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Structure-Activity Relationship of Potent, Selective, and Orally Bioavailable Molecular Glue Degraders of CK1α.
Nishiguchi G, Caine EA, McGowan K, Shi Z, Aggarwal A, Mayasundari A, Price J, Yang L, Li Y, Fu X, Mascibroda LG, Das S, Daniels DL, Urh M, Klco JM, Riching KM, Rankovic Z. Nishiguchi G, et al. Among authors: riching km. ACS Med Chem Lett. 2024 Sep 12;15(10):1692-1698. doi: 10.1021/acsmedchemlett.4c00250. eCollection 2024 Oct 10. ACS Med Chem Lett. 2024. PMID: 39411539 Free PMC article.
Selective CK1α degraders exert antiproliferative activity against a broad range of human cancer cell lines.
Nishiguchi G, Mascibroda LG, Young SM, Caine EA, Abdelhamed S, Kooijman JJ, Miller DJ, Das S, McGowan K, Mayasundari A, Shi Z, Barajas JM, Hiltenbrand R, Aggarwal A, Chang Y, Mishra V, Narina S, Thomas M, Loughran AJ, Kalathur R, Yu K, Zhou S, Wang X, High AA, Peng J, Pruett-Miller SM, Daniels DL, Urh M, Shelat AA, Mullighan CG, Riching KM, Zaman GJR, Fischer M, Klco JM, Rankovic Z. Nishiguchi G, et al. Among authors: riching km. Nat Commun. 2024 Jan 16;15(1):482. doi: 10.1038/s41467-024-44698-1. Nat Commun. 2024. PMID: 38228616 Free PMC article.
SRSF2 plays an unexpected role as reader of m5C on mRNA, linking epitranscriptomics to cancer.
Ma HL, Bizet M, Soares Da Costa C, Murisier F, de Bony EJ, Wang MK, Yoshimi A, Lin KT, Riching KM, Wang X, Beckman JI, Arya S, Droin N, Calonne E, Hassabi B, Zhang QY, Li A, Putmans P, Malbec L, Hubert C, Lan J, Mies F, Yang Y, Solary E, Daniels DL, Gupta YK, Deplus R, Abdel-Wahab O, Yang YG, Fuks F. Ma HL, et al. Among authors: riching km. Mol Cell. 2023 Dec 7;83(23):4239-4254.e10. doi: 10.1016/j.molcel.2023.11.003. Mol Cell. 2023. PMID: 38065062 Free PMC article.
Trivalent PROTACs enhance protein degradation via combined avidity and cooperativity.
Imaide S, Riching KM, Makukhin N, Vetma V, Whitworth C, Hughes SJ, Trainor N, Mahan SD, Murphy N, Cowan AD, Chan KH, Craigon C, Testa A, Maniaci C, Urh M, Daniels DL, Ciulli A. Imaide S, et al. Among authors: riching km. Nat Chem Biol. 2021 Nov;17(11):1157-1167. doi: 10.1038/s41589-021-00878-4. Epub 2021 Oct 21. Nat Chem Biol. 2021. PMID: 34675414 Free PMC article.
Discovery and resistance mechanism of a selective CDK12 degrader.
Jiang B, Gao Y, Che J, Lu W, Kaltheuner IH, Dries R, Kalocsay M, Berberich MJ, Jiang J, You I, Kwiatkowski N, Riching KM, Daniels DL, Sorger PK, Geyer M, Zhang T, Gray NS. Jiang B, et al. Among authors: riching km. Nat Chem Biol. 2021 Jun;17(6):675-683. doi: 10.1038/s41589-021-00765-y. Epub 2021 Mar 22. Nat Chem Biol. 2021. PMID: 33753926 Free PMC article.
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