AP24534, a Pan-BCR-ABL Inhibitor for Chronic Myeloid Leukemia, Potently Inhibits the T315I Mutant and Overcomes Mutation-Based Resistance

Thomas O’Hare, William C. Shakespeare, Xiaotian Zhu, +25

Cancer Cell

Hematological MalignancyTumor BiologyChronic Myeloid LeukemiaOncologyPan-bcr-abl Inhibitor +7

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

Wei‐Sheng Huang, Shuangying Liu, Dong Zou, +31

Journal of Medicinal Chemistry

Drug TargetAnaplastic Lymphoma KinaseTumor BiologyMedicinal ChemistrySelective Alk Inhibitors +16

Discovery of 3-[2-(Imidazo[1,2-<i>b</i>]pyridazin-3-yl)ethynyl]-4-methyl-<i>N</i>-{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, +31

Journal of Medicinal Chemistry

Drug TargetImmunologyMolecular BiologyT315i Gatekeeper MutantNative Bcr-abl +23

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

Tianjun Zhou, Lois Commodore, Wei‐Sheng Huang, +9

Chemical Biology & Drug Design

A Newtinman-Related Gene,nkx2.7,Anticipates the Expression ofnkx2.5andnkx2.3in Zebrafish Heart and Pharyngeal Endoderm

Kyu‐Ho Lee, Qihong Xu, Roger E. Breitbart

Developmental Biology

Cell LineageDevelopmental BiologyMolecular PhysiologyEpendymaNewtinman-related Gene +8

Functional and biochemical interactions of Wnts with FrzA, a secreted Wnt antagonist

Qihong Xu, Patrìcia A. D'Amore, Sergei Y. Sokol

Development

Crystal Structure of the T315I Mutant of Abl Kinase

Tianjun Zhou, Lois Parillon, Feng Li, +7

Chemical Biology & Drug Design

Crystal StructureEngineeringMixed-phenotype Acute LeukemiaMolecular BiologyTumor Biology +15

Multiplex quantitative assays indicate a need for reevaluating reported small-molecule TrkB agonists

Umed Boltaev, Yves Meyer, Farangis Tolibzoda, +8

Science Signaling

Drug TargetMultiplex Quantitative AssaysReliable ProbesTrkb Receptor ActivationReceptor Tyrosine Kinase +16

<i>Xenopus Cyr61</i>regulates gastrulation movements and modulates Wnt signalling

Branko Latinkic, Sara Mercurio, Brydon L. Bennett, +5

Development

Xenopus LaevisMolecular RegulationCell AdhesionCytoskeletonCellular Physiology +15

9-(Arenethenyl)purines as Dual Src/Abl Kinase Inhibitors Targeting the Inactive Conformation: Design, Synthesis, and Biological Evaluation

Wei‐Sheng Huang, Xiaotian Zhu, Yihan Wang, +22

Journal of Medicinal Chemistry

ImmunologyPharmacotherapyActive Enzyme ConformationChemical BiologyPharmaceutical Chemistry +17