Enzyme-linked receptor

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An enzyme-linked receptor, also known as a catalytic receptor, is a transmembrane receptor, where the binding of an extracellular ligand causes enzymatic activity on the intracellular side.[1] Hence a catalytic receptor is an integral membrane protein possessing both enzymatic catalytic and receptor functions.[2]

They have two important domains, an extra-cellular ligand binding domain and an intracellular domain, which has a Catalytic function; and a transmembrane helix. The signaling molecule binds to the receptor outside of the cell and causes a conformational change on the Catalytic function located on the receptor inside of the cell.

Examples of the enzymatic activity include:

Types[edit]

The following is a list of the five major families of catalytic receptors:

Family Member Gene Catalytic activity Endogenous Ligands Synthetic Ligands
Erb[4] ErbB1 (epidermal growth factor receptor) EGFR tyrosine kinase EC 2.7.10.1 Epidermal growth factor, amphiregulin, betacellulin, epigen, epiregulin, HB-EGF, TGFa GW583340, gefitinib, erlotinib, tyrphostins AG879 and AG1478
ErbB2 ERBB2 "
ErbB3 ERBB3 " NRG-1, NRG-2 GW583340, gefitinib, erlotinib, tyrphostins AG879 and AG1478
ErbB4 ERBB4 " Betacellulin, epiregulin, HB-EGF, NRG-1, NRG-2, NRG-3, NRG-4 GW583340, gefitinib, erlotinib, tyrphostins AG879 and AG1478
GDNF (glial cell-derived neurotrophic factor)[5] GFRa1 GFRa1 " GDNF > neurturin > artemin
GFRa2 GFRa2 " Neurturin > GDNF
GFRa3 GFRa3 " Artemin
GFRa4 GFRa4 " Persephin
NPR (natriuretic peptide receptor)[6] NPR1 NPR1 guanylyl cyclase EC 4.6.1.2 Atrial natriuretic peptide
NPR2 NPR2 " C-type natriuretic peptide
NPR3 NPR3 " Atrial natriuretic peptide
NPR4 NPR4 " Uroguanylin
trk neurotrophin receptor[7] TrkA NTRK1 tyrosine kinase EC 2.7.10.1 Nerve growth factor > NT-3 GW441756, tyrphostin AG879
TrkB NTRK2 " Brain-derived neurotrophic factor, NT-4/NT-5 > NT-3
TrkC NTRK3 " NT-3
p75 NGFR " NGF, BDNF, NT3, NT4/5
Toll-like[8] TLR1 TLR1 "
TLR2 TLR2 " Peptidoglycan
TLR3 TLR3 " polyIC, polyinosine-polycytosine
TLR4 TLR4 " LPS, lipopolysaccharide derived from Gram-negative bacteria
TLR5 TLR5 " Flagellin
TLR6 TLR6 "
TLR7 TLR7 " resiquimod, imiquimod
TLR8 TLR8 "
TLR9 TLR9 " CpG, DNA enriched in cytosine:guanosine pairs
TLR10 TLR10 "

References[edit]

  1. ^ Ronald W. Dudek (1 November 2006). High-yield cell and molecular biology. Lippincott Williams & Wilkins. pp. 19–. ISBN 978-0-7817-6887-0. Retrieved 16 December 2010. 
  2. ^ Alexander SP, Mathie A, Peters JA (February 2007). "Catalytic Receptors". Br. J. Pharmacol. 150 Suppl 1 (S1): S122–7. doi:10.1038/sj.bjp.0707205. PMC 2013840. PMID 17279064. 
  3. ^ lecture10
  4. ^ Alexander SP, Mathie A, Peters JA (February 2007). "Catalytic receptors: ErbB family". Br. J. Pharmacol. 150 Suppl 1: S146. doi:10.1038/sj.bjp.0706476. 
  5. ^ Alexander SP, Mathie A, Peters JA (February 2007). "Catalytic receptors: GDNF family". Br. J. Pharmacol. 150 Suppl 1: S147. doi:10.1038/sj.bjp.0706477. 
  6. ^ Alexander SP, Mathie A, Peters JA (February 2007). "Catalytic receptors: Natriuretic peptide family". Br. J. Pharmacol. 150 Suppl 1: S148. doi:10.1038/sj.bjp.0706478. 
  7. ^ Alexander SP, Mathie A, Peters JA (February 2007). "Catalytic receptors: Neurotrophin family". Br. J. Pharmacol. 150 Suppl 1: S149. doi:10.1038/sj.bjp.0706479. 
  8. ^ Alexander SP, Mathie A, Peters JA (February 2007). "Catalytic receptors: Toll-like receptor family". Br. J. Pharmacol. 150 Suppl 1: S150. doi:10.1038/sj.bjp.0706480. 

External links[edit]