BioCentury
ARTICLE | Targets & Mechanisms

Insider signaling

Takeda believes endosomal signaling for substance P could revive the pain target

July 13, 2017 9:45 PM UTC

With evidence mounting that cell surface receptors keep signaling after they are internalized, a Takeda-backed study from Monash University has shown how the phenomenon could solve the riddle of why antagonists of the substance P receptor failed as analgesics in the clinic, despite having shown so much preclinical promise. Using compounds that act only in the endosome, the partners want to lead the way in rethinking targeting of GPCRs to produce greater efficacy.

The findings could not only open the door to a new class of inhibitors for GPCRs, but also re-ignite interest in the pain target at a time when the need for non-opioid analgesics is gaining national attention...