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Discovery of a Novel Potent and Selective Calcium Release-Activated Calcium Channel Inhibitor: 2,6-Difluoro-N-(2'-methyl-3'-(4-methyl-5-oxo-4,5-dihydro-1,3,4-oxadiazol-2-yl)-[1,1'-biphenyl]-4-yl)benzamide. Structure-Activity Relationship and Preclinical Characterization.
Khedkar NR, Irlapatti NR, Dadke D, Kanoje V, Shaikh Z, Karche V, Shinde V, Deshmukh G, Patil A, Jachak S, Phukan S, Kizhakinagath PA, Gholve M, Bhankhede T, Daler J, Nemade HN, Budhe S, Pareek H, Yeshodharan R, Gupta R, Kalia A, Pandey D, Wagh A, Kumar S, Patil V, Modi D, Sharma N, Ahirrao P, Mehta M, Kumar H, Nigade P, Tamane K, Mallurwar S, Kuldharan S, Pawar S, Vishwase G, Bokan S, Singh M, Naik K, Ingawale S, Shankar R, Kamalakannan P, Venugopal S, George SK, Padiya KJ, Nemmani KVS, Gundu J, Bhonde M, Narasimham L, Sindkhedkar M, Shah C, Sinha N, Sharma S, Bakhle D, Kamboj RK, Palle VP. Khedkar NR, et al. Among authors: budhe s. J Med Chem. 2021 Dec 9;64(23):17004-17030. doi: 10.1021/acs.jmedchem.1c01403. Epub 2021 Nov 29. J Med Chem. 2021. PMID: 34843241
Discovery of Potent, Selective, and State-Dependent NaV1.7 Inhibitors with Robust Oral Efficacy in Pain Models: Structure-Activity Relationship and Optimization of Chroman and Indane Aryl Sulfonamides.
Ramdas V, Talwar R, Kanoje V, Loriya RM, Banerjee M, Patil P, Joshi AA, Datrange L, Das AK, Walke DS, Kalhapure V, Khan T, Gote G, Dhayagude U, Deshpande S, Shaikh J, Chaure G, Pal RR, Parkale S, Suravase S, Bhoskar S, Gupta RV, Kalia A, Yeshodharan R, Azhar M, Daler J, Mali V, Sharma G, Kishore A, Vyawahare R, Agarwal G, Pareek H, Budhe S, Nayak A, Warude D, Gupta PK, Joshi P, Joshi S, Darekar S, Pandey D, Wagh A, Nigade PB, Mehta M, Patil V, Modi D, Pawar S, Verma M, Singh M, Das S, Gundu J, Nemmani K, Bock MG, Sharma S, Bakhle D, Kamboj RK, Palle VP. Ramdas V, et al. Among authors: budhe s. J Med Chem. 2020 Jun 11;63(11):6107-6133. doi: 10.1021/acs.jmedchem.0c00361. Epub 2020 May 19. J Med Chem. 2020. PMID: 32368909
GABARAP sequesters the FLCN-FNIP tumor suppressor complex to couple autophagy with lysosomal biogenesis.
Goodwin JM, Walkup WG 4th, Hooper K, Li T, Kishi-Itakura C, Ng A, Lehmberg T, Jha A, Kommineni S, Fletcher K, Garcia-Fortanet J, Fan Y, Tang Q, Wei M, Agrawal A, Budhe SR, Rouduri SR, Baird D, Saunders J, Kiselar J, Chance MR, Ballabio A, Appleton BA, Brumell JH, Florey O, Murphy LO. Goodwin JM, et al. Among authors: budhe sr. Sci Adv. 2021 Oct;7(40):eabj2485. doi: 10.1126/sciadv.abj2485. Epub 2021 Oct 1. Sci Adv. 2021. PMID: 34597140 Free PMC article.