Adenosine receptor A1

Function

Receptor for adenosine. The activity of this receptor is mediated by G proteins such as GNAI2 which inhibit adenylyl cyclase.

Classification

Family (Pfam)

PF00001 7tm_1

InterPro

Adeno_A1_rcpt, Adenosn_rcpt, GPCR_Rhodpsn, GPCR_Rhodpsn_7TM

Functional cluster

MFS & Drug-Efflux Transporters

Experimental structures · PDB · 5

• 5N2S X-ray 3.30A
• 5UEN X-ray 3.20A
• 6D9H EM 3.60A
• 7LD3 EM 3.20A
• 7LD4 EM 3.30A

A predicted model is available from AlphaFold.

Gene Ontology · 67

• GO:0032279 asymmetric synapse
• GO:0030673 axolemma
• GO:0016323 basolateral plasma membrane
• GO:0044305 calyx of Held
• GO:0030425 dendrite
• GO:0043197 dendritic spine
• GO:0140535 intracellular protein-containing complex
• GO:0043025 neuronal cell body
• GO:0005886 plasma membrane
• GO:0045211 postsynaptic membrane
• GO:0048786 presynaptic active zone
• GO:0042734 presynaptic membrane
• GO:0045202 synapse
• GO:0043195 terminal bouton
• GO:0001609 G protein-coupled adenosine receptor activity
• GO:0001664 G protein-coupled receptor binding
• GO:0031683 G-protein beta/gamma-subunit complex binding
• GO:0031072 heat shock protein binding
• GO:0032795 heterotrimeric G-protein binding
• GO:0046982 protein heterodimerization activity
• GO:0001883 purine nucleoside binding
• GO:0007193 adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway
• GO:0097190 apoptotic signaling pathway
• GO:0007267 cell-cell signaling
• GO:0050890 cognition
• GO:0050965 detection of temperature stimulus involved in sensory perception of pain
• GO:0007173 epidermal growth factor receptor signaling pathway
• GO:0060079 excitatory postsynaptic potential
• GO:0055089 fatty acid homeostasis
• GO:0035589 G protein-coupled purinergic nucleotide receptor signaling pathway
• GO:0007186 G protein-coupled receptor signaling pathway
• GO:0006954 inflammatory response
• GO:0016042 lipid catabolic process
• GO:0002674 negative regulation of acute inflammatory response
• GO:0043066 negative regulation of apoptotic process
• GO:0008285 negative regulation of cell population proliferation
• GO:0042323 negative regulation of circadian sleep/wake cycle, non-REM sleep
• GO:0014050 negative regulation of glutamate secretion
• GO:0046888 negative regulation of hormone secretion
• GO:0050995 negative regulation of lipid catabolic process
• GO:1900272 negative regulation of long-term synaptic potentiation
• GO:0032900 negative regulation of neurotrophin production
• GO:0032229 negative regulation of synaptic transmission, GABAergic
• GO:0051967 negative regulation of synaptic transmission, glutamatergic
• GO:0003085 negative regulation of systemic arterial blood pressure
• GO:0007399 nervous system development
• GO:0006909 phagocytosis
• GO:0035306 positive regulation of dephosphorylation
• GO:0045745 positive regulation of G protein-coupled receptor signaling pathway
• GO:0050996 positive regulation of lipid catabolic process
• GO:0043410 positive regulation of MAPK cascade
• GO:0032244 positive regulation of nucleoside transport
• GO:0002793 positive regulation of peptide secretion
• GO:0051897 positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction
• GO:0043268 positive regulation of potassium ion transport
• GO:0003084 positive regulation of systemic arterial blood pressure
• GO:0006612 protein targeting to membrane
• GO:0086004 regulation of cardiac muscle cell contraction
• GO:0099509 regulation of presynaptic cytosolic calcium ion concentration
• GO:0002087 regulation of respiratory gaseous exchange by nervous system process
• GO:0051930 regulation of sensory perception of pain
• GO:0001666 response to hypoxia
• GO:0014074 response to purine-containing compound
• GO:0007165 signal transduction
• GO:0001659 temperature homeostasis
• GO:0070328 triglyceride homeostasis
• GO:0042311 vasodilation

Drugs targeting this protein · 21

• CAFFEINE antagonist
• OXTRIPHYLLINE antagonist
• CAFFEINE CITRATE antagonist
• THEOPHYLLINE SODIUM GLYCINATE antagonist
• THEOPHYLLINE antagonist
• AMINOPHYLLINE antagonist
• SELODENOSON agonist
• CAPADENOSON partial agonist
• GS-9667 partial agonist
• AMP579 agonist
• TRABODENOSON agonist
• TECADENOSON agonist
• NAXIFYLLINE antagonist
• TONAPOFYLLINE antagonist
• FK453 antagonist
• ADENOSINE agonist
• ROLOFYLLINE antagonist
• BAY1067197 agonist
• GW493838 agonist
• T-62 modulator
• DERENOFYLLINE antagonist

Related proteins · sequence + function similarity

• Adenosine receptor A1 1.00
• Adenosine receptor A1 1.00
• Adenosine receptor A1 1.00
• Adenosine receptor A1 0.99
• Adenosine receptor A1 0.99
• Adenosine receptor A1 0.99
• Adenosine receptor A1 0.99
• Adenosine receptor A1 0.97
• Adenosine receptor A3 0.93
• Adenosine receptor A3 0.93
• Adenosine receptor A3 0.93
• Adenosine receptor A3 0.92

Co-cited proteins · studied together in the literature

• Putative peptidyl-tRNA hydrolase PTRHD1 1 shared papers
• Guanine nucleotide-binding protein G(i) subunit alpha-2 1 shared papers

Literature · 9 cited papers

• Structure of the adenosine-bound human adenosine A1 receptor-Gi complex. Nature · 2018
• Mutation in ADORA1 identified as likely cause of early-onset parkinsonism and cognitive dysfunction. Mov. Disord. · 2016
• The consensus coding sequences of human breast and colorectal cancers. Science · 2006
• The DNA sequence and biological annotation of human chromosome 1. Nature · 2006
• The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC). Genome Res. · 2004
• Complete sequencing and characterization of 21,243 full-length human cDNAs. Nat. Genet. · 2004
• Characterization of the human A1 adenosine receptor gene. Evidence for alternative splicing. J. Biol. Chem. · 1994
• Cloning and functional characterization of a human A1 adenosine receptor. Biochem. Biophys. Res. Commun. · 1992
• Molecular cloning and characterisation of a human brain A1 adenosine receptor cDNA. Brain Res. Mol. Brain Res. · 1992