Zobrazeno 1 - 10
of 16
pro vyhledávání: '"Zhihong O’Brien"'
Autor:
Bharat Majeti, Robiel Baclig, Wenbin Ying, Xiaoen Wang, Dhrubamitra Chatterjee, Hai Wang, Cima Cina, Jean-Pierre Clamme, J.-P. Jin, Jose Ibarra, Jennifer Daniels, Li Wang, Jens Harborth, James Chu, Zhihong O'Brien, James T. Lin
Publikováno v:
Cancer Research. 80:4060-4060
Pancreatic cancer is the third most common cause of death from cancer in the US. The disease has a poor prognosis with a five-year survival rate under 10%. Mutations in KRAS are driving tumor growth in about 95% of patients with pancreatic cancer. Cu
Publikováno v:
Expert Opinion on Drug Metabolism & Toxicology. 9:1597-1612
Fourteen drugs targeting protein kinases have been approved by the United States Food and Drug Administration (FDA) between the years 2000 and 2011. While the mechanisms of action and clinical data have been reported, the preclinical absorption, dist
Autor:
Robiel Baclig, Sonya Zabludoff, Steven Fong, James Chu, Jean-Pierre Clamme, Li Wang, Wenbin Ying, Jose Ibarra, Jens Harborth, Zhihong O'Brien, Clayton Zhang, Haiqing Yin, Roger Adami, Jing Yu, Bharat Majeti
Publikováno v:
Cancer Research. 78:5917-5917
Non-small cell lung cancer (NSCLC) accounts for about 85% of all lung cancers and KRAS mutation occurs in 25-30% of NSCLC. Therapeutics directly targeting KRAS mutant proteins are currently not available. We developed a novel siRNA therapeutic agains
Autor:
Wenbin Ying, Cima Cina, Zhihong O'Brien, J.-P. Jin, Nish Beltran-Raygoza, Jessica Xu, Sonya Zabludoff, Jens Harborth, Sang Jun Lee, Kwok Yin Tsang, Jiping Yao, Roger Adami
Publikováno v:
Cancer Research. 78:5918-5918
Lung cancer is the most common form of cancer worldwide and the leading cause of cancer-related deaths. Non-small cell lung cancer (NSCLC) accounts for approximately 85% of all lung cancers, and KRAS mutation occurs in 25-30% of NSCLC. However, to da
Autor:
Paul D. Crowe, Robert Farber, R. Colin Garner, Christopher F. O'Brien, Jianyun Wen, B. Oosterhuis, Ajay Madan, Zhihong O’Brien, Graham Lappin, Haig Bozigian, Graham Beaton
Publikováno v:
British Journal of Clinical Pharmacology. 67:288-298
AIMS: To evaluate the pharmacokinetics (PK) of five H1 receptor antagonists in human volunteers after a single oral and intravenous (i.v.) microdose (0.1 mg). METHODS: Five H1 receptor antagonists, namely NBI-1, NBI-2, NBI-3, NBI-4 and diphenhydramin
Autor:
Eric G. Vajda, Rob Hill, Kyoung-Jin Lee, Francisco J. López, Martin D. Meglasson, Yong-Hee Lee, William Y. Chang, Zhihong O'Brien, Yanling Chen, Peter J. Rix
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 328:663-670
Selective androgen receptor modulators (SARMs) are a new class of molecules in development to treat a variety of diseases. SARMs maintain the beneficial effects of androgens, including increased muscle mass and bone density, while having reduced acti
Autor:
John Saunders, Zhiqiang Guo, Xin-Jun Liu, Charles Q. Huang, Colin J. Loweth, Liren Zhao, R. Scott Struthers, Margaret J. Bradbury, Yun-Fei Zhu, James W. Behan, Stephen F. Betz, Neil J. Ashweek, Zhihong O’Brien, Marion Lanier, Jenny Wen, Mi Chen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:3845-3850
A novel series of 2-(4,5,6,7-tetrahydro-1H-pyrrolo[3,2-c]pyridin-3-yl)-ethylamine derivatives were designed and synthesized as GnRH receptor antagonists. SAR studies led to a series of highly active molecules against both the rat and human receptors.
Autor:
Ashutosh A. Kulkarni, Maria Bacolod, Mehran F. Moghaddam, Zhihong O’Brien, Samantha J. Richardson, Julius Apuy, Yang Tang, Prasoon Chaturedi
Publikováno v:
Drug metabolism letters. 8(1)
The in vitro and in vivo preclinical ADME properties of 10 clinically late stage or marketed covalent inhibitors were evaluated in order to define advancement criteria for discovery of future drugs in this arena. Our studies revealed the following: A
Autor:
Coon Timothy Richard, Raymond S. Gross, Siobhan Malany, Florence Jovic, Wilna J. Moree, Zhihong O’Brien, Sam R. J. Hoare, Paul D. Crowe, Fabio C. Tucci, Bin-Feng Li, Graham Beaton, Margaret J. Bradbury, Hua Wang, Jianyun Wen, Robert E. Petroski, Jinghua Yu, Aida Sacaan, Dragan Marinkovic, Lisa M. Hernández, Ajay Madan
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(7)
SAR of lead benzothiophene H1-antihistamine 2 was explored to identify backup candidates with suitable pharmacokinetic profiles for an insomnia program. Several potent and selective H1-antihistamines with a range of projected half-lives in humans wer
Autor:
Fabio C. Tucci, Lisa M. Hernández, Graham Beaton, Ajay Madan, Bin-Feng Li, Margaret J. Bradbury, Robert E. Petroski, Wilna J. Moree, Hua Wang, Dragan Marinkovic, Jinghua Yu, Jianyun Wen, Raymond S. Gross, Siobhan Malany, Florence Jovic, Paul D. Crowe, Said Zamani-Kord, Coon Timothy Richard, Zhihong O’Brien, Aida Sacaan, Sam R. J. Hoare
Publikováno v:
Journal of medicinal chemistry. 52(17)
Analogues of the known H(1)-antihistamine R-dimethindene were profiled as potential agents for the treatment of insomnia. Several highly selective compounds were efficacious in rodent sleep models. On the basis of overall profile, indene 1d and benzo