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Structural Determinants for Small-Molecule Activation of Skeletal Muscle AMPK α2β2γ1 by the Glucose Importagog SC4.
Ngoei KRW, Langendorf CG, Ling NXY, Hoque A, Varghese S, Camerino MA, Walker SR, Bozikis YE, Dite TA, Ovens AJ, Smiles WJ, Jacobs R, Huang H, Parker MW, Scott JW, Rider MH, Foitzik RC, Kemp BE, Baell JB, Oakhill JS. Ngoei KRW, et al. Among authors: varghese s. Cell Chem Biol. 2018 Jun 21;25(6):728-737.e9. doi: 10.1016/j.chembiol.2018.03.008. Epub 2018 Apr 12. Cell Chem Biol. 2018. PMID: 29657085 Free article.
Discovery of Benzoylsulfonohydrazides as Potent Inhibitors of the Histone Acetyltransferase KAT6A.
Leaver DJ, Cleary B, Nguyen N, Priebbenow DL, Lagiakos HR, Sanchez J, Xue L, Huang F, Sun Y, Mujumdar P, Mudududdla R, Varghese S, Teguh S, Charman SA, White KL, Katneni K, Cuellar M, Strasser JM, Dahlin JL, Walters MA, Street IP, Monahan BJ, Jarman KE, Sabroux HJ, Falk H, Chung MC, Hermans SJ, Parker MW, Thomas T, Baell JB. Leaver DJ, et al. Among authors: varghese s. J Med Chem. 2019 Aug 8;62(15):7146-7159. doi: 10.1021/acs.jmedchem.9b00665. Epub 2019 Jul 17. J Med Chem. 2019. PMID: 31256587
Crystal structure of the M5 muscarinic acetylcholine receptor.
Vuckovic Z, Gentry PR, Berizzi AE, Hirata K, Varghese S, Thompson G, van der Westhuizen ET, Burger WAC, Rahmani R, Valant C, Langmead CJ, Lindsley CW, Baell JB, Tobin AB, Sexton PM, Christopoulos A, Thal DM. Vuckovic Z, et al. Among authors: varghese s. Proc Natl Acad Sci U S A. 2019 Dec 17;116(51):26001-26007. doi: 10.1073/pnas.1914446116. Epub 2019 Nov 26. Proc Natl Acad Sci U S A. 2019. PMID: 31772027 Free PMC article.
Synthesis and structure-activity relationship study of pyrrolidine-oxadiazoles as anthelmintics against Haemonchus contortus.
Ruan B, Zhang Y, Tadesse S, Preston S, Taki AC, Jabbar A, Hofmann A, Jiao Y, Garcia-Bustos J, Harjani J, Le TG, Varghese S, Teguh S, Xie Y, Odiba J, Hu M, Gasser RB, Baell J. Ruan B, et al. Among authors: varghese s. Eur J Med Chem. 2020 Mar 15;190:112100. doi: 10.1016/j.ejmech.2020.112100. Epub 2020 Jan 25. Eur J Med Chem. 2020. PMID: 32018095
Discovery of Acylsulfonohydrazide-Derived Inhibitors of the Lysine Acetyltransferase, KAT6A, as Potent Senescence-Inducing Anti-Cancer Agents.
Priebbenow DL, Leaver DJ, Nguyen N, Cleary B, Lagiakos HR, Sanchez J, Xue L, Huang F, Sun Y, Mujumdar P, Mudududdla R, Varghese S, Teguh S, Charman SA, White KL, Shackleford DM, Katneni K, Cuellar M, Strasser JM, Dahlin JL, Walters MA, Street IP, Monahan BJ, Jarman KE, Jousset Sabroux H, Falk H, Chung MC, Hermans SJ, Downer NL, Parker MW, Voss AK, Thomas T, Baell JB. Priebbenow DL, et al. Among authors: varghese s. J Med Chem. 2020 May 14;63(9):4655-4684. doi: 10.1021/acs.jmedchem.9b02071. Epub 2020 Mar 19. J Med Chem. 2020. PMID: 32118427
Discovery of Potent N-Ethylurea Pyrazole Derivatives as Dual Inhibitors of Trypanosoma brucei and Trypanosoma cruzi.
Varghese S, Rahmani R, Russell S, Deora GS, Ferrins L, Toynton A, Jones A, Sykes M, Kessler A, Eufrásio A, Cordeiro AT, Sherman J, Rodriguez A, Avery VM, Piggott MJ, Baell JB. Varghese S, et al. ACS Med Chem Lett. 2019 Sep 9;11(3):278-285. doi: 10.1021/acsmedchemlett.9b00218. eCollection 2020 Mar 12. ACS Med Chem Lett. 2019. PMID: 32184957 Free PMC article.
Hit-to-lead optimization of novel phenyl imidazole carboxamides that are active against Leishmania donovani.
McNamara N, Saunders E, Varghese S, Zheng R, Simpson K, Varma DM, Johnson MM, Hasan Zahid MS, Bachelder EM, Ainslie KM, No JH, Koh D, Shum D, Das N, Patra B, Roy J, Talukdar A, Ganguly D, McConville M, Baell J. McNamara N, et al. Among authors: varghese s. Eur J Med Chem. 2022 Oct 5;240:114577. doi: 10.1016/j.ejmech.2022.114577. Epub 2022 Jul 1. Eur J Med Chem. 2022. PMID: 35810535
863 results