Michael V. Lee, Giuseppe A. Papalia, Melanie H. Wong, Katherine M. Brendza, Brian E. Schultz, Dmitry O. Koltun, Hyock Joo Kwon, Joy Y. Feng, Roman Sakowicz, Nikolai Novikov, Jamil S. Saad
Publikováno v:
Journal of Molecular Biology. 431:1440-1459
Calcium/calmodulin-dependent protein kinase II (CaMKII) is a multifunctional serine/threonine protein kinase that transmits calcium signals in various cellular processes. CaMKII is activated by calcium-bound calmodulin (Ca2+/CaM) through a direct bin
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::66ee4acd312eda128004cfb016e9d735
https://doi.org/10.1016/j.jmb.2019.02.001
https://doi.org/10.1016/j.jmb.2019.02.001
Autor:
Roy Bannister, George Stepan, Yili Xu, Roman Sakowicz, Michel Perron, Ona Barauskas, Eisuke Murakami, Cynthia Kim, Tomas Cihlar, Brian E. Schultz, Dmytro Kornyeyev, Gary Lee, Danielle P. Porter, Joy Y. Feng, Darius Babusis
Publikováno v:
Antimicrobial Agents and Chemotherapy
Remdesivir (RDV, GS-5734), the first FDA-approved antiviral for the treatment of COVID-19, is a single diastereomer monophosphoramidate prodrug of an adenosine analogue. It is intracellularly metabolized into the active triphosphate form, which in tu
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::09e35e6af2becb2fd0246022ee451bdc
https://doi.org/10.1128/aac.02237-20
https://doi.org/10.1128/aac.02237-20
Autor:
Jean-Yves Christophe Chiva, Peter Pyun, Andrew John Keats, Linos Lazarides, Karine G. Poullennec, Neil Andrew Dunbar, Brian E. Schultz, Mingzhe Ji, Gregory M. Watt, Karki Kapil Kumar, Ruby Cai, Carina E. Cannizzaro, Uli Schmitz, David Kenneth Dean, Yu-Jen Lee, Sangi Michael, Victoria Alexandra Steadman, Adam J. Schrier, Simon B. Pettit, Hans G. Fliri, Adrian John Highton, Todd C. Appleby, Carol Austin, Richard L. Mackman, Caroline A. Blakemore, Hui Hon Chung, Dustin Siegel, Gregory Chin, Bernard P. Murray, Hai Yang, Yang Tian, George Stepan, Jonathan Sanvoisin, Albert Liclican, Mish Michael R, David Sperandio, Rex Santos, Petr Jansa, Haolun Jin
Publikováno v:
Journal of Medicinal Chemistry. 61:9473-9499
Cyclophilins are a family of peptidyl-prolyl isomerases that are implicated in a wide range of diseases including hepatitis C. Our aim was to discover through total synthesis an orally bioavailable, non-immunosuppressive cyclophilin (Cyp) inhibitor w
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f349698a38c7c9924d318620a6fcc5d2
https://doi.org/10.1021/acs.jmedchem.8b00802
https://doi.org/10.1021/acs.jmedchem.8b00802
Autor:
David G. Breckenridge, Laurie A. Castonguay, Giuseppe A. Papalia, Swetha Pendem, Shawn S. Badal, Ford Hinojosa-Kirschenbaum, Gregory T. Notte, Sarah Wise, Michael V. Lee, Keith A. Koch, Agnes B. Fogo, Dorothy French, Britton Kenneth Corkey, Frank Y. Ma, Brian E. Schultz, Eric B. Lansdon, Melanie H. Wong, David J. Nikolic-Paterson, Tareq M Al-Tuhaifi, Theodore Sullivan, Michael Graupe, Haichun Yang, Erik Huntzicker, Grant R. Budas, John T. Liles
Publikováno v:
Journal of Clinical Investigation. 128:4485-4500
Oxidative stress is an underlying component of acute and chronic kidney disease. Apoptosis signal–regulating kinase 1 (ASK1) is a widely expressed redox-sensitive serine threonine kinase that activates p38 and c-Jun N-terminal kinase (JNK) mitogen-
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::38b037ace289b522c4f72e5fa892d048
https://doi.org/10.1172/jci99768
https://doi.org/10.1172/jci99768
Autor:
Yu-Jen Lee, Andrew John Keats, Karine G. Poullennec, Uli Schmitz, Todd C. Appleby, Hans G. Fliri, Linos Lazarides, Albert Liclican, Steven J. Stanway, David Kenneth Dean, Debi Jin, Victoria Alexandra Steadman, Simon B. Pettit, Stephanie A. Leavitt, Yang Tian, Jonathan Sanvoisin, Petr Jansa, Brian E. Schultz, Christian R. Frey, Melanie H. Wong, Gregory M. Watt, Richard L. Mackman, Carol Austin
Publikováno v:
Journal of Medicinal Chemistry. 60:1000-1017
Cyclophilin inhibition has been a target for the treatment of hepatitis C and other diseases, but the generation of potent, drug-like molecules through chemical synthesis has been challenging. In this study, a set of macrocyclic cyclophilin inhibitor
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::091df6df2743a293d5a795f54f7981a6
https://doi.org/10.1021/acs.jmedchem.6b01329
https://doi.org/10.1021/acs.jmedchem.6b01329
Discovery of Potent and Selective MTH1 Inhibitors for Oncology: Enabling Rapid Target (In)Validation
Autor:
Julie Farand, Jeffrey E. Kropf, Peter Blomgren, Jianjun Xu, Aaron C. Schmitt, Zachary E. Newby, Ting Wang, Eisuke Murakami, Ona Barauskas, Jawahar Sudhamsu, Joy Y. Feng, Anita Niedziela-Majka, Brian E. Schultz, Karen Schwartz, Serge Viatchenko-Karpinski, Dmytro Kornyeyev, Adam Kashishian, Peidong Fan, Xiaowu Chen, Eric B. Lansdon, Michael O. Ports, Kevin S. Currie, William J. Watkins, Gregory T. Notte
Publikováno v:
ACS Med Chem Lett
[Image: see text] We describe the discovery of three structurally differentiated potent and selective MTH1 inhibitors and their subsequent use to investigate MTH1 as an oncology target, culminating in target (in)validation. Tetrahydronaphthyridine 5
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8a8664fe5cf60201d9c5d872c2fbdf25
https://europepmc.org/articles/PMC7074220/
https://europepmc.org/articles/PMC7074220/
