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Leveraging Ligand Affinity and Properties: Discovery of Novel Benzamide-Type Cereblon Binders for the Design of PROTACs.
Steinebach C, Bricelj A, Murgai A, Sosič I, Bischof L, Ng YLD, Heim C, Maiwald S, Proj M, Voget R, Feller F, Košmrlj J, Sapozhnikova V, Schmidt A, Zuleeg MR, Lemnitzer P, Mertins P, Hansen FK, Gütschow M, Krönke J, Hartmann MD. Steinebach C, et al. Among authors: heim c. J Med Chem. 2023 Nov 9;66(21):14513-14543. doi: 10.1021/acs.jmedchem.3c00851. Epub 2023 Oct 30. J Med Chem. 2023. PMID: 37902300 Free PMC article.
Replacing the phthalimide core in thalidomide with benzotriazole.
Krasavin M, Bubyrev A, Kazantsev A, Heim C, Maiwald S, Zhukovsky D, Dar'in D, Hartmann MD, Bunev A. Krasavin M, et al. Among authors: heim c. J Enzyme Inhib Med Chem. 2022 Dec;37(1):527-530. doi: 10.1080/14756366.2021.2024525. J Enzyme Inhib Med Chem. 2022. PMID: 35220840 Free PMC article.
Synthesis of novel glutarimide ligands for the E3 ligase substrate receptor Cereblon (CRBN): Investigation of their binding mode and antiproliferative effects against myeloma cell lines.
Krasavin M, Adamchik M, Bubyrev A, Heim C, Maiwald S, Zhukovsky D, Zhmurov P, Bunev A, Hartmann MD. Krasavin M, et al. Among authors: heim c. Eur J Med Chem. 2023 Jan 15;246:114990. doi: 10.1016/j.ejmech.2022.114990. Epub 2022 Dec 1. Eur J Med Chem. 2023. PMID: 36476642
Chemical Ligand Space of Cereblon.
Boichenko I, Bär K, Deiss S, Heim C, Albrecht R, Lupas AN, Hernandez Alvarez B, Hartmann MD. Boichenko I, et al. Among authors: heim c. ACS Omega. 2018 Sep 14;3(9):11163-11171. doi: 10.1021/acsomega.8b00959. eCollection 2018 Sep 30. ACS Omega. 2018. PMID: 31459225 Free PMC article.
386 results