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histatin 1   Click here for help

GtoPdb Ligand ID: 14556

Comment: Histatin 1 is an endogenous cationic and histidine-rich secreted peptide. It binds to the σ2 receptor (TMEM97) on epithelial cells [8-9], and to the VEGFR2 (KDR) on endothelial cells [4]. Histatin 1 is the primary wound healing agent in saliva. It acts as a potent promoter of cell migration and angiogenesis [11], two important biological processes that contribute to the rapid rate of wound healing in the oral mucosa.
Preclinical evidence suggests that histatin 1, or more likely metabolically stablised derivatives, offer a novel therapeutic mechanism in non-oral tissues for wound healing properties [1-3,5-6,13], or for potential osteogenic activity [7,10,12,14].
Species: Human
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Selectivity at catalytic receptors
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Target Sp. Type Action Value Parameter Concentration range (M) Reference
kinase insert domain receptor Ligand is endogenous in the given species Hs Agonist Agonist - - - 4
[4]
Selectivity at other protein targets
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Target Sp. Type Action Value Parameter Concentration range (M) Reference
σ2 Ligand is endogenous in the given species Hs Agonist Agonist 6.6 pKi - 9
pKi 6.6 (Ki 2.39x10-7 M) [9]
Description: Determined in a radioligand binding assay, using membranes from HEK239T overexpressing TMEM97, and [3H]DOTG as tracer