Target type: biologicalprocess
The directed movement of adenosine, adenine riboside, into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. [GOC:mah]
Adenosine transport is a fundamental process in cellular physiology, involving the movement of adenosine across cell membranes. Adenosine, a purine nucleoside, plays a crucial role in various biological processes, including neurotransmission, inflammation, and energy metabolism. The transport of adenosine across cell membranes is mediated by a family of membrane-bound proteins known as nucleoside transporters (NTs). These transporters are responsible for the uptake and efflux of adenosine and other nucleosides, contributing to the regulation of adenosine levels both intracellularly and extracellularly.
There are two main types of adenosine transporters: equilibrative nucleoside transporters (ENTs) and concentrative nucleoside transporters (CNTs). ENTs facilitate the bidirectional transport of adenosine across the membrane, driven by the concentration gradient. They do not require energy and are responsible for the passive diffusion of adenosine. CNTs, on the other hand, are active transporters that utilize energy from the hydrolysis of ATP to transport adenosine against its concentration gradient. This allows for the accumulation of adenosine inside cells.
ENTs are further subdivided into two subtypes: ENT1 and ENT2. ENT1 is the most abundant nucleoside transporter in many tissues, including the brain, heart, and skeletal muscle. It exhibits a high affinity for adenosine and plays a significant role in the regulation of extracellular adenosine levels. ENT2 is less abundant and exhibits lower affinity for adenosine compared to ENT1. It is primarily involved in the uptake of adenosine in the liver and kidney.
CNTs are also classified into subtypes: CNT1, CNT2, and CNT3. CNT1 is the primary transporter responsible for the uptake of adenosine in the intestine and kidney. It exhibits a high affinity for adenosine and plays a crucial role in the absorption of adenosine from the diet. CNT2 is expressed in the brain, heart, and skeletal muscle. It transports adenosine with a lower affinity compared to CNT1. CNT3 is primarily localized to the liver and kidney and exhibits a low affinity for adenosine.
The transport of adenosine across cell membranes is a complex process regulated by various factors, including the concentration of adenosine, the expression levels of nucleoside transporters, and the presence of inhibitors. Dysregulation of adenosine transport can lead to various pathological conditions, such as neurodegenerative diseases, cardiovascular diseases, and inflammatory disorders. Therefore, understanding the mechanisms of adenosine transport is crucial for developing novel therapeutic strategies targeting these diseases.
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Protein | Definition | Taxonomy |
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Equilibrative nucleoside transporter 1 | An equilibrative nucleoside transporter 1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q99808] | Homo sapiens (human) |
Equilibrative nucleoside transporter 4 | An equilibrative nucleoside transporter 4 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q7RTT9] | Homo sapiens (human) |
Equilibrative nucleoside transporter 2 | An equilibrative nucleoside transporter 2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q14542] | Homo sapiens (human) |
Sodium/nucleoside cotransporter 2 | A sodium/nucleoside cotransporter 2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:O43868] | Homo sapiens (human) |
Compound | Definition | Classes | Roles |
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histamine | aralkylamino compound; imidazoles | human metabolite; mouse metabolite; neurotransmitter | |
dilazep | dilazep : A member of the class of diazepanes that is 1,4-diazepane substituted by 3-[(3,4,5-trimethoxybenzoyl)oxy]propyl groups at positions 1 and 4. It is a potent adenosine uptake inhibitor that exhibits antiplatelet, antianginal and vasodilator properties. Dilazep: Coronary vasodilator with some antiarrhythmic activity. | benzoate ester; diazepane; diester; methoxybenzenes | cardioprotective agent; platelet aggregation inhibitor; vasodilator agent |
dipyridamole | dipyridamole : A pyrimidopyrimidine that is 2,2',2'',2'''-(pyrimido[5,4-d]pyrimidine-2,6-diyldinitrilo)tetraethanol substituted by piperidin-1-yl groups at positions 4 and 8 respectively. A vasodilator agent, it inhibits the formation of blood clots. Dipyridamole: A phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells. Dipyridamole also potentiates the antiaggregating action of prostacyclin. (From AMA Drug Evaluations Annual, 1994, p752) | piperidines; pyrimidopyrimidine; tertiary amino compound; tetrol | adenosine phosphodiesterase inhibitor; EC 3.5.4.4 (adenosine deaminase) inhibitor; platelet aggregation inhibitor; vasodilator agent |
lidoflazine | Lidoflazine: Coronary vasodilator with some antiarrhythmic action. | diarylmethane | |
floxuridine | floxuridine : A pyrimidine 2'-deoxyribonucleoside compound having 5-fluorouracil as the nucleobase; used to treat hepatic metastases of gastrointestinal adenocarcinomas and for palliation in malignant neoplasms of the liver and gastrointestinal tract. Floxuridine: An antineoplastic antimetabolite that is metabolized to fluorouracil when administered by rapid injection; when administered by slow, continuous, intra-arterial infusion, it is converted to floxuridine monophosphate. It has been used to treat hepatic metastases of gastrointestinal adenocarcinomas and for palliation in malignant neoplasms of the liver and gastrointestinal tract. | nucleoside analogue; organofluorine compound; pyrimidine 2'-deoxyribonucleoside | antimetabolite; antineoplastic agent; antiviral drug; radiosensitizing agent |
uridine | uridines | drug metabolite; fundamental metabolite; human metabolite | |
phlorhizin | aryl beta-D-glucoside; dihydrochalcones; monosaccharide derivative | antioxidant; plant metabolite | |
methylthioinosine | Methylthioinosine: 6-(Methylthio)-9-beta-D-ribofuranosylpurine. An analog of inosine with a methylthio group replacing the hydroxyl group in the 6-position. | purine ribonucleoside; thiopurine | |
hyaluronoglucosaminidase | kinetin riboside: preferentially induces apoptosis by modulating Bcl-2 family proteins and caspase-3 in cancer cells; structure in first source | purine nucleoside | |
gemcitabine | gemcitabine : A 2'-deoxycytidine having geminal fluoro substituents in the 2'-position. An inhibitor of ribonucleotide reductase, gemcitabine is used in the treatment of various carcinomas, particularly non-small cell lung cancer, pancreatic cancer, bladder cancer and breast cancer. | organofluorine compound; pyrimidine 2'-deoxyribonucleoside | antimetabolite; antineoplastic agent; antiviral drug; DNA synthesis inhibitor; EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor; environmental contaminant; immunosuppressive agent; photosensitizing agent; prodrug; radiosensitizing agent; xenobiotic |
draflazine | draflazine: a nucleoside transport inhibitor; has cardioprotective effect; draflazine is the (-)-enantiomer; R 88016 is the (+)-enantiomer | ||
adenosine | quinquefolan B: isolated from roots of Panax quinquefolium L.; RN not in Chemline 10/87; RN from Toxlit | adenosines; purines D-ribonucleoside | analgesic; anti-arrhythmia drug; fundamental metabolite; human metabolite; vasodilator agent |
4-nitrobenzylthioinosine | 4-nitrobenzylthioinosine: inhibitor of nucleoside transport; acts on ENT1 | purine nucleoside | |
n(6)-benzyladenosine | N(6)-benzyladenosine: RN given refers to parent cpd | ||
6-(4-nitrobenzylthio)guanosine | 6-(4-nitrobenzylthio)guanosine: inhibitor of nucleoside transport | ||
5-iodotubercidin | 7-iodotubercidin: inhibits Toxoplasma gondii adenosine kinase | organoiodine compound | |
n(6)-phenyladenosine | purine nucleoside | ||
tecadenoson | tecadenoson: an A1 adenosine receptor agonist | ||
2-hydroxy-5-nitrobenzylthioguanosine | |||
n(6)-cyclopentyladenosine | |||
7,8,3'-trihydroxyflavone | 7,8,3'-trihydroxyflavone: a potent small molecule TrkB receptor agonist that protects spiral ganglion neurons from degeneration both in vitro and in vivo | ||
6-benzylthioinosine | 6-benzylthioinosine: a subversive substrate of T gondii adenosine kinase; structure in first source |