Two threonine residues and two serine residues in the second and third intracellular loops are both involved in histamine H1 receptor downregulation.

Article Details

Citation

Horio S, Kato T, Ogawa M, Fujimoto K, Fukui H

Two threonine residues and two serine residues in the second and third intracellular loops are both involved in histamine H1 receptor downregulation.

FEBS Lett. 2004 Aug 27;573(1-3):226-30.

PubMed ID
15328002 [ View in PubMed
]
Abstract

Human histamine H1 receptor (H1R) contains five possible phosphorylation residues (Thr140, Thr142, Ser396, Ser398 and Thr478) and the substitution of all these five residues to alanine completely impairs agonist-induced receptor downregulation. In the present study, to determine which residue(s) are responsible for receptor downregulation, we used mutant H1Rs in which single or multiple residues were substituted with alanine. The results suggested that two groups, i.e., residues Thr140 and Thr142, and residues Ser396 and Ser398, independently contributed to H1R downregulation. Thr140 and Ser398 mainly contributed to downregulation, and Thr142 or Ser396 had a slight inhibitory effect on Thr140- or Ser398-mediated process, respectively.

DrugBank Data that Cites this Article

Polypeptides
NameUniProt ID
Histamine H1 receptorP35367Details