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Structure-kinetic relationship reveals the mechanism of selectivity of FAK inhibitors over PYK2.
Berger BT, Amaral M, Kokh DB, Nunes-Alves A, Musil D, Heinrich T, Schröder M, Neil R, Wang J, Navratilova I, Bomke J, Elkins JM, Müller S, Frech M, Wade RC, Knapp S. Berger BT, et al. Among authors: heinrich t. Cell Chem Biol. 2021 May 20;28(5):686-698.e7. doi: 10.1016/j.chembiol.2021.01.003. Epub 2021 Jan 25. Cell Chem Biol. 2021. PMID: 33497606 Free article.
Fragment-based discovery of focal adhesion kinase inhibitors.
Grädler U, Bomke J, Musil D, Dresing V, Lehmann M, Hölzemann G, Greiner H, Esdar C, Krier M, Heinrich T. Grädler U, et al. Among authors: heinrich t. Bioorg Med Chem Lett. 2013 Oct 1;23(19):5401-9. doi: 10.1016/j.bmcl.2013.07.050. Epub 2013 Jul 31. Bioorg Med Chem Lett. 2013. PMID: 23973211
Identification of Methionine Aminopeptidase-2 (MetAP-2) Inhibitor M8891: A Clinical Compound for the Treatment of Cancer.
Heinrich T, Seenisamy J, Becker F, Blume B, Bomke J, Dietz M, Eckert U, Friese-Hamim M, Gunera J, Hansen K, Leuthner B, Musil D, Pfalzgraf J, Rohdich F, Siegl C, Spuck D, Wegener A, Zenke FT. Heinrich T, et al. J Med Chem. 2019 Dec 26;62(24):11119-11134. doi: 10.1021/acs.jmedchem.9b01070. Epub 2019 Dec 3. J Med Chem. 2019. PMID: 31725285
Discovery of novel 7-azaindoles as PDK1 inhibitors.
Wucherer-Plietker M, Merkul E, Müller TJJ, Esdar C, Knöchel T, Heinrich T, Buchstaller HP, Greiner H, Dorsch D, Finsinger D, Calderini M, Bruge D, Grädler U. Wucherer-Plietker M, et al. Among authors: heinrich t. Bioorg Med Chem Lett. 2016 Jul 1;26(13):3073-3080. doi: 10.1016/j.bmcl.2016.05.005. Epub 2016 May 4. Bioorg Med Chem Lett. 2016. PMID: 27217002
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. 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
211 results