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Defining Target Engagement Required for Efficacy In Vivo at the Retinoic Acid Receptor-Related Orphan Receptor C2 (RORγt).
Lugar CW, Clarke CA, Morphy R, Rudyk H, Sapmaz S, Stites RE, Vaught GM, Furness K, Broughton HB, Durst GL, Clawson DK, Stout SL, Guo SY, Durbin JD, Stayrook KR, Edmondson DD, Kikly K, New NE, Bina HA, Chambers MG, Shetler P, Chang WY, Chang VC, Barr R, Gough WH, Steele JP, Getman B, Patel N, Mathes BM, Richardson TI. Lugar CW, et al. J Med Chem. 2021 May 13;64(9):5470-5484. doi: 10.1021/acs.jmedchem.0c01918. Epub 2021 Apr 14. J Med Chem. 2021. PMID: 33852312
Design and synthesis of a potent and selective triazolone-based peroxisome proliferator-activated receptor alpha agonist.
Xu Y, Mayhugh D, Saeed A, Wang X, Thompson RC, Dominianni SJ, Kauffman RF, Singh J, Bean JS, Bensch WR, Barr RJ, Osborne J, Montrose-Rafizadeh C, Zink RW, Yumibe NP, Huang N, Luffer-Atlas D, Rungta D, Maise DE, Mantlo NB. Xu Y, et al. Among authors: barr rj. J Med Chem. 2003 Nov 20;46(24):5121-4. doi: 10.1021/jm034173l. J Med Chem. 2003. PMID: 14613314
Identification of potent and selective retinoic acid receptor gamma (RARγ) antagonists for the treatment of osteoarthritis pain using structure based drug design.
Hughes NE, Bleisch TJ, Jones SA, Richardson TI, Doti RA, Wang Y, Stout SL, Durst GL, Chambers MG, Oskins JL, Lin C, Adams LA, Page TJ, Barr RJ, Zink RW, Osborne H, Montrose-Rafizadeh C, Norman BH. Hughes NE, et al. Among authors: barr rj. Bioorg Med Chem Lett. 2016 Jul 15;26(14):3274-3277. doi: 10.1016/j.bmcl.2016.05.056. Epub 2016 May 20. Bioorg Med Chem Lett. 2016. PMID: 27261179
A peroxisome proliferator-activated receptor alpha/gamma dual agonist with a unique in vitro profile and potent glucose and lipid effects in rodent models of type 2 diabetes and dyslipidemia.
Reifel-Miller A, Otto K, Hawkins E, Barr R, Bensch WR, Bull C, Dana S, Klausing K, Martin JA, Rafaeloff-Phail R, Rafizadeh-Montrose C, Rhodes G, Robey R, Rojo I, Rungta D, Snyder D, Wilbur K, Zhang T, Zink R, Warshawsky A, Brozinick JT. Reifel-Miller A, et al. Mol Endocrinol. 2005 Jun;19(6):1593-605. doi: 10.1210/me.2005-0015. Epub 2005 Apr 14. Mol Endocrinol. 2005. PMID: 15831517
The hypolipidemic natural product guggulsterone is a promiscuous steroid receptor ligand.
Burris TP, Montrose C, Houck KA, Osborne HE, Bocchinfuso WP, Yaden BC, Cheng CC, Zink RW, Barr RJ, Hepler CD, Krishnan V, Bullock HA, Burris LL, Galvin RJ, Bramlett K, Stayrook KR. Burris TP, et al. Among authors: barr rj. Mol Pharmacol. 2005 Mar;67(3):948-54. doi: 10.1124/mol.104.007054. Epub 2004 Dec 15. Mol Pharmacol. 2005. PMID: 15602004
A natural product ligand of the oxysterol receptor, liver X receptor.
Bramlett KS, Houck KA, Borchert KM, Dowless MS, Kulanthaivel P, Zhang Y, Beyer TP, Schmidt R, Thomas JS, Michael LF, Barr R, Montrose C, Eacho PI, Cao G, Burris TP. Bramlett KS, et al. J Pharmacol Exp Ther. 2003 Oct;307(1):291-6. doi: 10.1124/jpet.103.052852. Epub 2003 Jul 31. J Pharmacol Exp Ther. 2003. PMID: 12893846
210 results