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Page 1
Discovery of Ligands for TRIM58, a Novel Tissue-Selective E3 Ligase.
Hoegenauer K, An S, Axford J, Benander C, Bergsdorf C, Botsch J, Chau S, Fernández C, Gleim S, Hassiepen U, Hunziker J, Joly E, Keller A, Lopez Romero S, Maher R, Mangold AS, Mickanin C, Mihalic M, Neuner P, Patterson AW, Perruccio F, Roggo S, Scesa J, Schröder M, Shkoza D, Thai B, Vulpetti A, Renatus M, Reece-Hoyes JS. Hoegenauer K, et al. Among authors: renatus m. ACS Med Chem Lett. 2023 Nov 13;14(12):1631-1639. doi: 10.1021/acsmedchemlett.3c00259. eCollection 2023 Dec 14. ACS Med Chem Lett. 2023. PMID: 38116426
Discovery of New Binders for DCAF1, an Emerging Ligase Target in the Targeted Protein Degradation Field.
Vulpetti A, Holzer P, Schmiedeberg N, Imbach-Weese P, Pissot-Soldermann C, Hollingworth GJ, Radimerski T, Thoma CR, Stachyra TM, Wojtynek M, Maschlej M, Chau S, Schuffenhauer A, Fernández C, Schröder M, Renatus M. Vulpetti A, et al. Among authors: renatus m. ACS Med Chem Lett. 2023 Jun 2;14(7):949-954. doi: 10.1021/acsmedchemlett.3c00104. eCollection 2023 Jul 13. ACS Med Chem Lett. 2023. PMID: 37465299
DCAF1-based PROTACs with activity against clinically validated targets overcoming intrinsic- and acquired-degrader resistance.
Schröder M, Renatus M, Liang X, Meili F, Zoller T, Ferrand S, Gauter F, Li X, Sigoillot F, Gleim S, Stachyra TM, Thomas JR, Begue D, Khoshouei M, Lefeuvre P, Andraos-Rey R, Chung B, Ma R, Pinch B, Hofmann A, Schirle M, Schmiedeberg N, Imbach P, Gorses D, Calkins K, Bauer-Probst B, Maschlej M, Niederst M, Maher R, Henault M, Alford J, Ahrne E, Tordella L, Hollingworth G, Thomä NH, Vulpetti A, Radimerski T, Holzer P, Carbonneau S, Thoma CR. Schröder M, et al. Among authors: renatus m. Nat Commun. 2024 Jan 4;15(1):275. doi: 10.1038/s41467-023-44237-4. Nat Commun. 2024. PMID: 38177131 Free PMC article.
Discovery of Potent, Highly Selective, and In Vivo Efficacious, Allosteric MALT1 Inhibitors by Iterative Scaffold Morphing.
Pissot Soldermann C, Simic O, Renatus M, Erbel P, Melkko S, Wartmann M, Bigaud M, Weiss A, McSheehy P, Endres R, Santos P, Blank J, Schuffenhauer A, Bold G, Buschmann N, Zoller T, Altmann E, Manley PW, Dix I, Buchdunger E, Scesa J, Quancard J, Schlapbach A, Bornancin F, Radimerski T, Régnier CH. Pissot Soldermann C, et al. Among authors: renatus m. J Med Chem. 2020 Dec 10;63(23):14576-14593. doi: 10.1021/acs.jmedchem.0c01245. Epub 2020 Nov 30. J Med Chem. 2020. PMID: 33252239
Optimization of the In Vivo Potency of Pyrazolopyrimidine MALT1 Protease Inhibitors by Reducing Metabolism and Increasing Potency in Whole Blood.
Quancard J, Simic O, Pissot Soldermann C, Aichholz R, Blatter M, Renatus M, Erbel P, Melkko S, Endres R, Sorge M, Kieffer L, Wagner T, Beltz K, Mcsheehy P, Wartmann M, Régnier CH, Calzascia T, Radimerski T, Bigaud M, Weiss A, Bornancin F, Schlapbach A. Quancard J, et al. Among authors: renatus m. J Med Chem. 2020 Dec 10;63(23):14594-14608. doi: 10.1021/acs.jmedchem.0c01246. Epub 2020 Nov 20. J Med Chem. 2020. PMID: 33216547
Structure-Based Design and Preclinical Characterization of Selective and Orally Bioavailable Factor XIa Inhibitors: Demonstrating the Power of an Integrated S1 Protease Family Approach.
Lorthiois E, Roache J, Barnes-Seeman D, Altmann E, Hassiepen U, Turner G, Duvadie R, Hornak V, Karki RG, Schiering N, Weihofen WA, Perruccio F, Calhoun A, Fazal T, Dedic D, Durand C, Dussauge S, Fettis K, Tritsch F, Dentel C, Druet A, Liu D, Kirman L, Lachal J, Namoto K, Bevan D, Mo R, Monnet G, Muller L, Zessis R, Huang X, Lindsley L, Currie T, Chiu YH, Fridrich C, Delgado P, Wang S, Hollis-Symynkywicz M, Berghausen J, Williams E, Liu H, Liang G, Kim H, Hoffmann P, Hein A, Ramage P, D'Arcy A, Harlfinger S, Renatus M, Ruedisser S, Feldman D, Elliott J, Sedrani R, Maibaum J, Adams CM. Lorthiois E, et al. Among authors: renatus m. J Med Chem. 2020 Aug 13;63(15):8088-8113. doi: 10.1021/acs.jmedchem.0c00279. Epub 2020 Jul 21. J Med Chem. 2020. PMID: 32551603
Structural Basis of BRCC36 Function in DNA Repair and Immune Regulation.
Rabl J, Bunker RD, Schenk AD, Cavadini S, Gill ME, Abdulrahman W, Andrés-Pons A, Luijsterburg MS, Ibrahim AFM, Branigan E, Aguirre JD, Marceau AH, Guérillon C, Bouwmeester T, Hassiepen U, Peters AHFM, Renatus M, Gelman L, Rubin SM, Mailand N, van Attikum H, Hay RT, Thomä NH. Rabl J, et al. Among authors: renatus m. Mol Cell. 2019 Aug 8;75(3):483-497.e9. doi: 10.1016/j.molcel.2019.06.002. Epub 2019 Jun 25. Mol Cell. 2019. PMID: 31253574 Free PMC article.
An allosteric MALT1 inhibitor is a molecular corrector rescuing function in an immunodeficient patient.
Quancard J, Klein T, Fung SY, Renatus M, Hughes N, Israël L, Priatel JJ, Kang S, Blank MA, Viner RI, Blank J, Schlapbach A, Erbel P, Kizhakkedathu J, Villard F, Hersperger R, Turvey SE, Eder J, Bornancin F, Overall CM. Quancard J, et al. Among authors: renatus m. Nat Chem Biol. 2019 Mar;15(3):304-313. doi: 10.1038/s41589-018-0222-1. Epub 2019 Jan 28. Nat Chem Biol. 2019. PMID: 30692685
44 results