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Page 1
Optimization of LpxC Inhibitors for Antibacterial Activity and Cardiovascular Safety.
Cohen F, Aggen JB, Andrews LD, Assar Z, Boggs J, Choi T, Dozzo P, Easterday AN, Haglund CM, Hildebrandt DJ, Holt MC, Joly K, Jubb A, Kamal Z, Kane TR, Konradi AW, Krause KM, Linsell MS, Machajewski TD, Miroshnikova O, Moser HE, Nieto V, Phan T, Plato C, Serio AW, Seroogy J, Shakhmin A, Stein AJ, Sun AD, Sviridov S, Wang Z, Wlasichuk K, Yang W, Zhou X, Zhu H, Cirz RT. Cohen F, et al. Among authors: stein aj. ChemMedChem. 2019 Aug 20;14(16):1560-1572. doi: 10.1002/cmdc.201900287. Epub 2019 Aug 5. ChemMedChem. 2019. PMID: 31283109
Biochemical Characterization and Structure-Based Mutational Analysis Provide Insight into the Binding and Mechanism of Action of Novel Aspartate Aminotransferase Inhibitors.
Holt MC, Assar Z, Beheshti Zavareh R, Lin L, Anglin J, Mashadova O, Haldar D, Mullarky E, Kremer DM, Cantley LC, Kimmelman AC, Stein AJ, Lairson LL, Lyssiotis CA. Holt MC, et al. Among authors: stein aj. Biochemistry. 2018 Nov 27;57(47):6604-6614. doi: 10.1021/acs.biochem.8b00914. Epub 2018 Nov 12. Biochemistry. 2018. PMID: 30365304 Free PMC article.
Optimization of spirocyclic proline tryptophan hydroxylase-1 inhibitors.
Goldberg DR, De Lombaert S, Aiello R, Bourassa P, Barucci N, Zhang Q, Paralkar V, Stein AJ, Holt M, Valentine J, Zavadoski W. Goldberg DR, et al. Among authors: stein aj. Bioorg Med Chem Lett. 2017 Feb 1;27(3):413-419. doi: 10.1016/j.bmcl.2016.12.053. Epub 2016 Dec 23. Bioorg Med Chem Lett. 2017. PMID: 28041831
Difluoromethylene at the γ-Lactam α-Position Improves 11-Deoxy-8-aza-PGE1 Series EP4 Receptor Binding and Activity: 11-Deoxy-10,10-difluoro-8-aza-PGE1 Analog (KMN-159) as a Potent EP4 Agonist.
Barrett SD, Holt MC, Kramer JB, Germain B, Ho CS, Ciske FL, Kornilov A, Colombo JM, Uzieblo A, O'Malley JP, Owen TA, Stein AJ, Morano MI. Barrett SD, et al. Among authors: stein aj. J Med Chem. 2019 May 9;62(9):4731-4741. doi: 10.1021/acs.jmedchem.9b00336. Epub 2019 Apr 26. J Med Chem. 2019. PMID: 30964292
Discovery of acyl guanidine tryptophan hydroxylase-1 inhibitors.
Goldberg DR, De Lombaert S, Aiello R, Bourassa P, Barucci N, Zhang Q, Paralkar V, Stein AJ, Valentine J, Zavadoski W. Goldberg DR, et al. Among authors: stein aj. Bioorg Med Chem Lett. 2016 Jun 15;26(12):2855-2860. doi: 10.1016/j.bmcl.2016.04.057. Epub 2016 Apr 21. Bioorg Med Chem Lett. 2016. PMID: 27146606
Selective Inhibition of Autotaxin Is Efficacious in Mouse Models of Liver Fibrosis.
Bain G, Shannon KE, Huang F, Darlington J, Goulet L, Prodanovich P, Ma GL, Santini AM, Stein AJ, Lonergan D, King CD, Calderon I, Lai A, Hutchinson JH, Evans JF. Bain G, et al. Among authors: stein aj. J Pharmacol Exp Ther. 2017 Jan;360(1):1-13. doi: 10.1124/jpet.116.237156. Epub 2016 Oct 17. J Pharmacol Exp Ther. 2017. PMID: 27754931
Exploiting an Asp-Glu "switch" in glycogen synthase kinase 3 to design paralog-selective inhibitors for use in acute myeloid leukemia.
Wagner FF, Benajiba L, Campbell AJ, Weïwer M, Sacher JR, Gale JP, Ross L, Puissant A, Alexe G, Conway A, Back M, Pikman Y, Galinsky I, DeAngelo DJ, Stone RM, Kaya T, Shi X, Robers MB, Machleidt T, Wilkinson J, Hermine O, Kung A, Stein AJ, Lakshminarasimhan D, Hemann MT, Scolnick E, Zhang YL, Pan JQ, Stegmaier K, Holson EB. Wagner FF, et al. Among authors: stein aj. Sci Transl Med. 2018 Mar 7;10(431):eaam8460. doi: 10.1126/scitranslmed.aam8460. Sci Transl Med. 2018. PMID: 29515000 Free PMC article.
SALL4B, not targeted by IMiD, is important for SALL4-mediated tumorigenesis.
L Vu KA, Kumari K, Liu BH, Gao C, Li F, Tang JP, Maddalo D, Auld DS, Casalena DE, Tian X, Liu M, Bassal MA, Moein S, Iakovleva V, Tan JL, Stein AJ, Zhou Q, Fischer PD, Sigua LH, Qi J, Arthanari H, Tenen DG, Chai L. L Vu KA, et al. Among authors: stein aj. bioRxiv [Preprint]. 2023 Jul 7:2023.07.07.548071. doi: 10.1101/2023.07.07.548071. bioRxiv. 2023. PMID: 37461690 Free PMC article. Preprint.
58 results