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Discovery of reversible and covalent TEAD 1 selective inhibitors MSC-1254 and MSC-5046 based on one scaffold.
Carswell E, Heinrich T, Petersson C, Gunera J, Garg S, Schwarz D, Schlesiger S, Fischer F, Eichhorn T, Calder M, Smith G, MacDonald E, Wilson H, Hazel K, Trivier E, Broome R, Balsiger A, Sirohi S, Musil D, Freire F, Schilke H, Dillon C, Wienke D. Carswell E, et al. Among authors: trivier e. Bioorg Med Chem Lett. 2024 Dec 1;114:129981. doi: 10.1016/j.bmcl.2024.129981. Epub 2024 Oct 5. Bioorg Med Chem Lett. 2024. PMID: 39369801
Optimization of TEAD P-Site Binding Fragment Hit into In Vivo Active Lead MSC-4106.
Heinrich T, Peterson C, Schneider R, Garg S, Schwarz D, Gunera J, Seshire A, Kötzner L, Schlesiger S, Musil D, Schilke H, Doerfel B, Diehl P, Böpple P, Lemos AR, Sousa PMF, Freire F, Bandeiras TM, Carswell E, Pearson N, Sirohi S, Hooker M, Trivier E, Broome R, Balsiger A, Crowden A, Dillon C, Wienke D. Heinrich T, et al. Among authors: trivier e. J Med Chem. 2022 Jul 14;65(13):9206-9229. doi: 10.1021/acs.jmedchem.2c00403. Epub 2022 Jun 28. J Med Chem. 2022. PMID: 35763499
Discovery of potent inhibitors of the lysophospholipase autotaxin.
Shah P, Cheasty A, Foxton C, Raynham T, Farooq M, Gutierrez IF, Lejeune A, Pritchard M, Turnbull A, Pang L, Owen P, Boyd S, Stowell A, Jordan A, Hamilton NM, Hitchin JR, Stockley M, MacDonald E, Quesada MJ, Trivier E, Skeete J, Ovaa H, Moolenaar WH, Ryder H. Shah P, et al. Among authors: trivier e. Bioorg Med Chem Lett. 2016 Nov 15;26(22):5403-5410. doi: 10.1016/j.bmcl.2016.10.036. Epub 2016 Oct 14. Bioorg Med Chem Lett. 2016. PMID: 27780639
3-(3,4-Dihydroisoquinolin-2(1H)-ylsulfonyl)benzoic Acids: highly potent and selective inhibitors of the type 5 17-β-hydroxysteroid dehydrogenase AKR1C3.
Jamieson SM, Brooke DG, Heinrich D, Atwell GJ, Silva S, Hamilton EJ, Turnbull AP, Rigoreau LJ, Trivier E, Soudy C, Samlal SS, Owen PJ, Schroeder E, Raynham T, Flanagan JU, Denny WA. Jamieson SM, et al. Among authors: trivier e. J Med Chem. 2012 Sep 13;55(17):7746-58. doi: 10.1021/jm3007867. Epub 2012 Aug 21. J Med Chem. 2012. PMID: 22877157
Selective AKR1C3 inhibitors do not recapitulate the anti-leukaemic activities of the pan-AKR1C inhibitor medroxyprogesterone acetate.
Khanim F, Davies N, Veliça P, Hayden R, Ride J, Pararasa C, Chong MG, Gunther U, Veerapen N, Winn P, Farmer R, Trivier E, Rigoreau L, Drayson M, Bunce C. Khanim F, et al. Among authors: trivier e. Br J Cancer. 2014 Mar 18;110(6):1506-16. doi: 10.1038/bjc.2014.83. Epub 2014 Feb 25. Br J Cancer. 2014. PMID: 24569460 Free PMC article.
Synthesis and structure-activity relationships for 1-(4-(piperidin-1-ylsulfonyl)phenyl)pyrrolidin-2-ones as novel non-carboxylate inhibitors of the aldo-keto reductase enzyme AKR1C3.
Heinrich DM, Flanagan JU, Jamieson SM, Silva S, Rigoreau LJ, Trivier E, Raynham T, Turnbull AP, Denny WA. Heinrich DM, et al. Among authors: trivier e. Eur J Med Chem. 2013 Apr;62:738-44. doi: 10.1016/j.ejmech.2013.01.047. Epub 2013 Feb 9. Eur J Med Chem. 2013. PMID: 23454516
MoA Studies of the TEAD P-Site Binding Ligand MSC-4106 and Its Optimization to TEAD1-Selective Amide M3686.
Heinrich T, Schwarz D, Petersson C, Gunera J, Garg S, Schneider R, Keil M, Grimmeisen L, Unzue Lopez A, Albers L, Schlesiger S, Gambardella A, Bomke J, Carswell E, Schilke H, Diehl P, Doerfel B, Musil D, Trivier E, Broome R, Marshall S, Balsiger A, Friedrich E, Lemos AR, Santos SP, Sousa PMF, Freire F, Bandeiras TM, Bortoluzzi A, Wienke D. Heinrich T, et al. Among authors: trivier e. J Med Chem. 2024 Dec 20. doi: 10.1021/acs.jmedchem.4c01949. Online ahead of print. J Med Chem. 2024. PMID: 39704449
24 results