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Crizotinib acts as ABL1 inhibitor combining ATP-binding with allosteric inhibition and is active against native BCR-ABL1 and its resistance and compound mutants BCR-ABL1T315I and BCR-ABL1T315I-E255K.
Mian AA, Haberbosch I, Khamaisie H, Agbarya A, Pietsch L, Eshel E, Najib D, Chiriches C, Ottmann OG, Hantschel O, Biondi RM, Ruthardt M, Mahajna J. Mian AA, et al. Among authors: biondi rm. Ann Hematol. 2021 Aug;100(8):2023-2029. doi: 10.1007/s00277-020-04357-z. Epub 2021 Jun 10. Ann Hematol. 2021. PMID: 34110462 Free PMC article.
An Allosteric Inhibitor Scaffold Targeting the PIF-Pocket of Atypical Protein Kinase C Isoforms.
Arencibia JM, Fröhner W, Krupa M, Pastor-Flores D, Merker P, Oellerich T, Neimanis S, Schmithals C, Köberle V, Süß E, Zeuzem S, Stark H, Piiper A, Odadzic D, Schulze JO, Biondi RM. Arencibia JM, et al. Among authors: biondi rm. ACS Chem Biol. 2017 Feb 17;12(2):564-573. doi: 10.1021/acschembio.6b00827. Epub 2017 Jan 13. ACS Chem Biol. 2017. PMID: 28045490
Camptothecin and its analog SN-38, the active metabolite of irinotecan, inhibit binding of the transcriptional regulator and oncoprotein FUBP1 to its DNA target sequence FUSE.
Khageh Hosseini S, Kolterer S, Steiner M, von Manstein V, Gerlach K, Trojan J, Waidmann O, Zeuzem S, Schulze JO, Hahn S, Steinhilber D, Gatterdam V, Tampé R, Biondi RM, Proschak E, Zörnig M. Khageh Hosseini S, et al. Among authors: biondi rm. Biochem Pharmacol. 2017 Dec 15;146:53-62. doi: 10.1016/j.bcp.2017.10.003. Epub 2017 Oct 13. Biochem Pharmacol. 2017. PMID: 29031818
Demonstrating Ligandability of the LC3A and LC3B Adapter Interface.
Hartmann M, Huber J, Kramer JS, Heering J, Pietsch L, Stark H, Odadzic D, Bischoff I, Fürst R, Schröder M, Akutsu M, Chaikuad A, Dötsch V, Knapp S, Biondi RM, Rogov VV, Proschak E. Hartmann M, et al. Among authors: biondi rm. J Med Chem. 2021 Apr 8;64(7):3720-3746. doi: 10.1021/acs.jmedchem.0c01564. Epub 2021 Mar 26. J Med Chem. 2021. PMID: 33769048
76 results