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Updated: Jul 4, 2026

Chemical Inactivation of the E3 Ubiquitin Ligase Cereblon by Pomalidomide-based Homo-PROTACs
Published on: May 15, 2019
CCR1 antagonists
1Tanabe Research Laboratories-USA, Inc., San Diego, CA 92121, USA. jcheng@trlusa.com
Abstract:
CCR1 (CC Chemokine receptor 1) is a widely studied G protein-coupled receptor target expressed on multiple types of leukocytes. It is implicated in initiating and exacerbating inflammatory conditions and thus is viewed as a good target for autoimmune and inflammatory therapeutic applications. Numerous CCR1 antagonists have been reported. Although some early CCR1 antagonists lacked the species cross reactivity that made in vivo animal model study difficult, efforts have been made to improve the compound potency in rodents. Recent identification of new and improved CCR1 antagonists has resulted in promising, in vivo efficacy in a variety of animal models of disease. While several early compounds have been withdrawn from clinical trials due to lack of efficacy, work continues to evaluate CCR1 antagonists in preclinical and clinical settings.
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