Yihan Wang

发表

Structural Analysis of DFG‐in and DFG‐out Dual Src‐Abl Inhibitors Sharing a Common Vinyl Purine Template

T. Clackson, T. Zhou, T. Sawyer, 2009, Chemical biology & drug design.

SAR of Carbon‐Linked, 2‐Substituted Purines: Synthesis and Characterization of AP23451 as a novel Bone‐Targeted Inhibitor of Src Tyrosine Kinase With In Vivo Anti‐Resorptive Activity

R. Bohacek, L. Xing, B. Boyce, 2008, Chemical biology & drug design.

Src Inhibitors in Metastatic Bone Disease

L. Xing, T. Yamashita, B. Boyce, 2006, Clinical Cancer Research.

Future Anti‐Catabolic Therapeutic Targets in Bone Disease

L. Xing, B. Boyce, T. Sawyer, 2006, Annals of the New York Academy of Sciences.

AP23846, a novel and highly potent Src family kinase inhibitor, reduces vascular endothelial growth factor and interleukin-8 expression in human solid tumor cell lines and abrogates downstream angiogenic processes

J. Trevino, T. Sawyer, W. Shakespeare, 2005, Molecular Cancer Therapeutics.

The Potent ALK Inhibitor Brigatinib (AP26113) Overcomes Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in Preclinical Models

T. Clackson, R. Anjum, V. Rivera, 2016, Clinical Cancer Research.

Abstract LB-298: AP26113, a potent ALK inhibitor, overcomes mutations in EML4-ALK that confer resistance to PF-02341066 (PF1066)

T. Clackson, R. Anjum, V. Rivera, 2010 .

Abstract #3738: Discovery of potent and selective orally active inhibitors of anaplastic lymphoma kinase (ALK)

T. Clackson, R. Anjum, V. Rivera, 2009 .

Structural Basis of Src Tyrosine Kinase Inhibition with a New Class of Potent and Selective Trisubstituted Purine‐based Compounds

Susan Adams, William Shakespeare, Thilo Stehle, 2006, Chemical biology & drug design.

AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance.

T. Clackson, B. Druker, A. Corbin, 2009, Cancer cell.

Novel bone-targeted Src tyrosine kinase inhibitor drug discovery.

R. Bohacek, T. Sawyer, W. Shakespeare, 2003, Current opinion in drug discovery & development.

SRC homology-2 inhibitors: peptidomimetic and nonpeptide.

C. Eyermann, R. Bohacek, T. Sawyer, 2002, Mini reviews in medicinal chemistry.

Bone-targeted Src kinase inhibitors: novel pyrrolo- and pyrazolopyrimidine analogues.

R. Bohacek, T. Sawyer, W. Shakespeare, 2003, Bioorganic & medicinal chemistry letters.

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, Jan Romero, Shuangying Liu, 2010, Journal of medicinal chemistry.

Design and synthesis of novel quinazolin‐4(1H)‐one derivatives as potent and selective inhibitors targeting AKR1B1

Changjin Zhu, Xin Hao, Zhongfei Han, 2023, Archiv der Pharmazie.

Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase.

T. Clackson, R. Anjum, V. Rivera, 2016, Journal of medicinal chemistry.

Crystal Structure of the T315I Mutant of Abl Kinase

T. Zhou, W. Shakespeare, Sarah D. Lamore, 2007, Chemical biology & drug design.

Crizotinib-Resistant Mutants of EML4-ALK Identified Through an Accelerated Mutagenesis Screen

T. Clackson, R. Anjum, V. Rivera, 2011, Chemical biology & drug design.

Structural Mechanism of the Pan‐BCR‐ABL Inhibitor Ponatinib (AP24534): Lessons for Overcoming Kinase Inhibitor Resistance

T. Clackson, V. Rivera, T. Zhou, 2011, Chemical biology & drug design.

Activity of dual SRC-ABL inhibitors highlights the role of BCR/ABL kinase dynamics in drug resistance.

Piotr Sliz, Mohammad Azam, Tomi K Sawyer, 2006, Proceedings of the National Academy of Sciences of the United States of America.

Inhibition of wild-type and mutant Bcr-Abl by AP23464, a potent ATP-based oncogenic protein kinase inhibitor: implications for CML.

T. Clackson, R. Bohacek, B. Druker, 2004, Blood.

Antiangiogenic and antitumor effects of SRC inhibition in ovarian carcinoma.

Liz Y. Han, A. Sood, C. Landen, 2006, Cancer research.

Fragment growing and linking lead to novel nanomolar lactate dehydrogenase inhibitors.

T. Clackson, V. Rivera, T. Zhou, 2013, Journal of medicinal chemistry.

Novel protein kinase inhibitors: SMART drug design technology.

R. Bohacek, T. Sawyer, W. Shakespeare, 2003, BioTechniques.

SMART Drug Design: Novel Phosphopeptide and ATP Mimetic-Based Small Molecule Inhibitors of the Oncogenic Protein Kinase pp60 src (Src)

R. Bohacek, T. Sawyer, W. Shakespeare, 2005 .

9-(Arenethenyl)purines as dual Src/Abl kinase inhibitors targeting the inactive conformation: design, synthesis, and biological evaluation.

G. Daley, T. Clackson, M. Azam, 2009, Journal of medicinal chemistry.

Orally Active Inhibitors of the Imatinib Resistant Bcr-Abl Mutant T315I.

T. Clackson, B. Druker, A. Corbin, 2006 .

Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant.

Wei-Sheng Huang, Jan Romero, Shuangying Liu, 2011, Bioorganic & medicinal chemistry letters.

Novel N9-arenethenyl purines as potent dual Src/Abl tyrosine kinase inhibitors.

T. Clackson, T. Sawyer, W. Shakespeare, 2008, Bioorganic & medicinal chemistry letters.

AP23848 against activation loop mutants of Kit In vitro and in vivo activity of ATP-based kinase inhibitors AP23464 and

B. Druker, M. Heinrich, T. Sawyer, 2013 .

In vitro and in vivo activity of ATP-based kinase inhibitors AP23464 and AP23848 against activation-loop mutants of Kit.

B. Druker, M. Heinrich, A. Corbin, 2005, Blood.

Derives heterocycliques insatures

T. Sawyer, W. Shakespeare, D. Dalgarno, 2006 .

Regulation of bone remodeling and emerging breakthrough drugs for osteoporosis and osteolytic bone metastases.

William Shakespeare, Brendan F Boyce, L. Xing, 2003, Kidney international. Supplement.

Novel Small Molecule Inhibitors of Choline Kinase Identified by Fragment-Based Drug Discovery.

T. Zhou, M. Greenfield, J. Miret, 2016, Journal of medicinal chemistry.

Abstract 3623: Efficacy and pharmacodynamic analysis of AP26113, a potent and selective orally active inhibitor of Anaplastic Lymphoma Kinase (ALK)

Juan J. Miret, Wei-Sheng Huang, Shuangying Liu, 2010 .

Bone-targeted 2,6,9-trisubstituted purines: novel inhibitors of Src tyrosine kinase for the treatment of bone diseases.

R. Bohacek, T. Sawyer, W. Shakespeare, 2003, Bioorganic & medicinal chemistry letters.

Structural Mechanism of the Pan‐BCR‐ABL Inhibitor Ponatinib (AP24534): Lessons for Overcoming Kinase Inhibitor Resistance

T. Clackson, V. Rivera, T. Zhou, 2011, Chemical biology & drug design.

Structure-based design of novel nonpeptide inhibitors of the Src SH2 domain:phosphotyrosine mimetics exploiting multifunctional group replacement chemistry.

C. Eyermann, R. Bohacek, T. Sawyer, 2003, Biopolymers.

Bone-targeted pyrido[2,3-d]pyrimidin-7-ones: potent inhibitors of Src tyrosine kinase as novel antiresorptive agents.

S. Violette, R. Bohacek, T. Sawyer, 2003, Bioorganic & medicinal chemistry letters.