Divergent effects of strontium and calcium-sensing receptor positive allosteric modulators (calcimimetics) on human osteoclast activity.

ABSTRACT:

Background and purpose

Strontium ranelate, a drug approved and until recently used for the treatment of osteoporosis, mediates its effects on bone at least in part via the calcium-sensing (CaS) receptor. However, it is not known whether bone-targeted CaS receptor positive allosteric modulators (PAMs; calcimimetics) represent an alternative (or adjunctive) therapy to strontium (Sr²⁺ _o ).

Experimental approach

We assessed three structurally distinct calcimimetics [cinacalcet, AC-265347 and a benzothiazole tri-substituted urea (BTU-compound 13)], alone and in combination with extracellular calcium (Ca²⁺ _o ) or Sr²⁺ _o , in G protein-dependent signalling assays and trafficking experiments in HEK293 cells and their

SUBMITTER: Diepenhorst NA 

PROVIDER: S-EPMC6177624 | biostudies-literature | 2018 Nov

REPOSITORIES: biostudies-literature