[HTML][HTML] Allosteric modulation of the calcium-sensing receptor rectifies signaling abnormalities associated with G-protein α-11 mutations causing hypercalcemic and …
Germline loss-and gain-of-function mutations of G-protein α-11 (Gα 11), which couples the
calcium-sensing receptor (CaSR) to intracellular calcium (Ca 2+ i) signaling, lead to familial
hypocalciuric hypercalcemia type 2 (FHH2) and autosomal dominant hypocalcemia type 2
(ADH2), respectively, whereas somatic Gα 11 mutations mediate uveal melanoma
development by constitutively up-regulating MAPK signaling. Cinacalcet and NPS-2143 are
allosteric CaSR activators and inactivators, respectively, that ameliorate signaling …
calcium-sensing receptor (CaSR) to intracellular calcium (Ca 2+ i) signaling, lead to familial
hypocalciuric hypercalcemia type 2 (FHH2) and autosomal dominant hypocalcemia type 2
(ADH2), respectively, whereas somatic Gα 11 mutations mediate uveal melanoma
development by constitutively up-regulating MAPK signaling. Cinacalcet and NPS-2143 are
allosteric CaSR activators and inactivators, respectively, that ameliorate signaling …