Zobrazeno 1 - 10
of 27
pro vyhledávání: '"Elfatih Elzein"'
Publikováno v:
Regular and Young Investigator Award Abstracts.
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
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
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
Autor:
Dmitry O, Koltun, Eric Q, Parkhill, Elfatih, Elzein, Tetsuya, Kobayashi, Gregory T, Notte, Rao, Kalla, Robert H, Jiang, Xiaofen, Li, Thao D, Perry, Belem, Avila, Wei-Qun, Wang, Catherine, Smith-Maxwell, Arvinder K, Dhalla, Sridharan, Rajamani, Brian, Stafford, Jennifer, Tang, Nevena, Mollova, Luiz, Belardinelli, Jeff A, Zablocki
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:3202-3206
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
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
Autor:
Jeff A, Zablocki, Elfatih, Elzein, Xiaofen, Li, Dmitry O, Koltun, Eric Q, Parkhill, Tetsuya, Kobayashi, Ruben, Martinez, Britton, Corkey, Haibo, Jiang, Thao, Perry, Rao, Kalla, Gregory T, Notte, Oliver, Saunders, Michael, Graupe, Yafan, Lu, Chandru, Venkataramani, Juan, Guerrero, Jason, Perry, Mark, Osier, Robert, Strickley, Gongxin, Liu, Wei-Qun, Wang, Lufei, Hu, Xiao-Jun, Li, Nesrine, El-Bizri, Ryoko, Hirakawa, Kris, Kahlig, Cheng, Xie, Cindy Hong, Li, Arvinder K, Dhalla, Sridharan, Rajamani, Nevena, Mollova, Daniel, Soohoo, Eve-Irene, Lepist, Bernard, Murray, Gerry, Rhodes, Luiz, Belardinelli, Manoj C, Desai
Publikováno v:
Journal of medicinal chemistry. 59(19)
Late sodium current (late I
Autor:
Xiaofen Li, Rao Kalla, Art Gimbel, Thao Perry, Elfatih Elzein, Jeff Zablocki, Ming Yang, Dewan Zeng
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:1397-1401
A series of N-1 monosubstituted 8-pyrazolyl xanthines have been synthesized and evaluated for their affinity for the adenosine receptors (AdoRs). We have discovered two compounds 18 (CVT-7124) and 28 (CVT-6694) that display good affinity for the A(2B
Publikováno v:
Expert Opinion on Therapeutic Patents. 16:1347-1357
The intense efforts by many pharmaceutical companies and academics in the A2B adenosine receptor (AdoR) antagonist field are driven by the plethora of disease states where the A2B AdoR has been implicated to play a role: asthma, in which it mediates
Autor:
Kwan Leung, Ken Rehder, Xiaofen Li, Bob Jiang, Marie Nguyen, Timothy A. Marquart, Nancy Chu, Victoria Y. Maydanik, David Lustig, Kevin D. Shenk, Yuan Li, Elfatih Elzein, Reina Natero, Daniel Soohoo, Prabha Ibrahim, Jeff Zablocki, Suresh S. Kerwar, Dmitry Koltun, Jia Hao, Dewan Zeng
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:6017-6021
New inhibitors of palmitoyl-CoA oxidation are based on the introduction of nitrogen heterocycles in the ‘Western Portion’ of the molecule. SAR studies led to the discovery of CVT-4325 (shown), a potent FOXi (IC50 = 380 nM rat mitochondria) with f