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Glucocorticoid receptor modulators informed by crystallography lead to a new rationale for receptor selectivity, function, and implications for structure-based design.
Carson MW, Luz JG, Suen C, Montrose C, Zink R, Ruan X, Cheng C, Cole H, Adrian MD, Kohlman DT, Mabry T, Snyder N, Condon B, Maletic M, Clawson D, Pustilnik A, Coghlan MJ. Carson MW, et al. Among authors: luz jg. J Med Chem. 2014 Feb 13;57(3):849-60. doi: 10.1021/jm401616g. Epub 2014 Feb 4. J Med Chem. 2014. PMID: 24446728
Structure-based, multi-targeted drug discovery approach to eicosanoid inhibition: Dual inhibitors of mPGES-1 and 5-lipoxygenase activating protein (FLAP).
Ho JD, Lee MR, Rauch CT, Aznavour K, Park JS, Luz JG, Antonysamy S, Condon B, Maletic M, Zhang A, Hickey MJ, Hughes NE, Chandrasekhar S, Sloan AV, Gooding K, Harvey A, Yu XP, Kahl SD, Norman BH. Ho JD, et al. Among authors: luz jg. Biochim Biophys Acta Gen Subj. 2021 Feb;1865(2):129800. doi: 10.1016/j.bbagen.2020.129800. Epub 2020 Nov 25. Biochim Biophys Acta Gen Subj. 2021. PMID: 33246032
Discovery and Characterization of 2-Acylaminoimidazole Microsomal Prostaglandin E Synthase-1 Inhibitors.
Schiffler MA, Antonysamy S, Bhattachar SN, Campanale KM, Chandrasekhar S, Condon B, Desai PV, Fisher MJ, Groshong C, Harvey A, Hickey MJ, Hughes NE, Jones SA, Kim EJ, Kuklish SL, Luz JG, Norman BH, Rathmell RE, Rizzo JR, Seng TW, Thibodeaux SJ, Woods TA, York JS, Yu XP. Schiffler MA, et al. Among authors: luz jg. J Med Chem. 2016 Jan 14;59(1):194-205. doi: 10.1021/acs.jmedchem.5b01249. Epub 2015 Dec 18. J Med Chem. 2016. PMID: 26653180
2-Chloro-4-[[(1R,2R)-2-hydroxy-2-methyl-cyclopentyl]amino]-3-methyl-benzonitrile: A Transdermal Selective Androgen Receptor Modulator (SARM) for Muscle Atrophy.
Saeed A, Vaught GM, Gavardinas K, Matthews D, Green JE, Losada PG, Bullock HA, Calvert NA, Patel NJ, Sweetana SA, Krishnan V, Henck JW, Luz JG, Wang Y, Jadhav P. Saeed A, et al. Among authors: luz jg. J Med Chem. 2016 Jan 28;59(2):750-5. doi: 10.1021/acs.jmedchem.5b01168. Epub 2016 Jan 7. J Med Chem. 2016. PMID: 26683992
Characterization of 3,3-dimethyl substituted N-aryl piperidines as potent microsomal prostaglandin E synthase-1 inhibitors.
Kuklish SL, Antonysamy S, Bhattachar SN, Chandrasekhar S, Fisher MJ, Fretland AJ, Gooding K, Harvey A, Hughes NE, Luz JG, Manninen PR, McGee JE, Navarro A, Norman BH, Partridge KM, Quimby SJ, Schiffler MA, Sloan AV, Warshawsky AM, York JS, Yu XP. Kuklish SL, et al. Among authors: luz jg. Bioorg Med Chem Lett. 2016 Oct 1;26(19):4824-4828. doi: 10.1016/j.bmcl.2016.08.023. Epub 2016 Aug 10. Bioorg Med Chem Lett. 2016. PMID: 27554445
The 2.5 Å crystal structure of the SIRT1 catalytic domain bound to nicotinamide adenine dinucleotide (NAD+) and an indole (EX527 analogue) reveals a novel mechanism of histone deacetylase inhibition.
Zhao X, Allison D, Condon B, Zhang F, Gheyi T, Zhang A, Ashok S, Russell M, MacEwan I, Qian Y, Jamison JA, Luz JG. Zhao X, et al. Among authors: luz jg. J Med Chem. 2013 Feb 14;56(3):963-9. doi: 10.1021/jm301431y. Epub 2013 Jan 29. J Med Chem. 2013. PMID: 23311358
Discovery and characterization of [(cyclopentyl)ethyl]benzoic acid inhibitors of microsomal prostaglandin E synthase-1.
Partridge KM, Antonysamy S, Bhattachar SN, Chandrasekhar S, Fisher MJ, Fretland A, Gooding K, Harvey A, Hughes NE, Kuklish SL, Luz JG, Manninen PR, McGee JE, Mudra DR, Navarro A, Norman BH, Quimby SJ, Schiffler MA, Sloan AV, Warshawsky AM, Weller JM, York JS, Yu XP. Partridge KM, et al. Among authors: luz jg. Bioorg Med Chem Lett. 2017 Mar 15;27(6):1478-1483. doi: 10.1016/j.bmcl.2016.11.011. Epub 2016 Nov 7. Bioorg Med Chem Lett. 2017. PMID: 28190634
Structures of PHR domains from Mus musculus Phr1 (Mycbp2) explain the loss-of-function mutation (Gly1092-->Glu) of the C. elegans ortholog RPM-1.
Sampathkumar P, Ozyurt SA, Miller SA, Bain KT, Rutter ME, Gheyi T, Abrams B, Wang Y, Atwell S, Luz JG, Thompson DA, Wasserman SR, Emtage JS, Park EC, Rongo C, Jin Y, Klemke RL, Sauder JM, Burley SK. Sampathkumar P, et al. Among authors: luz jg. J Mol Biol. 2010 Apr 9;397(4):883-92. doi: 10.1016/j.jmb.2010.02.017. Epub 2010 Feb 13. J Mol Biol. 2010. PMID: 20156452 Free PMC article.
102 results