Discovery of novel Jak2-Stat pathway inhibitors with extended residence time on target.

Guan, Huiping; Lamb, Michelle L; Peng, Bo; Huang, Shan; Degrace, Nancy; Read, Jon; Hussain, Syeed; Wu, Jiaquan; Rivard, Caroline; Alimzhanov, Marat; Bebernitz, Geraldine; Bell, Kirsten; Ye, Minwei; Zinda, Michael; Ioannidis, Stephanos

Guan, Huiping; Lamb, Michelle L; Peng, Bo; Huang, Shan; Degrace, Nancy; Read, Jon; Hussain, Syeed; Wu, Jiaquan; Rivard, Caroline; Alimzhanov, Marat; Bebernitz, Geraldine; Bell, Kirsten; Ye, Minwei; Zinda, Michael; Ioannidis, Stephanos.

Affiliation

Guan H; Department of Cancer Chemistry, Oncology Innovative Medicines Unit, AstraZeneca R&D Boston, 35 Gatehouse Drive, Waltham, MA 02451, USA.

Bioorg Med Chem Lett ; 23(10): 3105-10, 2013 May 15.

Article in En | MEDLINE | ID: mdl-23562594

Subject(s)

Drug Discovery; Janus Kinase 2/antagonists & inhibitors; Protein Kinase Inhibitors/pharmacology; STAT5 Transcription Factor/antagonists & inhibitors; Animals; Cell Line, Transformed; Cell Proliferation/drug effects; Dogs; Dose-Response Relationship, Drug; Female; Humans; Janus Kinase 2/genetics; Janus Kinase 2/metabolism; Male; Mice; Mice, Inbred Strains; Models, Molecular; Molecular Conformation; Phosphorylation/drug effects; Protein Kinase Inhibitors/chemical synthesis; Protein Kinase Inhibitors/chemistry; Rats; Rats, Wistar; STAT5 Transcription Factor/metabolism; Structure-Activity Relationship; Substrate Specificity; Time Factors

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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Protein Kinase Inhibitors / STAT5 Transcription Factor / Janus Kinase 2 / Drug Discovery Type of study: Prognostic_studies Limits: Animals / Female / Humans / Male Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2013 Document type: Article Affiliation country: United States Country of publication: United kingdom

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