Abstract: Recruitment of suppressive CD4+ Foxp3+ regulatory T cells (Treg) to the tumor microenvironment (TME) is suspected to be a key driver in tumor immune evasion. Inhibiting mechanisms of Treg recruitment to the TME is hypothesized to activate the immune system against tumors. A major mechanism of tumor Treg recruitment is the chemoattraction of Treg to the chemokines CCL17 and CCL22, which recruit Treg by binding the chemokine receptor CCR4. The discovery of potent, selective, and orally bioavailable inhibitors of CCR4 and their effects in in vivo models is described. The design, synthesis, and ADME properties of key compounds will also be discussed.

Preventing regulatory T cell trafficking into the tumor microenvironment: Discovery of potent and selective CCR4 antagonists

256th National Meeting (2018)

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.