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Discovery and characterization of orally bioavailable 4-chloro-6-fluoroisophthalamides as covalent PPARG inverse-agonists.
Orsi DL, Ferrara SJ, Siegel S, Friberg A, Bouché L, Pook E, Lienau P, Bluck JP, Lemke CT, Akcay G, Stellfeld T, Meyer H, Pütter V, Holton SJ, Korr D, Jerchel-Furau I, Pantelidou C, Strathdee CA, Meyerson M, Eis K, Goldstein JT. Orsi DL, et al. Bioorg Med Chem. 2023 Jan 15;78:117130. doi: 10.1016/j.bmc.2022.117130. Epub 2022 Dec 13. Bioorg Med Chem. 2023. PMID: 36542958 Free article.
Correction to "Discovery and Structure-Based Design of Potent Covalent PPARγ Inverse-Agonists BAY-4931 and BAY-0069".
Orsi DL, Pook E, Bräuer N, Friberg A, Lienau P, Lemke CT, Stellfeld T, Brüggemeier U, Pütter V, Meyer H, Baco M, Tang S, Cherniack AD, Westlake L, Bender SA, Kocak M, Strathdee CA, Meyerson M, Eis K, Goldstein JT. Orsi DL, et al. J Med Chem. 2023 Jan 12;66(1):1082. doi: 10.1021/acs.jmedchem.2c02002. Epub 2022 Dec 21. J Med Chem. 2023. PMID: 36542814 Free PMC article. No abstract available.
Discovery and Structure-Based Design of Potent Covalent PPARγ Inverse-Agonists BAY-4931 and BAY-0069.
Orsi DL, Pook E, Bräuer N, Friberg A, Lienau P, Lemke CT, Stellfeld T, Brüggemeier U, Pütter V, Meyer H, Baco M, Tang S, Cherniack AD, Westlake L, Bender SA, Kocak M, Strathdee CA, Meyerson M, Eis K, Goldstein JT. Orsi DL, et al. J Med Chem. 2022 Nov 10;65(21):14843-14863. doi: 10.1021/acs.jmedchem.2c01379. Epub 2022 Oct 21. J Med Chem. 2022. PMID: 36270630 Free PMC article.
Development of VU6019650: A Potent, Highly Selective, and Systemically Active Orthosteric Antagonist of the M5 Muscarinic Acetylcholine Receptor for the Treatment of Opioid Use Disorder.
Garrison AT, Orsi DL, Capstick RA, Whomble D, Li J, Carter TR, Felts AS, Vinson PN, Rodriguez AL, Han A, Hajari K, Cho HP, Teal LB, Ragland MG, Ghamari-Langroudi M, Bubser M, Chang S, Schnetz-Boutaud NC, Boutaud O, Blobaum AL, Foster DJ, Niswender CM, Conn PJ, Lindsley CW, Jones CK, Han C. Garrison AT, et al. Among authors: orsi dl. J Med Chem. 2022 Apr 28;65(8):6273-6286. doi: 10.1021/acs.jmedchem.2c00192. Epub 2022 Apr 13. J Med Chem. 2022. PMID: 35417155
15 results