Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
3
pubmed:dateCreated
2008-9-10
pubmed:abstractText
The human extracellular Ca(2+)-sensing receptor (CaR) plays a key role in the regulation of serum calcium and parathyroid hormone. This large dimeric receptor consists of domains with topologically distinctive orthosteric and allosteric sites. Positive allosteric modulators of the CaR, which increase CaR activation and thereby decrease secretion of parathyroid hormone, are potential for the treatment of primary and secondary hyperparathyroidism. Conversely, negative allosteric modulators of the CaR, which decrease the receptor activation and thereby stimulate endogenous parathyroid hormone secretion, are potential for the treatment of osteoporosis and autosomal dominant hypocalcemia. Significant progress has been made in recent years in screening for allosteric modulators selectively targeting the CaR and identification of receptor residues important for allosteric modulation.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Sep
pubmed:issn
1871-5303
pubmed:author
pubmed:issnType
Print
pubmed:volume
8
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
192-7
pubmed:meshHeading
pubmed:year
2008
pubmed:articleTitle
Allosteric modulators of the human calcium-sensing receptor: structures, sites of action, and therapeutic potentials.
pubmed:affiliation
Molecular Signaling Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, 9000 Rockville Pike, Bethesda, MD 20892, USA. jianxinh@niddk.nih.gov
pubmed:publicationType
Journal Article, Review, Research Support, N.I.H., Intramural