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Page 1
Trastuzumab-MMAU Antibody-Auristatin Conjugates: Valine-Glucoserine Linker with Stabilized Maleimide Conjugation Improves In Vivo Efficacy and Tolerability.
Goldberg SD, Satomaa T, Aina O, Aitio O, Burke K, Dudkin V, Geist B, Irrechukwu O, Hänninen AL, Heiskanen A, Helin J, Hiltunen JO, Kinyamu-Akunda J, Klein DM, Kohli N, Kotiranta T, Lähteenmäki T, Niemelä R, Pitkänen V, Pynnönen H, Rittase W, Wiley K, Zhou J, Saarinen J. Goldberg SD, et al. Among authors: kinyamu akunda j. Mol Cancer Ther. 2024 Feb 7. doi: 10.1158/1535-7163.MCT-23-0591. Online ahead of print. Mol Cancer Ther. 2024. PMID: 38324296
Discovery and characterization of a selective IKZF2 glue degrader for cancer immunotherapy.
Bonazzi S, d'Hennezel E, Beckwith REJ, Xu L, Fazal A, Magracheva A, Ramesh R, Cernijenko A, Antonakos B, Bhang HC, Caro RG, Cobb JS, Ornelas E, Ma X, Wartchow CA, Clifton MC, Forseth RR, Fortnam BH, Lu H, Csibi A, Tullai J, Carbonneau S, Thomsen NM, Larrow J, Chie-Leon B, Hainzl D, Gu Y, Lu D, Meyer MJ, Alexander D, Kinyamu-Akunda J, Sabatos-Peyton CA, Dales NA, Zécri FJ, Jain RK, Shulok J, Wang YK, Briner K, Porter JA, Tallarico JA, Engelman JA, Dranoff G, Bradner JE, Visser M, Solomon JM. Bonazzi S, et al. Among authors: kinyamu akunda j. Cell Chem Biol. 2023 Mar 16;30(3):235-247.e12. doi: 10.1016/j.chembiol.2023.02.005. Epub 2023 Mar 1. Cell Chem Biol. 2023. PMID: 36863346 Free article.
Antitarget Selectivity and Tolerability of Novel Pyrrolo[2,3-d]pyrimidine RET Inhibitors.
Mathison CJN, Yang Y, Nelson J, Huang Z, Jiang J, Chianelli D, Rucker PV, Roland J, Xie YF, Epple R, Bursulaya B, Lee C, Gao MY, Shaffer J, Briones S, Sarkisova Y, Galkin A, Li L, Li N, Li C, Hua S, Kasibhatla S, Kinyamu-Akunda J, Kikkawa R, Molteni V, Tellew JE. Mathison CJN, et al. Among authors: kinyamu akunda j. ACS Med Chem Lett. 2021 Nov 6;12(12):1912-1919. doi: 10.1021/acsmedchemlett.1c00450. eCollection 2021 Dec 9. ACS Med Chem Lett. 2021. PMID: 34917254 Free PMC article.
Species selection for nonclinical safety assessment of drug candidates: Examples of current industry practice.
Namdari R, Jones K, Chuang SS, Van Cruchten S, Dincer Z, Downes N, Mikkelsen LF, Harding J, Jäckel S, Jacobsen B, Kinyamu-Akunda J, Lortie A, Mhedhbi S, Mohr S, Schmitt MW, Prior H. Namdari R, et al. Among authors: kinyamu akunda j. Regul Toxicol Pharmacol. 2021 Nov;126:105029. doi: 10.1016/j.yrtph.2021.105029. Epub 2021 Aug 27. Regul Toxicol Pharmacol. 2021. PMID: 34455009 Free article.
Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4.
Fairhurst RA, Knoepfel T, Buschmann N, Leblanc C, Mah R, Todorov M, Nimsgern P, Ripoche S, Niklaus M, Warin N, Luu VH, Madoerin M, Wirth J, Graus-Porta D, Weiss A, Kiffe M, Wartmann M, Kinyamu-Akunda J, Sterker D, Stamm C, Adler F, Buhles A, Schadt H, Couttet P, Blank J, Galuba I, Trappe J, Voshol J, Ostermann N, Zou C, Berghausen J, Del Rio Espinola A, Jahnke W, Furet P. Fairhurst RA, et al. Among authors: kinyamu akunda j. J Med Chem. 2020 Nov 12;63(21):12542-12573. doi: 10.1021/acs.jmedchem.0c01019. Epub 2020 Oct 1. J Med Chem. 2020. PMID: 32930584
Efficacy and Tolerability of Pyrazolo[1,5-a]pyrimidine RET Kinase Inhibitors for the Treatment of Lung Adenocarcinoma.
Mathison CJN, Chianelli D, Rucker PV, Nelson J, Roland J, Huang Z, Yang Y, Jiang J, Xie YF, Epple R, Bursulaya B, Lee C, Gao MY, Shaffer J, Briones S, Sarkisova Y, Galkin A, Li L, Li N, Li C, Hua S, Kasibhatla S, Kinyamu-Akunda J, Kikkawa R, Molteni V, Tellew JE. Mathison CJN, et al. Among authors: kinyamu akunda j. ACS Med Chem Lett. 2020 Feb 12;11(4):558-565. doi: 10.1021/acsmedchemlett.0c00015. eCollection 2020 Apr 9. ACS Med Chem Lett. 2020. PMID: 32292564 Free PMC article.
FGF401, A First-In-Class Highly Selective and Potent FGFR4 Inhibitor for the Treatment of FGF19-Driven Hepatocellular Cancer.
Weiss A, Adler F, Buhles A, Stamm C, Fairhurst RA, Kiffe M, Sterker D, Centeleghe M, Wartmann M, Kinyamu-Akunda J, Schadt HS, Couttet P, Wolf A, Wang Y, Barzaghi-Rinaudo P, Murakami M, Kauffmann A, Knoepfel T, Buschmann N, Leblanc C, Mah R, Furet P, Blank J, Hofmann F, Sellers WR, Graus Porta D. Weiss A, et al. Among authors: kinyamu akunda j. Mol Cancer Ther. 2019 Dec;18(12):2194-2206. doi: 10.1158/1535-7163.MCT-18-1291. Epub 2019 Aug 13. Mol Cancer Ther. 2019. PMID: 31409633
Bile Acid Sequestration by Cholestyramine Mitigates FGFR4 Inhibition-Induced ALT Elevation.
Schadt HS, Wolf A, Mahl JA, Wuersch K, Couttet P, Schwald M, Fischer A, Lienard M, Emotte C, Teng CH, Skuba E, Richardson TA, Manenti L, Weiss A, Graus Porta D, Fairhurst RA, Kullak-Ublick GA, Chibout SD, Pognan F, Kluwe W, Kinyamu-Akunda J. Schadt HS, et al. Among authors: kinyamu akunda j. Toxicol Sci. 2018 May 1;163(1):265-278. doi: 10.1093/toxsci/kfy031. Toxicol Sci. 2018. PMID: 29432567 Free article.