Zobrazeno 1 - 10
of 47
pro vyhledávání: '"Jeff Zablocki"'
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:
Wanchi Fung, Kobayashi Tetsuya, Anita Niedziela-Majka, Bob Jiang, Kim Jordan, Saritha Kusam, David G. Breckenridge, Hai Yang, Britton Kenneth Corkey, Kristyna Elbel, Chin Tay, Elaine Kan, Sammy Metobo, David Sperandio, Du Jinfa, Richard M. Neve, Sophia L. Shevick, Eric B. Lansdon, Kerim Babaoglu, Gregory Chin, Heather Webb, Debi Jin, Annapurna Sapre, Vangelis Aktoudianakis, Latesh Lad, Jamie Bates, Xiaowu Chen, Jeff Zablocki, Gene Eisenberg, Nate Larson, Richard L. Mackman, Martinez Ruben, Magdeleine Hung, Zachary Newby, Mish Michael R
Publikováno v:
Bioorganic & Medicinal Chemistry. 27:457-469
The bromodomain and extra-terminal (BET) family of proteins, consisting of the bromodomains containing protein 2 (BRD2), BRD3, BRD4, and the testis-specific BRDT, are key epigenetic regulators of gene transcription and has emerged as an attractive ta
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::32393d33e86182931fa91168f5389d3c
https://doi.org/10.1016/j.bmc.2018.11.020
https://doi.org/10.1016/j.bmc.2018.11.020
Publikováno v:
Journal of medicinal chemistry. 62(5)
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f68f9bf3e21e6a45fb87b5d09a5d8217
https://pubmed.ncbi.nlm.nih.gov/30667219
https://pubmed.ncbi.nlm.nih.gov/30667219
Autor:
Elfatih Elzein, Cindy Hong Li, Daniel Soohoo, Britton Kenneth Corkey, Chandru Venkataramani, Xiao-Jun Li, Manoj C. Desai, Nesrine El-Bizri, Haibo Jiang, Kobayashi Tetsuya, Nevena Mollova, Sridharan Rajamani, Jason K. Perry, Arvinder Dhalla, Thao Perry, Xiaofen Li, Robert G. Strickley, Notte Gregory, Gerry Rhodes, Ryoko Hirakawa, Luiz Belardinelli, Eve-Irene Lepist, Parkhill Eric Q, Jeff Zablocki, Oliver L. Saunders, Lu Yafan, Rao Kalla, Dmitry Koltun, Cheng Xie, Gongxin Liu, Wei-Qun Wang, Kris M. Kahlig, Bernard P. Murray, Michael Graupe, Guerrero Juan A, Martinez Ruben, Mark Osier, Lufei Hu
Publikováno v:
Journal of Medicinal Chemistry. 59:9005-9017
Late sodium current (late INa) is enhanced during ischemia by reactive oxygen species (ROS) modifying the Nav 1.5 channel, resulting in incomplete inactivation. Compound 4 (GS-6615, eleclazine) a novel, potent, and selective inhibitor of late INa, is
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::4d94b0c7942e17b573ee6f2bc8434003
https://doi.org/10.1021/acs.jmedchem.6b00939
https://doi.org/10.1021/acs.jmedchem.6b00939
Autor:
Donglin Guo, Nevena Mollova, Elfatih Elzein, Sridharan Rajamani, Nesrine El-Bizri, Gongxin Liu, Luiz Belardinelli, Kristopher M. Kahlig, Jeff Zablocki, Xiao-Liang Chen, Cindy Hong Li
Publikováno v:
British Journal of Pharmacology. 173:3088-3098
Background and Purpose Enhanced late Na+ current (late INa) in the myocardium is pro-arrhythmic. Inhibition of this current is a promising strategy to stabilize ventricular repolarization and suppress arrhythmias. Here, we describe GS-6615, a selecti
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::3f37746a20cc21acfbbbaa6363f39e04
https://doi.org/10.1111/bph.13563
https://doi.org/10.1111/bph.13563
Autor:
Elfatih Elzein, Kobayashi Tetsuya, Brian Stafford, Ryoko Hirakawa, Nevena Mollova, Sridharan Rajamani, Belem Avila, Catherine Smith-Maxwell, Thao Perry, Lin Wu, Jennifer Tang, Jeff Zablocki, Xiaofen Li, Wei-Qun Wang, Dmitry Koltun, Parkhill Eric Q, Robert Jiang, Arvinder Dhalla, Luiz Belardinelli
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:3207-3211
We started with a medium throughput screen of heterocyclic compounds without basic amine groups to avoid hERG and β-blocker activity and identified [1,2,4]triazolo[4,3-a]pyridine as an early lead. Optimization of substituents for Late INa current in
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::98fe40fe24221536f142ea4df6dd02ec
https://doi.org/10.1016/j.bmcl.2016.03.096
https://doi.org/10.1016/j.bmcl.2016.03.096
Autor:
Leanna Lagpacan, Christopher Allen Ziebenhaus, Bruno Marchand, Elfatih Elzein, Jason K. Perry, Bernard P. Murray, Scott Preston Simonovich, Parkhill Eric Q, Armando G. Villaseñor, WaiLok K. Hung, Nikos Pagratis, Rao Kalla, Jeff Zablocki, Dmitry Koltun, John R. Somoza, Timothy R. Hansen, Ron Aoyama, Thao Perry, Magdeleine Hung, Xiaofen Li
Publikováno v:
Bioorganicmedicinal chemistry letters. 28(3)
We hereby disclose the discovery of inhibitors of CaMKII (7h and 7i) that are highly potent in rat ventricular myocytes, selective against hERG and other off-target kinases, while possessing good CaMKII tissue isoform selectivity (cardiac γ/δ vs. n
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::caba80ce7be1413193b5f5243755c5aa
https://pubmed.ncbi.nlm.nih.gov/29254643
https://pubmed.ncbi.nlm.nih.gov/29254643
Autor:
William H. Parsons, James R. Walker, Jeff Zablocki, J. Du Bois, Vijay S. Pande, Malcolm McGregor, Paul Novick
Publikováno v:
Proceedings of the National Academy of Sciences. 109:18102-18107
Human nociceptive voltage-gated sodium channel (Na v 1.7), a target of significant interest for the development of antinociceptive agents, is blocked by low nanomolar concentrations of (−)-tetrodotoxin(TTX) but not (+)-saxitoxin (STX) and (+)-gonya
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::20e9178c410efbae36c794cb1a4abf71
https://doi.org/10.1073/pnas.1206952109
https://doi.org/10.1073/pnas.1206952109
Autor:
Serge Karpinski, Sridharan Rajamani, Dmitry Koltun, Wei-Qun Wang, Cathy Smith-Maxwell, Nesrine El-Bizri, Lina Yao, William J. Crumb, Xiao-Jun Li, John C. Shryock, Arvinder Dhalla, Luiz Belardinelli, Lufei Hu, Cindy Hong Li, Gongxin Liu, Ryoko Hirakawa, Lin Wu, Jeff Zablocki
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 344:23-32
Inhibition of cardiac late sodium current (late I(Na)) is a strategy to suppress arrhythmias and sodium-dependent calcium overload associated with myocardial ischemia and heart failure. Current inhibitors of late I(Na) are unselective and can be proa
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8baa8f90713bb06ec124c0e561de524c
https://doi.org/10.1124/jpet.112.198887
https://doi.org/10.1124/jpet.112.198887
Autor:
Brent Blackburn, Maria Pia Arolfo, Jeff Zablocki, Hee Yong Kim, Kwan Leung, Nancy Chu, Lina Yao, Jeongrim Lee, Zhan Jiang, Hai Ling Sun, Peidong Fan, Ivan Diamond, John C. Shryock, M. Foster Olive
Publikováno v:
Nature Medicine. 16:1024-1028
There is no effective treatment for cocaine addiction despite extensive knowledge of the neurobiology of drug addiction. Here we show that a selective aldehyde dehydrogenase-2 (ALDH-2) inhibitor, ALDH2i, suppresses cocaine self-administration in rats
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1ff8a25a0c731e4c6712ffad8dfcb240
https://doi.org/10.1038/nm.2200
https://doi.org/10.1038/nm.2200