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TitleA Novel Irreversible TEAD Inhibitor, SWTX-143, Blocks Hippo Pathway Transcriptional Output and Causes Tumor Regression in Preclinical Mesothelioma Models.
Journal, issue, pagesMol. Cancer Ther., Vol. 23, Page 3-13, Year 2024
Publish dateAug 11, 2023 (structure data deposition date)
AuthorsHillen, H. / Candi, A. / Vanderhoydonck, B. / Kowalczyk, W. / Sansores-Garcia, L. / Kesikiadou, E.C. / Van Huffel, L. / Spiessens, L. / Nijs, M. / Soons, E. ...Hillen, H. / Candi, A. / Vanderhoydonck, B. / Kowalczyk, W. / Sansores-Garcia, L. / Kesikiadou, E.C. / Van Huffel, L. / Spiessens, L. / Nijs, M. / Soons, E. / Haeck, W. / Klaassen, H. / Smets, W. / Spieser, S.A. / Marchand, A. / Chaltin, P. / Ciesielski, F. / Debaene, F. / Chen, L. / Kamal, A. / Gwaltney, S.L. / Versele, M. / Halder, G.A.
External linksMol. Cancer Ther. / PubMed:37748190
MethodsX-ray diffraction
Resolution1.58 Å
Structure data

PDB-8q68:
Crystal structure of TEAD1-YBD in complex with irreversible compound SWTX-143
Method: X-RAY DIFFRACTION / Resolution: 1.58 Å

Chemicals

ChemComp-K46:
~{N}-[(3~{S})-5-azanyl-1-[4-(trifluoromethyl)phenyl]-3,4-dihydro-2~{H}-quinolin-3-yl]propanamide

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsTRANSCRIPTION / irreversible covalent inhibitor / mesothelioma tumor regression

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