Zobrazeno 1 - 10
of 5 309
pro vyhledávání: '"Jian J. Chen"'
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
Publikováno v:
Tetrahedron Letters. 55:7229-7232
Four multiply halogenated azaxanthones 3, 4b, 5, and 6 were synthesized as novel core building blocks of β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors. Each of these heterocycles requires a specific synthetic strategy to cont
Autor:
Alexander J. Pickrell, Brian A. Lanman, Joon Won Jeong, Karen Rex, Anthony B. Reed, Jude Canon, Victor J. Cee, Hui-Ling Wang, Longbin Liu, Jian J. Chen, Anne Y. Saiki, Patricia Lopez, Pragathi Achanta, Laurie P. Volak, J. Russell Lipford, Daniel A. Erlanson, Christopher Mohr, Raymond V. Fucini
Publikováno v:
Cancer Research. 79:4455-4455
The RAS gene family encodes the small GTPase proteins NRAS, HRAS, and KRAS, which play an essential role in cellular growth and proliferation. KRAS is one of the most frequently mutated oncogenes in human cancer, with KRAS p.G12D, p.G12V, and p.G12C
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:
Smriti Joseph, Janan Jona, Jason Brooks Human, Leyla Arik, Gondi N. Kumar, Toshihiro Aya, Randall W. Hungate, Jian J. Chen, Kaustav Biswas, Tanya Peterkin, Jiawang Zhu, Zufan Wu, Wenyuan Qian, Hong-Xun Guo, Eileen Johnson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:1061-1067
In a series of bradykinin B1 antagonists, we discovered that replacement of oxopiperazine acetamides with dehydro-oxopiperazine acetamides provided compounds with enhanced activity against the B1 receptor. The synthesis and SAR leading to potent anal
Autor:
Randall W. Hungate, Ming Huang, Gloria Biddlecome, Jason Brooks Human, Benny C. Askew, Jian J. Chen, Dianna Lester-Zeiner, Eileen Johnson, Wenyuan Qian, Barton H. Manning, Leyla Arik, Richard Loeloff, Toshihiro Aya, Kaustav Biswas, Hong Dong, Tanya Peterkin, Hong Sun, Gondi N. Kumar
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:4764-4769
We report the development of aryl sulfones as Bradykinin B1 receptor antagonists. Variation of the linker region identified diol 23 as a potent B1 antagonist, while modifications of the aryl moiety led to compound 26, both of which were efficacious i
Autor:
Randall W. Hungate, Eileen Johnson, Kaustav Biswas, Leyla Arik, Benny C. Askew, Stephen Hitchcock, Vellarkad N. Viswanadhan, Wenyuan Qian, Jian J. Chen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:4477-4481
Replacement of the core beta-amino acid in our previously reported piperidine acetic acid and beta-phenylalanine-based Bradykinin B1 antagonists by dihydroquinoxalinone acetic acid increases the in vitro potency and metabolic stability. The most pote
Autor:
Xiao Ding, Jian J. Chen, Eileen Johnson, Hong Dong, Hong Sun, Gondi N. Kumar, Barton H. Manning, Ella Magal
Publikováno v:
Journal of Neuroscience Methods. 168:76-87
The discovery of novel analgesic compounds that target some receptors can be challenging due to species differences in ligand pharmacology. If a putative analgesic compound has markedly lower affinity for rodent versus other mammalian orthologs of a
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:
Andrew Tasker, Pedro J. Beltran, Darren L. Reid, Robert Radinsky, Jian J. Chen, Dina A. Andrews, David J. St. Jean, Keegan Cooke, Ryan Wurz, Tian Wu, Nataraj Kalyanaraman, Essa Hu-Harrington, Faye Hsieh, Simon J. Hedley, Kristin L. Andrews, Brad Herberich, Nancy E. Everds, Seifu Tadesse, Michele Kubryk, Jinghui Zhan, Jason S. Tedrow, Kate Ashton, Petia Mitchell, Andrew T. Parsons, Roberto E. Guzman, Liping H. Pettus, James Brown, Dean Hickman, Tom Nguyen, Matthew S. Potter, Edward K. Lobenhofer, David Bauer, Fang-Tsao Hong, Oliver R. Thiel
Publikováno v:
ACS medicinal chemistry letters. 6(9)
In nonsmall cell lung cancer (NSCLC), the threonine(790)-methionine(790) (T790M) point mutation of EGFR kinase is one of the leading causes of acquired resistance to the first generation tyrosine kinase inhibitors (TKIs), such as gefitinib and erloti