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Pirtobrutinib targets BTK C481S in ibrutinib-resistant CLL but second-site BTK mutations lead to resistance.
Naeem A, Utro F, Wang Q, Cha J, Vihinen M, Martindale S, Zhou Y, Ren Y, Tyekucheva S, Kim AS, Fernandes SM, Saksena G, Rhrissorrakrai K, Levovitz C, Danysh BP, Slowik K, Jacobs RA, Davids MS, Lederer JA, Zain R, Smith CIE, Leshchiner I, Parida L, Getz G, Brown JR. Naeem A, et al. Among authors: zain r. Blood Adv. 2023 May 9;7(9):1929-1943. doi: 10.1182/bloodadvances.2022008447. Blood Adv. 2023. PMID: 36287227 Free PMC article.
Therapeutic Oligonucleotides: State of the Art.
Smith CIE, Zain R. Smith CIE, et al. Among authors: zain r. Annu Rev Pharmacol Toxicol. 2019 Jan 6;59:605-630. doi: 10.1146/annurev-pharmtox-010818-021050. Epub 2018 Oct 9. Annu Rev Pharmacol Toxicol. 2019. PMID: 30285540 Review.
Chemical Development of Therapeutic Oligonucleotides.
Lundin KE, Gissberg O, Smith CIE, Zain R. Lundin KE, et al. Among authors: zain r. Methods Mol Biol. 2019;2036:3-16. doi: 10.1007/978-1-4939-9670-4_1. Methods Mol Biol. 2019. PMID: 31410788
BTK gatekeeper residue variation combined with cysteine 481 substitution causes super-resistance to irreversible inhibitors acalabrutinib, ibrutinib and zanubrutinib.
Estupiñán HY, Wang Q, Berglöf A, Schaafsma GCP, Shi Y, Zhou L, Mohammad DK, Yu L, Vihinen M, Zain R, Smith CIE. Estupiñán HY, et al. Among authors: zain r. Leukemia. 2021 May;35(5):1317-1329. doi: 10.1038/s41375-021-01123-6. Epub 2021 Feb 1. Leukemia. 2021. PMID: 33526860 Free PMC article.
211 results