GR Dimerization and the Impact of GR Dimerization on GR Protein Stability and Half-Life.

ABSTRACT: Pharmacologically, glucocorticoids, which mediate their effects via the glucocorticoid receptor (GR), are a most effective therapy for inflammatory diseases despite the fact that chronic use causes side-effects and acquired GC resistance. The design of drugs with fewer side-effects and less potential for the development of resistance is therefore considered crucial for improved therapy. Dimerization of the GR is an integral step in glucocorticoid signaling and has been identified as a possible molecular site to target for drug development of anti-inflammatory drugs with an improved therapeutic index. Most of the current understanding regarding the role of GR dimerization in GC signaling derives for dimerization deficient mutants, although the role of ligands biased toward monomerization ha

SUBMITTER: Louw A 

PROVIDER: S-EPMC6653659 | biostudies-literature | 2019

REPOSITORIES: biostudies-literature