Indolobenzazepin-7-ones and 6-, 8-, and 9-Membered Ring Derivatives as Tubulin Polymerization Inhibitors: Synthesis and Structure−Activity Relationship Studies

Aurélien Putey, Florence Popowycz, Quoc‐Tuan Do, +5

Journal of Medicinal Chemistry

Chemoprevention StrategyNanomolar Antiproliferative ActivityTubulin Polymerization InhibitorsPharmaceutical ChemistryStructure−activity Relationship Studies +14

Structural Insights into a Unique Inhibitor Binding Pocket in Kinesin Spindle Protein

Venkatasubramanian Ulaganathan, Sandeep K. Talapatra, Oliver Rath, +3

Journal of the American Chemical Society

Drug TargetProtein AssemblyMolecular BiologyCytoskeletonProtein Folding +16

The structure of the ternary Eg5–ADP–ispinesib complex

Sandeep K. Talapatra, Alexander W. Schüttelkopf, Frank Kozielski

Acta Crystallographica Section D Biological Crystallography

Inorganic ChemistryBipolar Spindle FormationCrystal StructureEngineeringBiochemistry +13

Optimized <i>S</i>-Trityl-<scp>l</scp>-cysteine-Based Inhibitors of Kinesin Spindle Protein with Potent in Vivo Antitumor Activity in Lung Cancer Xenograft Models

James A. D. Good, Fang Wang, Oliver Rath, +5

Journal of Medicinal Chemistry

Molecular BiologyPharmacotherapyTumor BiologyMedicinal ChemistryAnti-cancer Agent +16

The C-terminal region of the motor protein MCAK controls its structure and activity through a conformational switch

Sandeep K. Talapatra, Bethany Harker, Julie P. I. Welburn

eLife

C-terminal RegionMolecular BiologyMotor Protein McakKinesin-13 ActivityCytoskeleton +15

The depolymerase activity of MCAK shows a graded response to Aurora B kinase phosphorylation through allosteric regulation

Toni McHugh, Juan Zou, Vladimir A. Volkov, +5

Journal of Cell Science

Precise Microtubule DynamicsMolecular BiologyCytoskeletonSignaling PathwayGraded Response +15

Mitotic Kinesin Eg5 Overcomes Inhibition to the Phase I/II Clinical Candidate SB743921 by an Allosteric Resistance Mechanism

Sandeep K. Talapatra, Nahoum G. Anthony, Simon P. Mackay, +1

Journal of Medicinal Chemistry

Drug TargetProtein FunctionAllosteric Resistance MechanismMedicinePharmacology +12

Modified Peptide Inhibitors of the Keap1–Nrf2 Protein–Protein Interaction Incorporating Unnatural Amino Acids

Nikolaos Georgakopoulos, Sandeep K. Talapatra, Jemma Gatliff, +2

ChemBioChem

Medicinal ChemistryBiochemistryG Protein-coupled ReceptorNatural SciencesMedicine +13

Analysis of the human cofilin 1 structure reveals conformational changes required for actin binding

Marta Klejnot, Mads Gabrielsen, Jenifer Cameron, +5

Acta Crystallographica Section D Biological Crystallography

Cofilin 1Protein AssemblyMolecular BiologyHuman Cofilin 1Cytoskeleton +17

Crystal structure of the Eg5 - K858 complex and implications for structure-based design of thiadiazole-containing inhibitors

Sandeep K. Talapatra, Chuin Lean Tham, Paolo Guglielmi, +5

European Journal of Medicinal Chemistry

Crystal StructureMedicinal ChemistryBiochemistryNatural SciencesRational Drug Design +11