Zobrazeno 1 - 10
of 14
pro vyhledávání: '"Tran Khanh Tuan"'
Autor:
Kephart Susan Elizabeth, Tran Khanh Tuan, Kevin Daniel Freeman-Cook, Sherry Niessen, James Solowiej, Buwen Huang, Qin Zhang, Douglas Carl Behenna, Inish O'Doherty, Sacha Ninkovic, Rose Ann Ferre, Andrea Hui, Nichol Miller, Jordan Carelli, Lisa Nguyen, Brion W. Murray, Robert Louis Hoffman, John Lapek, Rhys M. Jones, Meirong Xu, Stephen Dann, Sutton Scott Channing, Asako Nagata, Nanni Huser, Ravi Visswanathan, Zehnder Luke Raymond, Elaine E. Tseng, Britton Boras, You-Ai He, Michele McTigue, Wade Diehl, Cathy Zhang, Martha A. Ornelas
Publikováno v:
Journal of medicinal chemistry. 64(13)
Control of the cell cycle through selective pharmacological inhibition of CDK4/6 has proven beneficial in the treatment of breast cancer. Extending this level of control to additional cell cycle CDK isoforms represents an opportunity to expand to add
Autor:
Ben Bolaňos, Sherry Niessen, Martha A. Ornelas, Paulina Delgado Cuenca, Douglas Carl Behenna, Lawrence G. Lum, Prakash B. Palde, Tran Khanh Tuan, Kevin Ryan, Stephen Kaiser, Marissa Smith, Lianglin Zhang, Todd VanArsdale, Al Stewart, Ketan S. Gajiwala
Publikováno v:
The Journal of Biological Chemistry
Poly-ADP-ribosyltransferases play a critical role in DNA repair and cell death, and poly(ADP-ribosyl) polymerase 1 (PARP1) is a particularly important therapeutic target for the treatment of breast cancer because of its synthetic lethal relationship
Autor:
Xinmeng Jasmine Mu, Meirong Xu, Shahram Salek-Ardakani, Cinthia Costa-Jones, Lisa Nguyen, James Solowiej, David Looper, Scott L. Weinrich, Robert Louis Hoffman, Sutton Scott Channing, Sacha Ninkovic, Kephart Susan Elizabeth, Sherry Niessen, John Chionis, Jadwiga Bienkowska, Kevin Daniel Freeman-Cook, Rose Ann Ferre, John Lapek, Cecilia Oderup, Jordan Carelli, Cathy Zhang, Nanni Huser, Elizabeth A. McMillan, Asako Nagata, Martha A. Ornelas, Brion W. Murray, Douglas Carl Behenna, Koleen Eisele, Todd VanArsdale, Zhou Zhu, Zhengyan Kan, Chaoting Liu, Nichol Miller, Zehnder Luke Raymond, Michael A. White, Ying Ding, Nathan V. Lee, Jonathan Almaden, Qin Zhang, Tran Khanh Tuan, Ping Wei, Stephen Dann, Britton Boras, Tim S. Wang, Ravi Visswanathan, You-Ai He, Michele McTigue, Elizabeth Wilson
Publikováno v:
Cancer Cell. 39:1404-1421.e11
Summary The CDK4/6 inhibitor, palbociclib (PAL), significantly improves progression-free survival in HR+/HER2− breast cancer when combined with anti-hormonals. We sought to discover PAL resistance mechanisms in preclinical models and through analys
Autor:
Chengyi Zhang, Sujin Cho-Schultz, Tran Khanh Tuan, Manli Shi, Rose Ann Ferre, Sherry Niessen, Sajiv Krishnan Nair, Douglas Carl Behenna, Dac M. Dinh, Elaine E. Tseng, Theodore O. Johnson, Cheng Hengmiao, Ru Zhou, Michael Zientek, T. Eric Ballard, Brion W. Murray, Suvi T. M. Orr, James Solowiej, Jennifer Lafontaine, Jean Joo Matthews, Scott L. Weinrich, Paolo Vicini, Deal Judith G, Longqing Liu, John Charles Kath, Pairish Mason Alan, Simon Paul Planken, Louise Bernier, Deepak Dalvie, Yiqin Luo, Martin Paul Edwards, Asako Nagata, Hong Shen, Neal W. Sach, Yuli Wang, Ketan S. Gajiwala, Shuibo Xin, Simon Bailey, Chau Almaden, Robert Steven Kania, Michelle Hemkens
Publikováno v:
Journal of Medicinal Chemistry. 60:3002-3019
Mutant epidermal growth factor receptor (EGFR) is a major driver of non-small-cell lung cancer (NSCLC). Marketed first generation inhibitors, such as erlotinib, effect a transient beneficial response in EGFR mutant NSCLC patients before resistance me
Autor:
Marlena Walls, Tod Smeal, Suvi T. M. Orr, Zhengyu Liu, Cheng Hengmiao, Shuiwang Wang, Kephart Susan Elizabeth, Jean Joo Matthews, Rose Ann Ferre, Neal W. Sach, Scott L. Weinrich, Doug Behenna, Sherry Niessen, Sangita M. Baxi, Deepak Dalvie, Sujin Cho-Schultz, Dac M. Dinh, Kevin Ryan, Jim Solowiej, Elaine E. Tseng, Simon Paul Planken, Sajiv Krishnan Nair, Brion W. Murray, Jun Li Feng, Jennifer Lafontaine, Pairish Mason Alan, Shijian Ren, Michelle Hemkens, Shuibo Xin, Mehran Jalaie, Tran Khanh Tuan, Robert Steven Kania, Sutton Scott Channing, William F. Vernier, Kevin K.-C. Liu, Amy Jackson-Fisher, Beth Lunney, Min-Jean Yin, Ketan S. Gajiwala, Asako Nagata, Haiwei Xu, Michael Zientek, Ru Zhou, Daniel Tyler Richter, Simon Bailey, Martin Paul Edwards, Martha A. Ornelas, Chau Almaden, John Charles Kath, Hong Shen, Theodore O. Johnson
Publikováno v:
Journal of Medicinal Chemistry. 59:2005-2024
First generation EGFR TKIs (gefitinib, erlotinib) provide significant clinical benefit for NSCLC cancer patients with oncogenic EGFR mutations. Ultimately, these patients’ disease progresses, often driven by a second-site mutation in the EGFR kinas
Autor:
Tran Khanh Tuan, Qiyue Hu, Zhang Junhu, Scott L. Butler, Atsuo Kuki, Qinghai Peng, Erik Jon Flahive, Graham L. Smith, Huichun Zhu, Deepak Dalvie, Plewe Michael Bruno, Jim Solowiej, Dorothy Delisle, Ted William Johnson, Wen Liu, Steven P. Tanis, Klaus Ruprecht Dress, Jon E. Kuehler, Guy A. McClellan, Xiaoming Yu, Hai Wang, Paul F. Richardson
Publikováno v:
Journal of Medicinal Chemistry. 54:3393-3417
HIV-1 integrase (IN) is one of three enzymes encoded by the HIV genome and is essential for viral replication, and HIV-1 IN inhibitors have emerged as a new promising class of therapeutics. Recently, we reported the synthesis of orally bioavailable a
Autor:
Qinghai Peng, Tran Khanh Tuan, Atsuo Kuki, Steven P. Tanis, Zhang Junhu, Deepak Dalvie, Yang Anle, Xiaoming Yu, Jim Solowiej, Ted William Johnson, Hai Wang, Wen Liu, Plewe Michael Bruno, Buwen Huang, Graham L. Smith, Jon E. Kuehler, Klaus Ruprecht Dress, Chunfeng Yin, Qiyue Hu, Dorothy Delisle, Huichun Zhu, Scott L. Butler
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:7429-7434
HIV-1 integrase is one of three enzymes encoded by the HIV genome and is essential for viral replication, and HIV-1 IN inhibitors have emerged as a new promising class of therapeutics. Recently, we reported the discovery of azaindole hydroxamic acids
Autor:
Qinghai Peng, Nowlin Dawn Marie, Hieu Lam, Ted William Johnson, Yang Anle, Wen Liu, Atsuo Kuki, Steven P. Tanis, Jon E. Kuehler, Zhang Junhu, Hai Wang, Plewe Michael Bruno, Scott L. Butler, Tran Khanh Tuan, Qiyue Hu, Sadayappan V. Rahavendran, Klaus Ruprecht Dress
Publikováno v:
Journal of Medicinal Chemistry. 52:7211-7219
HIV-1 integrase (IN) is one of three enzymes encoded by the HIV genome and is essential for viral replication. Recently, HIV-1 IN inhibitors have emerged as a new promising class of therapeutics. Herein, we report the discovery of azaindole carboxyli
Autor:
Murphy Sean T, Gordon Alton, Xiao-Hong Yu, Stan Kupchinsky, Steven P. Tanis, Jacques Ermolieff, Tran Khanh Tuan, Min-Jean Yin, Sangita M. Baxi, William F. Vernier, Natasha M. Kablaoui, Michael J. Hickey, Benjamin J. Burke, John Charles Kath, Zhi Xie, Daniel Tyler Richter, John M. Humphrey, Michelle Kraus, RoseAnn Ferre, John Li, Matthew A. Marx, Thomas Allen Chappie, Samantha Elizabeth Greasley, Steven Kazmirski, Simon Bailey, Laura Lingardo
Publikováno v:
Journal of medicinal chemistry. 54(24)
Analogues substituted with various amines at the 6-position of the pyrazine ring on (4-amino-7-isopropyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)pyrazin-2-ylmethanone were discovered as potent and selective inhibitors of PDK1 with potential as anticancer age