Modeling of human prokineticin receptors: interactions with novel small-molecule binders and potential off-target drugs.

ABSTRACT:

Background and motivation

The Prokineticin receptor (PKR) 1 and 2 subtypes are novel members of family A GPCRs, which exhibit an unusually high degree of sequence similarity. Prokineticins (PKs), their cognate ligands, are small secreted proteins of ∼80 amino acids; however, non-peptidic low-molecular weight antagonists have also been identified. PKs and their receptors play important roles under various physiological conditions such as maintaining circadian rhythm and pain perception, as well as regulating angiogenesis and modulating immunity. Identifying binding sites for known antagonists and for additional potential binders will facilitate studying and regulating these novel receptors. Blocking PKRs may serve as a therapeutic tool for various diseases, including acute pain, inf

SUBMITTER: Levit A 

PROVIDER: S-EPMC3221691 | biostudies-literature | 2011

REPOSITORIES: biostudies-literature