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Discovery of Bispecific Antagonists of Retinol Binding Protein 4 That Stabilize Transthyretin Tetramers: Scaffolding Hopping, Optimization, and Preclinical Pharmacological Evaluation as a Potential Therapy for Two Common Age-Related Comorbidities.
Cioffi CL, Muthuraman P, Raja A, Varadi A, Racz B, Petrukhin K. Cioffi CL, et al. J Med Chem. 2020 Oct 8;63(19):11054-11084. doi: 10.1021/acs.jmedchem.0c00996. Epub 2020 Sep 17. J Med Chem. 2020. PMID: 32878437 Free PMC article.
Identification of Transthyretin Tetramer Kinetic Stabilizers That Are Capable of Inhibiting the Retinol-Dependent Retinol Binding Protein 4-Transthyretin Interaction: Potential Novel Therapeutics for Macular Degeneration, Transthyretin Amyloidosis, and Their Common Age-Related Comorbidities.
Cioffi CL, Raja A, Muthuraman P, Jayaraman A, Jayakumar S, Varadi A, Racz B, Petrukhin K. Cioffi CL, et al. J Med Chem. 2021 Jul 8;64(13):9010-9041. doi: 10.1021/acs.jmedchem.1c00099. Epub 2021 Jun 17. J Med Chem. 2021. PMID: 34138572 Free PMC article.
Design, synthesis, and SAR of N-((1-(4-(propylsulfonyl)piperazin-1-yl)cycloalkyl)methyl)benzamide inhibitors of glycine transporter-1.
Cioffi CL, Wolf MA, Guzzo PR, Sadalapure K, Parthasarathy V, Dethe D, Maeng JH, Carulli E, Loong DT, Fang X, Hu M, Gupta P, Chung M, Bai M, Moore N, Luche M, Khmelnitsky Y, Love PL, Watson MA, Mhyre AJ, Liu S. Cioffi CL, et al. Bioorg Med Chem Lett. 2013 Mar 1;23(5):1257-61. doi: 10.1016/j.bmcl.2013.01.006. Epub 2013 Jan 11. Bioorg Med Chem Lett. 2013. PMID: 23380375
49 results