Zobrazeno 1 - 10
of 12
pro vyhledávání: '"Chester Chenguang Yuan"'
Autor:
Jeffrey Clarine, Qingyian Liu, Beth D. Youngblood, Chester Chenguang Yuan, Michelle Horner, James Brown, Jian J. Chen, Michael D. Bartberger, Vu Van Ma, Matthew R. Kaller, Carl D. Davis, Maosheng Zhang, Thomas T. Nguyen, Narender R. Gavva, Scott Harried, Sonya G. Lehto, Jennifer R. Allen, Holger Monenschein, Daniel B. Horne, Vijay Keshav Gore, Wenge Zhong, Kaustav Biswas
Publikováno v:
Journal of medicinal chemistry. 61(18)
Transient-receptor-potential melastatin 8 (TRPM8), the predominant mammalian cold-temperature thermosensor, is a nonselective cation channel expressed in a subpopulation of sensory neurons in the peripheral nervous system, including nerve circuitry i
Autor:
Qingyian Liu, Kaustav Biswas, Frank Koegler, Tiffany L. Correll, Toni Williamson, Jodi Bradley, Jennifer R. Allen, Leeanne Zalameda, Darren L. Reid, Michael D. Bartberger, Joe Zhu, Stephen J. Wood, Randy Hungate, Yichin Liu, Frank Chavez, Robert M. Rzasa, Jianhua Zhang, John D. McCarter, Thomas Nixey, Paul H. Wen, Li Zhu, Shannon Rumfelt, Yi Luo, Safura Babu-Khan, Stephen Hitchcock, Ning Chen, Mqhele Ncube, Wenyuan Qian, Frenel Fils Demorin, Dean Hickman, Christopher M. Tegley, Jian J. Chen, Albert Amegadzie, Charles W. Dean, Chester Chenguang Yuan
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:6447-6454
γ-Secretase modulators (GSMs) are potentially disease-modifying treatments for Alzheimer's disease. They selectively lower pathogenic Aβ42 levels by shifting the enzyme cleavage sites without inhibiting γ-secretase activity, possibly avoiding know
Autor:
David Chow, David J. St. Jean, Michelle Chen, Murielle M. Véniant, Xiping Zhang, Minghan Wang, Maurice Emery, Chester Chenguang Yuan, Renee Komorowski, Clarence Hale, Aiwen Li, Raju Subramanian, Christopher H. Fotsch
Publikováno v:
ACS Medicinal Chemistry Letters. 2:824-827
All eight of the major active metabolites of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221, compound 1), an inhibitor of 11β-hydroxysteroid dehydrogenase type 1 that has entered the clinic for the t
Autor:
Fang-Tsao Hong, Christopher H. Fotsch, Xianghong Wang, Qingping Zeng, John G. Allen, G. Erich Wohlhieter, Chun Li, Yihong Zhou, Guomin Yao, Seifu Tadesse, Matthew P. Bourbeau, Chester Chenguang Yuan, Sekhar Surapaneni, Matthew R. Lee, Gary L. Skiles, Raju Subramanian, Xiaochun Zhu
Publikováno v:
Chemical Research in Toxicology. 23:653-663
A 2-aminothiazole derivative 1 was developed as a potential inhibitor of the oncology target AKT, a serine/threonine kinase. When incubated in rat and human liver microsomes in the presence of NADPH, 1 underwent significant metabolic activation on it
Autor:
Minghan Wang, James Busby, James Zondlo, Chester Chenguang Yuan, Stephen W. Young, Shou-Hua Xiao, Ki Won Kim, Mei-Chu Lo, Harvey Yamane
Publikováno v:
Analytical Biochemistry. 376:122-130
Malonyl-CoA decarboxylase (MCD) catalyzes the conversion of malonyl-CoA to acetyl-CoA and thereby regulates malonyl-CoA levels in cells. Malonyl-CoA is a potent inhibitor of mitochondrial carnitine palmitoyltransferase-1, a key enzyme involved in the
Autor:
Maurice Emery, Rod Cupples, David J. St. Jean, George A. Moniz, David Pyring, Randall W. Hungate, Chester Chenguang Yuan, Lars Johansson, Aiwen Li, Michelle Chen, Qingyian Liu, Meredith Williams, Steven R. Jordan, Lynn Cai, Lars Tedenborg, Minghan Wang, Christopher H. Fotsch, Nianhe Han, Michael D. Bartberger, Jiandong Zhang, Clarence Hale, Yaxiong Sun, Ben C. Askew
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:6056-6061
A series of 2-anilinothiazolones were prepared as inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1). The most potent compounds contained a 2-chloro or 2-fluoro group on the aniline ring with an isopropyl substituent on the 5-posi
Autor:
Lynn Cai, Xiaohu Ouyang, Leon M. Smith, Sesha Neervannan, Chester Chenguang Yuan, Gondi N. Kumar, Tae-Seong Kim, Richard Kendall, Charles Starnes, Angela Coxon, Celia Dominguez, Joseph Kim, Anthony Polverino, Paul Chen, Timothy S. Harvey, Michael Zhang, Danlin Chen, Andrew Tasker, Rashid Syed, James Bready, Ling Wang, Qi Huang, Yongmei Gan
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:6003-6008
Inhibition of tumor-induced angiogenesis is a promising strategy in anticancer research. Neovascularization is a process required for both tumor growth and metastasis. Enhanced understanding of the underlying molecular mechanisms has led to the disco
Autor:
Burgess Laurence E, Leyla Arik, Chester Chenguang Yuan, Nianhe Han, Randall W. Hungate, Derin C. D'amico, David A. Mareska, Feng-Yin Hsieh, Eileen Johnson, Hong Sun, Qingyian Liu, Barton H. Manning, Bobby Riahi, Christopher H. Fotsch, Gloria Biddlecome, Mark H. Norman, Augustus Kamassah, Ming Huang, Richard Loeloff, Gondi N. Kumar, Andras Toro, Jian J. Chen, Jason Brooks Human, Hideo Suzuki, Robert D. Groneberg, Benny C. Askew, Aiwen Li, Gordon Ng, James Zhan, Kaustav Biswas, Dianna Lester-Zeiner, Hong Dong, David E. Clarke
Publikováno v:
Journal of Medicinal Chemistry. 50:2200-2212
The bradykinin B1 receptor is induced following tissue injury and/or inflammation. Antagonists of this receptor have been studied as promising candidates for treatment of chronic pain. We have identified aryl sulfonamides containing a chiral chroman
Autor:
Vinod F. Patel, Timothy Powers, Michael D. Bartberger, Ted Judd, Ryan White, Stephen J. Wood, Ana Elena Minatti, Stephen Hitchcock, Vijay Keshav Gore, Wenge Zhong, Hugo M. Vargas, Jason Brooks Human, Kui Chen, Steven Vonderfecht, Robert T. Fremeau, Robert T. Dunn, James Brown, Patricia Lopez, Qingyian Liu, Vu Van Ma, Nancy E. Everds, Matthew Weiss, Charles Kreiman, Oleg Epstein, May Xue, Chester Chenguang Yuan, Jonathan Werner, Alan C. Cheng, Jian J. Chen, Albert Amegadzie, Paul H. Wen, Yuan Cheng, Douglas A. Whittington, Wenyuan Qian, Isaac E. Marx, Thomas Dineen, Dean Hickman
Publikováno v:
Bioorganicmedicinal chemistry letters. 25(4)
The β-site amyloid precursor protein (APP) cleaving enzyme 1 (BACE1) is one of the most hotly pursued targets for the treatment of Alzheimer’s disease. We used a structure- and property-based drug design approach to identify 2-aminooxazoline 3-aza
Autor:
Harvey Yamane, Qingping Zeng, Celia Dominguez, Shiwen Zhang, Chun Li, Matthew P. Bourbeau, Suijin Yang, Christopher H. Fotsch, Douglas Hoffman, Randall W. Hungate, Xiaoling Zhang, Rider James Thomas, Matthew R. Lee, Daniel J. Freeman, Fang-Tsao Hong, Xin Huang, John G. Allen, Guomin Yao, Seifu Tadesse, Chester Chenguang Yuan, Xianghong Wang, Julie A. Lofgren, Elizabeth Tominey
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(5)
Through a combination of screening and structure-based rational design, we have discovered a series of N1-(5-(heterocyclyl)-thiazol-2-yl)-3-(4-trifluoromethylphenyl)-1,2-propanediamines that were developed into potent ATP competitive inhibitors of AK