Discovery of 1-(Phenylsulfonyl)-1,2,3,4-tetrahydroquinoline Derivative as Orally Bioavailable and Safe RORγt Inverse Agonists for Potential Treatment of Rheumatoid Arthritis.
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DOI: 10.1021/acs.jmedchem.4c01727
Abstract: The retinoic acid receptor-related orphan receptor γt (RORγt) is a key regulator of Th17 cells, associated with autoimmune diseases, making it a significant drug target. Herein, we designed and synthesized 1-(phenylsulfonyl)-1,2,3,4-tetrahydroquinoline derivatives, improving upon GSK2981278… read more here.
Keywords: ror inverse; rheumatoid arthritis; orally bioavailable; phenylsulfonyl tetrahydroquinoline ... See more keywords
Discovery of Novel N-Sulfonamide-tetrahydroquinolines as Potent Retinoic Acid Receptor-Related Orphan Receptor γt (RORγt) Inverse Agonists for the Treatment of Psoriasis.
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DOI: 10.1021/acs.jmedchem.4c02318
Abstract: Guided by the mode of action of 13, our previously discovered RORγt inverse agonist, we conducted five rounds of design syntheses and structure-activity relationship (SAR) studies, ultimately identifying RORγt inverse agonist 5a, which exhibited superior… read more here.
Keywords: receptor; ror inverse; discovery novel; inverse agonist ... See more keywords
Design, Synthesis, and Biological Evaluation of Retinoic Acid-Related Orphan Receptor γt (RORγt) Agonist Structure-Based Functionality Switching Approach from In House RORγt Inverse Agonist to RORγt Agonist.
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DOI: 10.1021/acs.jmedchem.8b01181
Abstract: Retinoic acid receptor-related orphan receptor γt (RORγt) agonists are expected to provide a novel class of immune-activating anticancer drugs via activation of Th17 cells and Tc17 cells. Herein, we describe a novel structure-based functionality switching… read more here.
Keywords: agonist; ror; chemistry; ror agonist ... See more keywords
Novel Tricyclic Pyroglutamide Derivatives as Potent RORγt Inverse Agonists Identified using a Virtual Screening Approach.
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DOI: 10.1021/acsmedchemlett.0c00496
Abstract: Employing a virtual screening approach, we identified the pyroglutamide moiety as a nonacid replacement for the cyclohexanecarboxylic acid group which, when coupled to our previously reported conformationally locked tricyclic core, provided potent and selective RORγt… read more here.
Keywords: virtual screening; ror; screening approach; inverse agonists ... See more keywords
RORγt inverse agonists demonstrating a margin between inhibition of IL-17A and thymocyte apoptosis
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DOI: 10.1371/journal.pone.0317090
Abstract: Multiple genetic associations suggest a causative relationship between Th17-related genes coding for proteins, such as IL-17A, IL-23 and STAT3, and psoriasis. Further support for this link comes from the findings that neutralizing antibodies directed against… read more here.
Keywords: inverse agonists; ror; ror inverse; agonists demonstrating ... See more keywords