Q
Qihong Xu
Researcher at ARIAD Pharmaceuticals, Inc.
Publications - 10
Citations - 2107
Qihong Xu is an academic researcher from ARIAD Pharmaceuticals, Inc.. The author has contributed to research in topics: Ponatinib & ABL. The author has an hindex of 9, co-authored 10 publications receiving 1825 citations.
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Journal ArticleDOI
AP24534, a Pan-BCR-ABL Inhibitor for Chronic Myeloid Leukemia, Potently Inhibits the T315I Mutant and Overcomes Mutation-Based Resistance
Thomas O'Hare,Thomas O'Hare,William C. Shakespeare,Xiaotian Zhu,Christopher A. Eide,Christopher A. Eide,Victor M. Rivera,Frank Wang,Lauren T. Adrian,Lauren T. Adrian,Tianjun Zhou,Huang Wei Sheng,Qihong Xu,Chester A. Metcalf,Jeffrey W. Tyner,Marc M. Loriaux,Amie S. Corbin,Amie S. Corbin,Scott Wardwell,Yaoyu Ning,Jeffrey A. Keats,Yihan Wang,Raji Sundaramoorthi,Mathew Thomas,Dong Zhou,Joseph Snodgrass,Lois Commodore,Tomi K. Sawyer,David C. Dalgarno,Michael W. Deininger,Brian J. Druker,Brian J. Druker,Tim Clackson +32 more
TL;DR: Design and preclinical evaluation of AP24534, a potent, orally available multitargeted kinase inhibitor active against T315I and other BCR-ABL mutants, and clinical evaluation ofAP24534 as a pan-BCR-ABl inhibitor for treatment of CML are reported.
Journal ArticleDOI
Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including the T315I gatekeeper mutant.
Wei-Sheng Huang,Chester A. Metcalf,Raji Sundaramoorthi,Yihan Wang,Dong Zou,R. Mathew Thomas,Xiaotian Zhu,Lisi Cai,David Wen,Shuangying Liu,Jan Romero,Jiwei Qi,Ingrid Chen,Geetha Banda,Scott Paul Lentini,Sasmita Das,Qihong Xu,Jeff Keats,Frank Wang,Scott Wardwell,Yaoyu Ning,Joseph Snodgrass,Marc I Broudy,Karin Russian,Tianjun Zhou,Lois Commodore,Narayana I. Narasimhan,Qurish K. Mohemmad,John Iuliucci,Victor M. Rivera,David C. Dalgarno,Tomi K. Sawyer,Tim Clackson,William C. Shakespeare +33 more
TL;DR: Daily oral administration of 20g significantly prolonged survival of mice injected intravenously with BCR-ABL(T315I) expressing Ba/F3 cells, and coupled with a favorable ADME profile, support the potential of 20G to be an effective treatment for CML, including patients refractory to all currently approved therapies.
Journal ArticleDOI
Structural Mechanism of the Pan-BCR-ABL Inhibitor Ponatinib (AP24534): Lessons for Overcoming Kinase Inhibitor Resistance
Tianjun Zhou,Lois Commodore,Wei-Sheng Huang,Yihan Wang,Mathew Thomas,Jeff Keats,Qihong Xu,Victor M. Rivera,William C. Shakespeare,Tim Clackson,David C. Dalgarno,Xiaotian Zhu +11 more
TL;DR: The inhibitory mechanism exemplified by ponatinib may have broad relevance to designing inhibitors against other kinases with mutated gatekeeper residues, and the extensive network of optimized molecular contacts found in the DFG‐out binding mode leads to high potency and renders binding less susceptible to disruption by single point mutations.
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Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase.
Wei-Sheng Huang,Shuangying Liu,Dong Zou,Mathew Thomas,Yihan Wang,Tianjun Zhou,Jan Romero,Anna Kohlmann,Feng Li,Jiwei Qi,Lisi Cai,Timothy A. Dwight,Yongjin Xu,Rongsong Xu,Rory Dodd,Angela Toms,Lois Parillon,Xiaohui Lu,Rana Anjum,Sen Zhang,Frank Wang,Jeffrey A. Keats,Scott Wardwell,Yaoyu Ning,Qihong Xu,Lauren Moran,Qurish K. Mohemmad,Hyun Gyung Jang,Tim Clackson,Narayana I. Narasimhan,Victor M. Rivera,Xiaotian Zhu,David C. Dalgarno,William C. Shakespeare +33 more
TL;DR: Brigatinib represents the most clinically advanced phosphine oxide-containing drug candidate to date and is currently being evaluated in a global phase 2 registration trial.
Journal ArticleDOI
Crystal Structure of the T315I Mutant of Abl Kinase
Tianjun Zhou,Lois Parillon,Feng Li,Yihan Wang,Jeff Keats,Sarah Lamore,Qihong Xu,William C. Shakespeare,David C. Dalgarno,Xiaotian Zhu +9 more
TL;DR: The crystal structure of the kinase domain of the c‐Abl T315I mutant, as well as the wild‐type form, is presented, in complex with a pyrrolopyridine inhibitor, PPY‐A, to provide structural guidance for the design of clinically useful inhibitors of Bcr‐A Bl T 315I.