Пређи на садржај

Adenozinski A3 receptor — разлика између измена

С Википедије, слободне енциклопедије
Интерактиван преглед историје
← Старија изменаНовија измена →
Садржај обрисан Садржај додат
ВизуелноВикитекст
Ред 12: Ред 12:
== Terapeutske implikacije ==
== Terapeutske implikacije ==
Agonist adenozinskog A<sub>3</sub> receptora (-{CF}--101) je u kliničkim ispitivanjima za lečenje [[Reumatoidni artritis|reumatoidnog artritisa]].<ref name="pmid18050382">{{cite journal | author = 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 | title = Clinical evidence for utilization of the A<sub>3</sub> adenosine receptor as a target to treat rheumatoid arthritis: data from a phase II clinical trial | journal = J. Rheumatol. | volume = 35 | issue = 1 | pages = 41–8 | year = 2008 | month = January | pmid = 18050382 | doi = | url = http://www.jrheum.org/content/35/1/41.abstract | issn = }}</ref>
Agonist adenozinskog A<sub>3</sub> receptora (-{CF}--101) je u kliničkim ispitivanjima za lečenje [[Reumatoidni artritis|reumatoidnog artritisa]].<ref name="pmid18050382">{{cite journal | author = 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 | title = Clinical evidence for utilization of the A<sub>3</sub> adenosine receptor as a target to treat rheumatoid arthritis: data from a phase II clinical trial | journal = J. Rheumatol. | volume = 35 | issue = 1 | pages = 41–8 | year = 2008 | month = January | pmid = 18050382 | doi = | url = http://www.jrheum.org/content/35/1/41.abstract | issn = }}</ref>

==Selektivni ligandi==
Brojni selektivni A<sub>3</sub> ligandi su dostupni.<ref name="pmid16793299">{{cite journal | author = Kim SK, Gao ZG, Jeong LS, Jacobson KA | title = Docking studies of agonists and antagonists suggest an activation pathway of the A3 adenosine receptor | journal = Journal of Molecular Graphics & Modelling | volume = 25 | issue = 4 | pages = 562–77 | year = 2006 | month = December | pmid = 16793299 | doi = 10.1016/j.jmgm.2006.05.004 | url = | issn = }}</ref><ref name="pmid16985166">{{cite journal | author = Ge ZD, Peart JN, Kreckler LM, Wan TC, Jacobson MA, Gross GJ, Auchampach JA | title = Cl-IB-MECA [2-chloro-N6-(3-iodobenzyl)adenosine-5'-N-methylcarboxamide] reduces ischemia/reperfusion injury in mice by activating the A3 adenosine receptor | journal = The Journal of Pharmacology and Experimental Therapeutics | volume = 319 | issue = 3 | pages = 1200–10 | year = 2006 | month = December | pmid = 16985166 | pmc = 2430759 | doi = 10.1124/jpet.106.111351 | url = | issn = }}</ref><ref name="pmid17150618">{{cite journal | author = Jeong LS, Lee HW, Jacobson KA, Lee SK, Chun MW | title = Development of potent and selective human A3 adenosine receptor agonists | journal = Nucleic Acids Symposium Series (2004) | volume = 49| issue = 49 | pages = 31–2 | year = 2005 | pmid = 17150618 | doi = 10.1093/nass/49.1.31 | url = | issn = }}</ref><ref name="pmid17382926">{{cite journal | author = Bevan N, Butchers PR, Cousins R, Coates J, Edgar EV, Morrison V, Sheehan MJ, Reeves J, Wilson DJ | title = 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 | journal = European Journal of Pharmacology | volume = 564 | issue = 1-3 | pages = 219–25 | year = 2007 | month = June | pmid = 17382926 | doi = 10.1016/j.ejphar.2007.01.094 | url = | issn = }}</ref><ref name="pmid17874974">{{cite journal | author = Gao ZG, Jacobson KA | title = Emerging adenosine receptor agonists | journal = Expert Opinion on Emerging Drugs | volume = 12 | issue = 3 | pages = 479–92 | year = 2007 | month = September | pmid = 17874974 | doi = 10.1517/14728214.12.3.479 | url = | issn = }}</ref><ref name="pmid17906066">{{cite journal | author = Wan TC, Ge ZD, Tampo A, Mio Y, Bienengraeber MW, Tracey WR, Gross GJ, Kwok WM, Auchampach JA | title = The A<sub>3</sub> adenosine receptor agonist CP-532,903 [N6-(2,5-dichlorobenzyl)-3'-aminoadenosine-5'-N-methylcarboxamide] protects against myocardial ischemia/reperfusion injury via the sarcolemmal ATP-sensitive potassium channel | journal = J. Pharmacol. Exp. Ther. | volume = 324 | issue = 1 | pages = 234–43 | year = 2008 | month = January | pmid = 17906066 | pmc = 2435594 | doi = 10.1124/jpet.107.127480 | url = | issn = }}</ref><ref name="pmid17959910">{{cite journal | author = Cordeaux Y, Briddon SJ, Alexander SP, Kellam B, Hill SJ | title = Agonist-occupied A3 adenosine receptors exist within heterogeneous complexes in membrane microdomains of individual living cells | journal = The FASEB Journal : Official Publication of the Federation of American Societies for Experimental Biology | volume = 22 | issue = 3 | pages = 850–60 | year = 2008 | month = March | pmid = 17959910 | doi = 10.1096/fj.07-8180com | url = | issn = }}</ref><ref name="pmid18000937">{{cite journal | author = Priego EM, Pérez-Pérez MJ, von Frijtag Drabbe Kuenzel JK, de Vries H, Ijzerman AP, Camarasa MJ, Martín-Santamaría S | title = Selective human adenosine A3 antagonists based on pyrido[2,1-f]purine-2,4-diones: novel features of hA3 antagonist binding | journal = ChemMedChem | volume = 3 | issue = 1 | pages = 111–9 | year = 2008 | month = January | pmid = 18000937 | doi = 10.1002/cmdc.200700173 | url = | issn = }}</ref><ref name="pmid18255292">{{cite journal | author = Jeong LS, Lee HW, Kim HO, Tosh DK, Pal S, Choi WJ, Gao ZG, Patel AR, Williams W, Jacobson KA, Kim HD | title = Structure-activity relationships of 2-chloro-N6-substituted-4'-thioadenosine-5'-N,N-dialkyluronamides as human A3 adenosine receptor antagonists | journal = Bioorganic & Medicinal Chemistry Letters | volume = 18 | issue = 5 | pages = 1612–6 | year = 2008 | month = March | pmid = 18255292 | doi = 10.1016/j.bmcl.2008.01.070 | url = | issn = }}</ref><ref name="pmid18424164">{{cite journal | author = Gao ZG, Jacobson KA | title = Translocation of arrestin induced by human A(3) adenosine receptor ligands in an engineered cell line: comparison with G protein-dependent pathways | journal = Pharmacological Research : the Official Journal of the Italian Pharmacological Society | volume = 57 | issue = 4 | pages = 303–11 | year = 2008 | month = April | pmid = 18424164 | pmc = 2409065 | doi = 10.1016/j.phrs.2008.02.008 | url = | issn = }}</ref><ref name="pmid18636149">{{cite journal | author = 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 | title = The A3 adenosine receptor agonist CF102 induces apoptosis of hepatocellular carcinoma via de-regulation of the Wnt and NF-kappaB signal transduction pathways | journal = International Journal of Oncology | volume = 33 | issue = 2 | pages = 287–95 | year = 2008 | month = August | pmid = 18636149 | doi = | url = http://www.spandidos-publications.com/ijo/article.jsp?article_id=ijo_33_2_287 | issn = }}</ref><ref name="pmid18670113">{{cite journal | author = Miwatashi S, Arikawa Y, Matsumoto T, Uga K, Kanzaki N, Imai YN, Ohkawa S | title = Synthesis and biological activities of 4-phenyl-5-pyridyl-1,3-thiazole derivatives as selective adenosine A3 antagonists | journal = Chemical & Pharmaceutical Bulletin | volume = 56 | issue = 8 | pages = 1126–37 | year = 2008 | month = August | pmid = 18670113 | doi = 10.1248/cpb.56.1126| url = http://joi.jlc.jst.go.jp/JST.JSTAGE/cpb/56.1126?from=PubMed | issn = }}{{dead link|date=May 2009}}</ref><ref name="pmid19077268">{{cite journal | author = Gao ZG, Ye K, Göblyös A, Ijzerman AP, Jacobson KA | title = Flexible modulation of agonist efficacy at the human A3 adenosine receptor by the imidazoquinoline allosteric enhancer LUF6000 | journal = BMC Pharmacology | volume = 8 | issue = | page = 20 | year = 2008 | pmid = 19077268 | pmc = 2625337 | doi = 10.1186/1471-2210-8-20 | url = | issn = }}</ref>
}}


== Literatura ==
== Literatura ==

Верзија на датум 30. јун 2011. у 04:35

Adenozinski A3 receptor
Identifikatori
Simboli ADORA3; A3AR; AD026; RP11-552M11.7; bA552M11.5
Vanjski ID OMIM: 600445 MGI: 104847 HomoloGene: 550 IUPHAR: A3 GeneCards: ADORA3 Gene
Pregled RNK izražavanja
podaci
Ortolozi
Vrsta Čovek Miš
Entrez 140 11542
Ensembl ENSG00000121933 ENSMUSG00000000562
UniProt P33765 Q3U4C5
RefSeq (mRNA) NM_000677 NM_009631
RefSeq (protein) NP_000668 NP_033761
Lokacija (UCSC) Chr 1:
111.83 - 111.91 Mb		 Chr 3:
106.03 - 106.04 Mb
PubMed pretraga [1] [2]

Adenozinski A3 receptor (ADORA3) je adenozinski receptor. On je kodiran humanim ADORA3 genom.

Funkcija

Adenozinski A3 receptori je G protein-spregnuti receptor koji učestvuje u mnogobrojnim ćelijskim signalnim putevima i fiziološkim funkcijama. On posreduje kontinuirane kardioprotektivne funkcije tokom srčane ishemije, i učestvuje u inhibiciji neutrofilne degranulacije kod neutrofilima-posredovane povrede tkiva. Smatra se da ima neurozaštitno ali i neurodegenerativno dejstvo.

Gen

Višestruke transkriptne varijante koje kodiraju različite izoforme su poznate za ovaj gen.[1]

Terapeutske implikacije

Agonist adenozinskog A3 receptora (CF-101) je u kliničkim ispitivanjima za lečenje reumatoidnog artritisa.[2]

Selektivni ligandi

Brojni selektivni A3 ligandi su dostupni.[3][4][5][6][7][8][9][10][11][12][13][14][15] }}

Literatura

  1. ^ „Entrez Gene: ADORA3 adenosine A3 receptor”. 
  2. ^ 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 (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.  Непознати параметар |month= игнорисан (помоћ)
  3. ^ Kim SK, Gao ZG, Jeong LS, Jacobson KA (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. PMID 16793299. doi:10.1016/j.jmgm.2006.05.004.  Непознати параметар |month= игнорисан (помоћ)
  4. ^ Ge ZD, Peart JN, Kreckler LM, Wan TC, Jacobson MA, Gross GJ, Auchampach JA (2006). „Cl-IB-MECA [2-chloro-N6-(3-iodobenzyl)adenosine-5'-N-methylcarboxamide] reduces ischemia/reperfusion injury in mice by activating the A3 adenosine receptor”. The Journal of Pharmacology and Experimental Therapeutics. 319 (3): 1200—10. PMC 2430759 Слободан приступ. PMID 16985166. doi:10.1124/jpet.106.111351.  Непознати параметар |month= игнорисан (помоћ)
  5. ^ 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 (49): 31—2. PMID 17150618. doi:10.1093/nass/49.1.31. 
  6. ^ Bevan N, Butchers PR, Cousins R, Coates J, Edgar EV, Morrison V, Sheehan MJ, Reeves J, Wilson DJ (2007). „Pharmacological characterisation and inhibitory effects of (2R,3R,4S,5R)-2-(6-amino-2[(1S)-2-hydroxy-1-(phenylmethyl)ethyl]amino9H-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. PMID 17382926. doi:10.1016/j.ejphar.2007.01.094.  Непознати параметар |month= игнорисан (помоћ)
  7. ^ Gao ZG, Jacobson KA (2007). „Emerging adenosine receptor agonists”. Expert Opinion on Emerging Drugs. 12 (3): 479—92. PMID 17874974. doi:10.1517/14728214.12.3.479.  Непознати параметар |month= игнорисан (помоћ)
  8. ^ Wan TC, Ge ZD, Tampo A, Mio Y, Bienengraeber MW, Tracey WR, Gross GJ, Kwok WM, Auchampach JA (2008). „The A3 adenosine receptor agonist CP-532,903 [N6-(2,5-dichlorobenzyl)-3'-aminoadenosine-5'-N-methylcarboxamide] protects against myocardial ischemia/reperfusion injury via the sarcolemmal ATP-sensitive potassium channel”. J. Pharmacol. Exp. Ther. 324 (1): 234—43. PMC 2435594 Слободан приступ. PMID 17906066. doi:10.1124/jpet.107.127480.  Непознати параметар |month= игнорисан (помоћ)
  9. ^ Cordeaux Y, Briddon SJ, Alexander SP, Kellam B, Hill SJ (2008). „Agonist-occupied A3 adenosine receptors exist within heterogeneous complexes in membrane microdomains of individual living cells”. The FASEB Journal : Official Publication of the Federation of American Societies for Experimental Biology. 22 (3): 850—60. PMID 17959910. doi:10.1096/fj.07-8180com.  Непознати параметар |month= игнорисан (помоћ)
  10. ^ Priego EM, Pérez-Pérez MJ, von Frijtag Drabbe Kuenzel JK, de Vries H, Ijzerman AP, Camarasa MJ, Martín-Santamaría S (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. PMID 18000937. doi:10.1002/cmdc.200700173.  Непознати параметар |month= игнорисан (помоћ)
  11. ^ Jeong LS, Lee HW, Kim HO, Tosh DK, Pal S, Choi WJ, Gao ZG, Patel AR, Williams W, Jacobson KA, Kim HD (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. PMID 18255292. doi:10.1016/j.bmcl.2008.01.070.  Непознати параметар |month= игнорисан (помоћ)
  12. ^ Gao ZG, Jacobson KA (2008). „Translocation of arrestin induced by human A(3) adenosine receptor ligands in an engineered cell line: comparison with G protein-dependent pathways”. Pharmacological Research : the Official Journal of the Italian Pharmacological Society. 57 (4): 303—11. PMC 2409065 Слободан приступ. PMID 18424164. doi:10.1016/j.phrs.2008.02.008.  Непознати параметар |month= игнорисан (помоћ)
  13. ^ 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 (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. PMID 18636149.  Непознати параметар |month= игнорисан (помоћ)
  14. ^ Miwatashi S, Arikawa Y, Matsumoto T, Uga K, Kanzaki N, Imai YN, Ohkawa S (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. PMID 18670113. doi:10.1248/cpb.56.1126.  Непознати параметар |month= игнорисан (помоћ)[мртва веза]
  15. ^ 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. PMC 2625337 Слободан приступ. PMID 19077268. doi:10.1186/1471-2210-8-20. 
Преузето из „https://sr.wikipedia.org/w/index.php?title=Adenozinski_A3_receptor&oldid=4509396”