아데노신A수용체3

Adenosine A3 receptor
아도라3
사용 가능한 구조물
PDB직교 검색: PDBe RCSB
식별자
별칭ADORA3, A3AR, AD026, bA552M11.5, 아데노신 A3 수용체
외부 IDOMIM: 600445 MGI: 104847 호몰로진: 550 GeneCard: ADORA3
직교체
종인간마우스
엔트레스

140

11542

앙상블

ENSG00000282608

ENSMUSG00000000562

유니프로트

P0DMS8

Q61618
Q3U4C5

RefSeq(mRNA)

NM_001302679
NM_000677
NM_001302678

NM_009631

RefSeq(단백질)

NP_000668
NP_001289607
NP_001289608

NP_033761

위치(UCSC)Chr 1: 111.5 – 111.5MbChr 3: 105.87 – 105.91Mb
PubMed 검색[3][4]
위키다타
인간 보기/편집마우스 보기/편집

아데노신A 수용체(Adenosine A3 수용체)는 아데노신 수용체라고도 하지만, 이를 인코딩하는 인간의 유전자를 나타내기도 한다.

함수

아데노신 A3 수용체는 G 단백질 결합 수용체로 Gi/Gq와 결합하며 다양한 세포내 신호 경로와 생리학적 기능에 관여한다. 심장 허혈 중에 지속적 심장 보호 기능을 매개하고, 중성미자 매개 조직 상해에서 중성미자 분해 억제와 관련이 있으며, 신경 보호 효과와 신경 퇴행 효과 모두에 관여했으며, 세포 증식과 세포 사망을[citation needed] 모두 중재할 수도 있다. 최근의 출판물은 아데노신 A3 수용체 길항제(SSR161421)가 기관지 천식(17,18)에서 치료 잠재력을 가질 수 있다는 것을 보여준다.

유전자

이 유전자에 대해 서로 다른 ISO 양식을 인코딩하는 다중 대본 변형이 발견되었다.[5]

치료적 함의

류머티스 관절염 치료를3 위해 아데노신A 수용체 작용제(CF-101)가 임상시험 중이다.[6] 마우스3 경색 모델에서 선택적 작용제 CP-532,903은 심근 허혈 및 레퍼시퓨전 손상으로부터 보호된다.[7]

선택적 리간즈

많은 선택적3 A 리간드를 이용할 수 있다.[8][9][10][11][12][13][14][15][16][17][18][19]

작용제/양성 알로스테릭 변조기

  • 2-(1-헥시닐)-N-메틸아데노신
  • CF-101(IB-MCA)
  • CF-102
  • 2-Cl-IB-MCA
  • CP-532,903
  • 이노신[20]
  • LUF 6000
  • MISS-3558
  • AST-004

길항자/부정합성 변조기

  • KF-267777
  • MISS-545
  • MISS-1191
  • MISS-1220
  • MISS-1334
  • MISS-1523
  • MISS-3777
  • MRE-3005-F20
  • MRE-3008-F20
  • PSB-11
  • OT-7999
  • VUF-5574
  • SSR161421[21][22]

역작용제

참조

  1. ^ a b c GRCh38: 앙상블 릴리스 89: ENSG00000282608 - 앙상블, 2017년 5월
  2. ^ a b c GRCm38: 앙상블 릴리스 89: ENSMUSG00000000562 - 앙상블, 2017년 5월
  3. ^ "Human PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
  4. ^ "Mouse PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
  5. ^ "Entrez Gene: ADORA3 adenosine A3 receptor".
  6. ^ Silverman MH, Strand V, Markovits D, Nahir M, Reitblat T, Molad Y, Rosner I, Rozenbaum M, Mader R, Adawi M, Caspi D, Tishler M, Langevitz P, Rubinow A, Friedman J, Green L, Tanay A, Ochaion A, Cohen S, Kerns WD, Cohn I, Fishman-Furman S, Farbstein M, Yehuda SB, Fishman P (January 2008). "Clinical evidence for utilization of the A3 adenosine receptor as a target to treat rheumatoid arthritis: data from a phase II clinical trial". J. Rheumatol. 35 (1): 41–8. PMID 18050382.
  7. ^ Wan TC, Ge ZD, Tampo A, Mio Y, Bienengraeber MW, Tracey WR, Gross GJ, Kwok WM, Auchampach JA (January 2008). "The A3 adenosine receptor agonist CP-532,903 protects against myocardial ischemia/reperfusion injury via the sarcolemmal ATP sensitive potassium channel". J. Pharmacol. Exp. Ther. 324 (1): 234–43. doi:10.1124/jpet.107.127480. PMC 2435594. PMID 17906066.
  8. ^ Jeong LS, Lee HW, Jacobson KA, Lee SK, Chun MW (2005). "Development of potent and selective human A3 adenosine receptor agonists". Nucleic Acids Symposium Series (2004). 49 (1): 31–2. doi:10.1093/nass/49.1.31. PMID 17150618.
  9. ^ Gao ZG, Jacobson KA (September 2007). "Emerging adenosine receptor agonists". Expert Opinion on Emerging Drugs. 12 (3): 479–92. doi:10.1517/14728214.12.3.479. PMID 17874974. S2CID 13777846.
  10. ^ Kim SK, Gao ZG, Jeong LS, Jacobson KA (December 2006). "Docking studies of agonists and antagonists suggest an activation pathway of the A3 adenosine receptor". Journal of Molecular Graphics & Modelling. 25 (4): 562–77. doi:10.1016/j.jmgm.2006.05.004. PMC 6262875. PMID 16793299.
  11. ^ Ge ZD, Peart JN, Kreckler LM, Wan TC, Jacobson MA, Gross GJ, Auchampach JA (December 2006). "Cl-IB-MECA Reduces Ischemia/Reperfusion Injury in Mice by Activating the A3 Adenosine Receptor". The Journal of Pharmacology and Experimental Therapeutics. 319 (3): 1200–10. doi:10.1124/jpet.106.111351. PMC 2430759. PMID 16985166.
  12. ^ Bevan N, Butchers PR, Cousins R, Coates J, Edgar EV, Morrison V, Sheehan MJ, Reeves J, Wilson DJ (June 2007). "Pharmacological characterisation and inhibitory effects of (2R,3R,4S,5R)-2-(6-amino-2-{[(1S)-2-hydroxy-1-(phenylmethyl)ethyl]amino}-9H-purin-9-yl)-5-(2-ethyl-2H-tetrazol-5-yl)tetrahydro-3,4-furandiol, a novel ligand that demonstrates both adenosine A(2A) receptor agonist and adenosine A(3) receptor antagonist activity". European Journal of Pharmacology. 564 (1–3): 219–25. doi:10.1016/j.ejphar.2007.01.094. PMID 17382926.
  13. ^ Priego EM, Pérez-Pérez MJ, von Frijtag Drabbe Kuenzel JK, de Vries H, Ijzerman AP, Camarasa MJ, Martín-Santamaría S (January 2008). "Selective human adenosine A3 antagonists based on pyrido[2,1-f]purine-2,4-diones: novel features of hA3 antagonist binding". ChemMedChem. 3 (1): 111–9. doi:10.1002/cmdc.200700173. hdl:10261/82277. PMID 18000937. S2CID 7128294.
  14. ^ Jeong LS, Lee HW, Kim HO, Tosh DK, Pal S, Choi WJ, Gao ZG, Patel AR, Williams W, Jacobson KA, Kim HD (March 2008). "Structure-activity relationships of 2-chloro-N6-substituted-4'-thioadenosine-5'-N,N-dialkyluronamides as human A3 adenosine receptor antagonists". Bioorganic & Medicinal Chemistry Letters. 18 (5): 1612–6. doi:10.1016/j.bmcl.2008.01.070. PMID 18255292.
  15. ^ Cordeaux Y, Briddon SJ, Alexander SP, Kellam B, Hill SJ (March 2008). "Agonist-occupied A3 adenosine receptors exist within heterogeneous complexes in membrane microdomains of individual living cells". The FASEB Journal. 22 (3): 850–60. doi:10.1096/fj.07-8180com. PMID 17959910. S2CID 10705640.
  16. ^ Gao ZG, Jacobson KA (April 2008). "Translocation of Arrestin Induced by Human A3 Adenosine Receptor Ligands in an Engineered Cell Line: Comparison with G Protein-dependent Pathways". Pharmacological Research. 57 (4): 303–11. doi:10.1016/j.phrs.2008.02.008. PMC 2409065. PMID 18424164.
  17. ^ Miwatashi S, Arikawa Y, Matsumoto T, Uga K, Kanzaki N, Imai YN, Ohkawa S (August 2008). "Synthesis and biological activities of 4-phenyl-5-pyridyl-1,3-thiazole derivatives as selective adenosine A3 antagonists". Chemical & Pharmaceutical Bulletin. 56 (8): 1126–37. doi:10.1248/cpb.56.1126. PMID 18670113.[데드링크]
  18. ^ Gao ZG, Ye K, Göblyös A, Ijzerman AP, Jacobson KA (2008). "Flexible modulation of agonist efficacy at the human A3 adenosine receptor by the imidazoquinoline allosteric enhancer LUF6000". BMC Pharmacology. 8: 20. doi:10.1186/1471-2210-8-20. PMC 2625337. PMID 19077268.
  19. ^ Bar-Yehuda S, Stemmer SM, Madi L, Castel D, Ochaion A, Cohen S, Barer F, Zabutti A, Perez-Liz G, Del Valle L, Fishman P (August 2008). "The A3 adenosine receptor agonist CF102 induces apoptosis of hepatocellular carcinoma via de-regulation of the Wnt and NF-kappaB signal transduction pathways". International Journal of Oncology. 33 (2): 287–95. doi:10.3892/ijo_00000008. PMID 18636149.
  20. ^ 샤오웨이 진, 레베카 K. 셰퍼드, 브라이언 R 덜링, 조엘 린덴. "이노신이 A3 아데노신 수용체에 결합해 마스트 세포 열화를 자극한다"
  21. ^ Mikus EG, Szeredi J, Boer K, Tímári G, Finet M, Aranyi P, Galzin AM (December 2012). "Evaluation of SSR161421, a novel orally active adenosine A(3) receptor antagonist on pharmacology models". Eur. J. Pharmacol. 699 (1–3): 172–179. doi:10.1016/j.ejphar.2012.11.049. PMID 23219796.
  22. ^ Mikus EG, Boér K, Timári G, Urbán-Szabó K, Kapui Z, Szeredi J, Gerber K, Szabó T, Bátori S, Finet M, Arányi P, Galzin AM (December 2012). "Interaction of SSR161421, a novel specific adenosine A(3) receptor antagonist with adenosine A(3) receptor agonists both in vitro and in vivo". Eur. J. Pharmacol. 699 (1–3): 62–66. doi:10.1016/j.ejphar.2012.11.046. PMID 23219789.

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