2024
Development of a Small Molecule Downmodulator for the Transcription Factor Brachyury
Chase D, Bebenek A, Nie P, Jaime‐Figueroa S, Butrin A, Castro D, Hines J, Linhares B, Crews C. Development of a Small Molecule Downmodulator for the Transcription Factor Brachyury. Angewandte Chemie International Edition 2024, 63: e202316496. PMID: 38348945, DOI: 10.1002/anie.202316496.Peer-Reviewed Original ResearchStructure-based drug design approachX-ray crystallographyDrug design approachMass spectrometryFDA-approved kinase inhibitorsX-raySmall moleculesChordoma cellsCrystallographyTumor cell growthCompoundsChordoma cell linesMoleculesChordoma growthOncogenic transcription factorKinase inhibitorsTranscription factors
2022
OligoTRAFTACs: A generalizable method for transcription factor degradation
Samarasinghe KTG, An E, Genuth MA, Chu L, Holley SA, Crews CM. OligoTRAFTACs: A generalizable method for transcription factor degradation. RSC Chemical Biology 2022, 3: 1144-1153. PMID: 36128504, PMCID: PMC9428672, DOI: 10.1039/d2cb00138a.Peer-Reviewed Original ResearchTranscription factorsOncogenic transcription factorGene expression circuitryTranscription factor degradationDNA binding abilityChordoma cell linesProteasomal degradationProteasomal pathwayZebrafish experimentsC-MycGeneralizable platformKey playersCell linesBrachyurySmall moleculesFactor degradationBinding abilityGeneralizable methodDegradationChimerasPathwayOligonucleotidePocketFirst generation