Phorbol Ester- and Growth Factor-Induced Growth Hormone (GH) Receptor Proteolysis and GH-Binding Protein Shedding: Relationship to GH Receptor Down-Regulation1

View Full Paper

Ask AI

Bookmark

Population

Murine 3T3-F442A and 3T3-L1 preadipocytes, and Chinese hamster ovary cells stably expressing rabbit GHR

Comparison

Phorbol ester, N-ethylmaleimide… vs Control conditions or pretreatment with inhibitors

Design

Preclinical

Authors

Discussion

Metalloprotease-mediated GHR proteolysis may downregulate GH signaling; leaves open whether hydroxamate inhibitors enhance GH action in vivo.

Population

Murine 3T3-F442A and 3T3-L1 preadipocytes, and Chinese hamster ovary (CHO) cells stably expressing rabbit GHR (rbGHR)

Intervention

Phorbol ester (PMA), N-ethylmaleimide, platelet-derived growth factor (PDGF), and serum

Comparator

Control conditions or pretreatment with inhibitors (IC3, MAPK/ERK kinase 1 inhibitors)

Outcome

GHR proteolysis, GHBP shedding, and GH-induced activation of Janus kinase-2surrogate

Inducible metalloprotease-mediated GHR proteolysis constitutes an important mechanism of receptor down-regulation and modulation of GH signaling.

Guan et al. (2001) studied this question.

View Full Paper

Ask AI

Bookmark

Metalloprotease-mediated GHR proteolysis may downregulate GH signaling; leaves open whether hydroxamate inhibitors enhance GH action in vivo.