Target General Infomation
Target ID
T91661
Former ID
TTDR00529
Target Name
Adenosine kinase
Gene Name
ADK
Synonyms
AK; Adenosine 5'-phosphotransferase; ADK
Target Type
Clinical Trial
Disease Convulsions [ICD9: 780.3; ICD10: R56.0]
Epileptic seizures [ICD9: 345.9, 780.3; ICD10: G40, P90, R56]
Epilepsy [ICD10: G40]
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89]
Function
Atp dependent phosphorylation of adenosine and other related nucleoside analogs to monophosphate derivatives. Serves as a potential regulator of concentrations of extracellular adenosine and intracellular adenine nucleotides.
BioChemical Class
Kinase
Target Validation
T91661
UniProt ID
EC Number
EC 2.7.1.20
Sequence
MAAAEEEPKPKKLKVEAPQALRENILFGMGNPLLDISAVVDKDFLDKYSLKPNDQILAED
KHKELFDELVKKFKVEYHAGGSTQNSIKVAQWMIQQPHKAATFFGCIGIDKFGEILKRKA
AEAHVDAHYYEQNEQPTGTCAACITGDNRSLIANLAAANCYKKEKHLDLEKNWMLVEKAR
VCYIAGFFLTVSPESVLKVAHHASENNRIFTLNLSAPFISQFYKESLMKVMPYVDILFGN
ETEAATFAREQGFETKDIKEIAKKTQALPKMNSKRQRIVIFTQGRDDTIMATESEVTAFA
VLDQDQKEIIDTNGAGDAFVGGFLSQLVSDKPLTECIRAGHYAASIIIRRTGCTFPEKPD
FH
Drugs and Mode of Action
Drug(s) GP-3269 Drug Info Phase 1 Convulsions [527887]
A-134974 Drug Info Terminated Epilepsy [468194], [546592]
ABT-702 Drug Info Terminated Pain [468195], [547299]
GP-683 Drug Info Terminated Pain [546153]
GP515 Drug Info Terminated Discovery agent [545930]
Inhibitor 5'-iodotubercidin Drug Info [536049]
5-iodo,5'-deoxytubercidin Drug Info [528569]
6-Benzylthioinosine Drug Info [530903]
A-134974 Drug Info [525955]
ABT-702 Drug Info [532399]
GP-3269 Drug Info [527887]
GP-683 Drug Info [534462]
GP515 Drug Info [535091]
Iodotubercidin Drug Info [531635]
MB-03966 Drug Info [544076]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
BioCyc Pathway Superpathway of purine nucleotide salvage
Adenine and adenosine salvage II
KEGG Pathway Purine metabolism
Metabolic pathways
Reactome Purine salvage
WikiPathways Metabolism of nucleotides
References
Ref 468194(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5130).
Ref 468195(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5131).
Ref 527887Adenosine kinase inhibitors. 6. Synthesis, water solubility, and antinociceptive activity of 5-phenyl-7-(5-deoxy-beta-D-ribofuranosyl)pyrrolo[2,3-d]pyrimidines substituted at C4 with glycinamides andrelated compounds. J Med Chem. 2005 Dec 1;48(24):7808-20.
Ref 545930Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005394)
Ref 546153Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006618)
Ref 546592Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009094)
Ref 547299Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014976)
Ref 525955Effects of A-134974, a novel adenosine kinase inhibitor, on carrageenan-induced inflammatory hyperalgesia and locomotor activity in rats: evaluation of the sites of action. J Pharmacol Exp Ther. 2001Feb;296(2):501-9.
Ref 527887Adenosine kinase inhibitors. 6. Synthesis, water solubility, and antinociceptive activity of 5-phenyl-7-(5-deoxy-beta-D-ribofuranosyl)pyrrolo[2,3-d]pyrimidines substituted at C4 with glycinamides andrelated compounds. J Med Chem. 2005 Dec 1;48(24):7808-20.
Ref 528569J Med Chem. 2006 Nov 16;49(23):6726-31.Crystal structures of human adenosine kinase inhibitor complexes reveal two distinct binding modes.
Ref 530903Bioorg Med Chem. 2010 May 15;18(10):3403-12. Epub 2010 Apr 8.Structure-activity relationships of carbocyclic 6-benzylthioinosine analogues as subversive substrates of Toxoplasma gondii adenosine kinase.
Ref 531635Therapeutic target database update 2012: a resource for facilitating target-oriented drug discovery. Nucleic Acids Res. 2012 Jan;40(Database issue):D1128-36.
Ref 532399ABT-702, an adenosine kinase inhibitor, attenuates inflammation in diabetic retinopathy. Life Sci. 2013 Jul 30;93(2-3):78-88.
Ref 534462The effect of GP683, an adenosine kinase inhibitor, on the desflurane anesthetic requirement in dogs. Anesth Analg. 1997 Sep;85(3):675-80.
Ref 535091Adenosine kinase inhibitor GP515 improves experimental colitis in mice. J Pharmacol Exp Ther. 2001 Jan;296(1):99-105.
Ref 536049Inhibition of adenosine kinase attenuates interleukin-1- and lipopolysaccharide-induced alterations in articular cartilage metabolism. Osteoarthritis Cartilage. 2005 Mar;13(3):250-7.
Ref 544076Engineered Adenosine-Releasing Cells for Epilepsy Therapy: Human Mesenchymal Stem Cells and Human Embryonic Stem Cells. Neurotherapeutics. 2009 April; 6(2): 278-283.

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