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Structure paper

TitleStructural basis for activation and allosteric modulation of full-length calcium-sensing receptor.
Journal, issue, pagesSci Adv, Vol. 7, Issue 23, Year 2021
Publish dateJun 4, 2021
AuthorsTianlei Wen / Ziyu Wang / Xiaozhe Chen / Yue Ren / Xuhang Lu / Yangfei Xing / Jing Lu / Shenghai Chang / Xing Zhang / Yuequan Shen / Xue Yang /
PubMed AbstractCalcium-sensing receptor (CaSR) is a class C G protein-coupled receptor (GPCR) that plays an important role in calcium homeostasis and parathyroid hormone secretion. Here, we present multiple cryo- ...Calcium-sensing receptor (CaSR) is a class C G protein-coupled receptor (GPCR) that plays an important role in calcium homeostasis and parathyroid hormone secretion. Here, we present multiple cryo-electron microscopy structures of full-length CaSR in distinct ligand-bound states. Ligands (Ca and l-tryptophan) bind to the extracellular domain of CaSR and induce large-scale conformational changes, leading to the closure of two heptahelical transmembrane domains (7TMDs) for activation. The positive modulator (evocalcet) and the negative allosteric modulator (NPS-2143) occupy the similar binding pocket in 7TMD. The binding of NPS-2143 causes a considerable rearrangement of two 7TMDs, forming an inactivated TM6/TM6 interface. Moreover, a total of 305 disease-causing missense mutations of CaSR have been mapped to the structure in the active state, creating hotspot maps of five clinical endocrine disorders. Our results provide a structural framework for understanding the activation, allosteric modulation mechanism, and disease therapy for class C GPCRs.
External linksSci Adv / PubMed:34088669 / PubMed Central
MethodsEM (single particle)
Resolution3.2 - 7.2 Å
Structure data

30644

7dd5

EMDB-30644, PDB-7dd5:
Structure of Calcium-Sensing Receptor in complex with NPS-2143
Method: EM (single particle) / Resolution: 3.2 Å

30645

7dd6

EMDB-30645, PDB-7dd6:
Structure of Ca2+/L-Trp-bonnd Calcium-Sensing Receptor in active state
Method: EM (single particle) / Resolution: 3.2 Å

EMDB-30646:
Structure of Calcium-Sensing Receptor in an inactive state
Method: EM (single particle) / Resolution: 7.2 Å

30647

7dd7

EMDB-30647, PDB-7dd7:
Structure of Calcium-Sensing Receptor in complex with Evocalcet
Method: EM (single particle) / Resolution: 3.2 Å

Chemicals

ChemComp-CL:
Unknown entry / Chloride

ChemComp-CA:
Unknown entry

ChemComp-NAG:
2-acetamido-2-deoxy-beta-D-glucopyranose / N-Acetylglucosamine

ChemComp-TRP:
TRYPTOPHAN / Tryptophan

ChemComp-YP1:
2-chloro-6-[(2R)-2-hydroxy-3-{[2-methyl-1-(naphthalen-2-yl)propan-2-yl]amino}propoxy]benzonitrile / antagonist, hormone*YM / NPS-2143

ChemComp-HOH:
WATER / Water

ChemComp-H43:
2-[4-[(3S)-3-[[(1R)-1-naphthalen-1-ylethyl]amino]pyrrolidin-1-yl]phenyl]ethanoic acid / agonist*YM / Evocalcet

Source
  • gallus gallus (chicken)
KeywordsMEMBRANE PROTEIN / Calcium-Sensing Receptor / CaSR / NPS-2143 / active state / Evocalcet

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