Pharmacokinetic Optimization of CCG-203971: Novel Inhibitors of the Rho/MRTF/SRF Transcriptional Pathway as Potential Antifibrotic Therapeutics for Systemic Scleroderma

We recently reported the development of a novel inhibitor of Rho-mediated gene transcription (1, CCG-203971) that is efficacious in multiple animal models of acute fibrosis, including scleroderma, when given intraperitoneally. The modest in vivo potency and poor pharmacokinetics (PK) of this lead, h...

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Bibliografske podrobnosti
izdano v:Bioorg Med Chem Lett
Main Authors: Hutchings, Kim M., Lisabeth, Erika M., Rajeswaran, Walajapet, Wilson, Michael W., Sorenson, Roderick J., Campbell, Phillip L., Ruth, Jeffrey H., Amin, Asif, Tsou, Pei-Suen, Leipprandt, Jeffrey R., Olson, Samuel R., Wen, Bo, Zhao, Ting, Sun, Duxin, Khanna, Dinesh, Fox, David A., Neubig, Richard R., Larsen, Scott D.
Format: Artigo
Jezik:Inglês
Izdano: 2017
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Article
Online dostop:https://ncbi.nlm.nih.gov/pmc/articles/PMC5395305/
https://ncbi.nlm.nih.gov/pubmed/28285914
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2017.02.070
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