Parallel Synthesis and Screening of a Solid Phase Carbohydrate Library

Rui Liang, Lin Yan, Jennifer Loebach, +10

Science

Combinatorial ChemistryBioorganic ChemistryGlycobiologyCell Surface CarbohydratesOrganic Chemistry +18

Highly Concise Routes to Epothilones:  The Total Synthesis and Evaluation of Epothilone 490

Kaustav Biswas, Hong Lin, Jón T. Njardarson, +7

Journal of the American Chemical Society

Unfolded Protein Response in Cancer: IRE1α Inhibition by Selective Kinase Ligands Does Not Impair Tumor Cell Viability

Paul E. Harrington, Kaustav Biswas, David J. Malwitz, +10

ACS Medicinal Chemistry Letters

Cellular ViabilityKinase SiteProtein ResponseCancer BiologyTumor Biology +18

Effects of temperature and concentration in some ring closing metathesis reactions

Kana Yamamoto, Kaustav Biswas, Christoph Gaul, +1

Tetrahedron Letters

Chemical EngineeringEngineeringAlkene MetathesisReaction IntermediateThermodynamics +3

Discovery of TRPM8 Antagonist (<i>S</i>)-6-(((3-Fluoro-4-(trifluoromethoxy)phenyl)(3-fluoropyridin-2-yl)methyl)carbamoyl)nicotinic Acid (AMG 333), a Clinical Candidate for the Treatment of Migraine

Daniel B. Horne, Kaustav Biswas, James Brown, +19

Journal of Medicinal Chemistry

Molecular PharmacologyMedicinal ChemistryTrpm8 AntagonistCluster HeadacheAmg 333 +13

NanoClick: A High Throughput, Target-Agnostic Peptide Cell Permeability Assay

Andrea Peier, Lan Ge, N. Boyer, +22

ACS Chemical Biology

Application of hitherto unexplored macrocyclization strategies in the epothilone series: novel epothilone analogs by total synthesisElectronic supplementary information (ESI) available: experimental details for the synthesis of 14 and 32. See http://www.rsc.org/suppdata/cc/b2/b209941a/

Jón T. Njardarson, Kaustav Biswas, Samuel J. Danishefsky

Chemical Communications

EngineeringHeterocyclicAlkene MetathesisNatural SciencesDiversity-oriented Synthesis +13

Single Residue Substitutions That Confer Voltage-Gated Sodium Ion Channel Subtype Selectivity in the Na_V1.7 Inhibitory Peptide GpTx-1

Justin K. Murray, Jason Long, Anruo Zou, +7

Journal of Medicinal Chemistry

Drug TargetMolecular BiologyPeptide ScienceMolecular PharmacologySingle Residue Substitutions +18

Total Syntheses of [17]- and [18]Dehydrodesoxyepothilones B via a Concise Ring-Closing Metathesis-Based Strategy:  Correlation of Ring Size with Biological Activity in the Epothilone Series

Alexey Rivkin, Jón T. Njardarson, Kaustav Biswas, +2

The Journal of Organic Chemistry

Bioorganic ChemistryAntitumor ActivityOrganic ChemistryTotal SynthesesTumor Biology +17

Pharmacological characterization of potent and selective NaV1.7 inhibitors engineered from Chilobrachys jingzhao tarantula venom peptide JzTx-V

Bryan D. Moyer, Justin K. Murray, Joseph Ligutti, +15

PLoS ONE

Pharmacological CharacterizationMolecular BiologyMolecular PainPharmacotherapyMolecular Pharmacology +15