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Page 1
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. Among authors: durst gl. 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
Acyl sulfonamide anti-proliferatives: benzene substituent structure-activity relationships for a novel class of antitumor agents.
Lobb KL, Hipskind PA, Aikins JA, Alvarez E, Cheung YY, Considine EL, De Dios A, Durst GL, Ferritto R, Grossman CS, Giera DD, Hollister BA, Huang Z, Iversen PW, Law KL, Li T, Lin HS, Lopez B, Lopez JE, Cabrejas LM, McCann DJ, Molero V, Reilly JE, Richett ME, Shih C, Teicher B, Wikel JH, White WT, Mader MM. Lobb KL, et al. Among authors: durst gl. J Med Chem. 2004 Oct 21;47(22):5367-80. doi: 10.1021/jm030594r. J Med Chem. 2004. PMID: 15481975
Design and synthesis of a novel series of [1-(4-hydroxy-benzyl)-1H-indol-5-yloxy]-acetic acid compounds as potent, selective, thyroid hormone receptor β agonists.
Burkholder TP, Cunningham BE, Clayton JR, Lander PA, Brown ML, Doti RA, Durst GL, Montrose-Rafizadeh C, King C, Osborne HE, Amos RM, Zink RW, Stramm LE, Burris TP, Cardona G, Konkol DL, Reidy C, Christe ME, Genin MJ. Burkholder TP, et al. Among authors: durst gl. Bioorg Med Chem Lett. 2015 Apr 1;25(7):1377-80. doi: 10.1016/j.bmcl.2015.02.062. Epub 2015 Mar 3. Bioorg Med Chem Lett. 2015. PMID: 25752984
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: durst gl. 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
SHIP1 therapeutic target enablement: Identification and evaluation of inhibitors for the treatment of late-onset Alzheimer's disease.
Jesudason CD, Mason ER, Chu S, Oblak AL, Javens-Wolfe J, Moussaif M, Durst G, Hipskind P, Beck DE, Dong J, Amarasinghe O, Zhang ZY, Hamdani AK, Singhal K, Mesecar AD, Souza S, Jacobson M, Salvo JD, Soni DM, Kandasamy M, Masters AR, Quinney SK, Doolen S, Huhe H, Rizzo SJS, Lamb BT, Palkowitz AD, Richardson TI. Jesudason CD, et al. Alzheimers Dement (N Y). 2023 Nov 17;9(4):e12429. doi: 10.1002/trc2.12429. eCollection 2023 Oct-Dec. Alzheimers Dement (N Y). 2023. PMID: 38023622 Free PMC article.
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