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Page 1
Exploration of macrocyclic peptide binders to the extracellular CRD domain of human receptor tyrosine kinase-like orphan receptor 1 (ROR1).
Qiao JX, Witmer MR, Lee V, Wang TC, Reid PC, Arioka Y, Farr G, Hill-Drzewi M, Schweizer L, Yamniuk A, Cheng L, Abramczyk B, Corbett M, Calambur D, Szapiel N, Ryseck R, Ponath P, Poss MA, Carter P. Qiao JX, et al. Among authors: szapiel n. Bioorg Med Chem Lett. 2024 Jan 15;98:129589. doi: 10.1016/j.bmcl.2023.129589. Epub 2023 Dec 13. Bioorg Med Chem Lett. 2024. PMID: 38097140
Discovery of 2-(Anilino)pyrimidine-4-carboxamides as Highly Potent, Selective, and Orally Active Glycogen Synthase Kinase-3 (GSK-3) Inhibitors.
Hartz RA, Ahuja VT, Luo G, Chen L, Sivaprakasam P, Xiao H, Krause CM, Clarke WJ, Xu S, Tokarski JS, Kish K, Lewis H, Szapiel N, Ravirala R, Mutalik S, Nakmode D, Shah D, Burton CR, Macor JE, Dubowchik GM. Hartz RA, et al. Among authors: szapiel n. J Med Chem. 2023 Jun 8;66(11):7534-7552. doi: 10.1021/acs.jmedchem.3c00364. Epub 2023 May 26. J Med Chem. 2023. PMID: 37235865
Design, Structure-Activity Relationships, and In Vivo Evaluation of Potent and Brain-Penetrant Imidazo[1,2-b]pyridazines as Glycogen Synthase Kinase-3β (GSK-3β) Inhibitors.
Hartz RA, Ahuja VT, Sivaprakasam P, Xiao H, Krause CM, Clarke WJ, Kish K, Lewis H, Szapiel N, Ravirala R, Mutalik S, Nakmode D, Shah D, Burton CR, Macor JE, Dubowchik GM. Hartz RA, et al. Among authors: szapiel n. J Med Chem. 2023 Mar 23;66(6):4231-4252. doi: 10.1021/acs.jmedchem.3c00133. Epub 2023 Mar 9. J Med Chem. 2023. PMID: 36950863
Discovery of Pyridazinone and Pyrazolo[1,5-a]pyridine Inhibitors of C-Terminal Src Kinase.
O'Malley DP, Ahuja V, Fink B, Cao C, Wang C, Swanson J, Wee S, Gavai AV, Tokarski J, Critton D, Paiva AA, Johnson BM, Szapiel N, Xie D. O'Malley DP, et al. Among authors: szapiel n. ACS Med Chem Lett. 2019 Sep 25;10(10):1486-1491. doi: 10.1021/acsmedchemlett.9b00354. eCollection 2019 Oct 10. ACS Med Chem Lett. 2019. PMID: 31620238 Free PMC article.
Discovery of new acylaminopyridines as GSK-3 inhibitors by a structure guided in-depth exploration of chemical space around a pyrrolopyridinone core.
Sivaprakasam P, Han X, Civiello RL, Jacutin-Porte S, Kish K, Pokross M, Lewis HA, Ahmed N, Szapiel N, Newitt JA, Baldwin ET, Xiao H, Krause CM, Park H, Nophsker M, Lippy JS, Burton CR, Langley DR, Macor JE, Dubowchik GM. Sivaprakasam P, et al. Among authors: szapiel n. Bioorg Med Chem Lett. 2015 May 1;25(9):1856-63. doi: 10.1016/j.bmcl.2015.03.046. Epub 2015 Mar 24. Bioorg Med Chem Lett. 2015. PMID: 25845281