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GPR65 inhibition counteracts low pH-dependant immunosuppressive effects on immune cells and displays pronounced anti-tumor activity in mice: Identification of PTT-4256 as a clinical drug candidate.Download Poster
PTT-4256 is a first-in-class GPR65 inhibitor that reverses the immuno-suppressive effects of acidic pH in macrophages, activates anti-tumorigenic pathways in the tumor microenvironment and displays single agent anti-tumor efficacy in mice.Download Poster
Inhibition of GPR65 counteracts low pH-induced immuno-suppressive polarization of macrophages. In vitro and in vivo characterization of potent, selective and orally bioavailable small molecule GPR65 antagonists.Download Poster
Inhibition of acid sensing by GPR65 normalizes gene expression in macrophages, increases immune cell infiltration in tumors, and restrains subcutaneous MC38 growth in mice.Download Poster
GPR65 is a critical mediator of low pH-induced immunosuppressive signalling in tumor associated macrophages: human target validation of a novel innate immune checkpoint and small molecule inhibitor drug discovery.Download Poster