베타-3 아드레날린 수용체

ADRB3
사용 가능한 구조
PDB	동원체 검색: PDBe RCSB
PDB ID 코드 목록
	2CDW
식별자
다른 이름	ADRB3, BETA3AR, adrenoceptor beta 3
외부 ID	OMIM: 109691 MGI: 87939 HomoloGene: 37250 GeneCards: ADRB3
유전자 위치 (인간)
염색체	8번 염색체
끝	37,966,599 bp
유전자 위치 (쥐)
염색체	8번 염색체 (쥐)
끝	27,250,616 bp
RNA 발현 패턴
	최상위 발현
	right ovary; ; left ovary; ; 고환; ; 왼자궁관; ; 태반; ; 방광; ; 쓸개; ; 생식샘; ; muscle layer of sigmoid colon; ; fundus;
	최상위 발현
	lactiferous gland; ; 백색지방조직; ; 갈색지방조직; ; tunica adventitia of aorta; ; subcutaneous adipose tissue; ; 늑간근; ; tunica media of zone of aorta; ; 기관; ; mesenteric lymph nodes; ; 배;
	추가 참조 발현 데이터
	; ;
	추가 참조 발현 데이터
유전자 온톨로지
분자 함수	beta-adrenergic receptor activity; G protein-coupled receptor activity; epinephrine binding; protein homodimerization activity; beta3-adrenergic receptor activity; norepinephrine binding; beta-3 adrenergic receptor binding; signal transducer activity; adrenergic receptor activity; 단백질 결합;
세포 성분	integral component of membrane; 세포막; receptor complex; 세포막; integral component of plasma membrane; 세포핵;
생물학적 과정	adenylate cyclase-activating G protein-coupled receptor signaling pathway; eating behavior; adenylate cyclase-modulating G protein-coupled receptor signaling pathway; response to antibiotic; negative regulation of multicellular organism growth; cell-cell signaling; G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger; 노화; 수용체 매개 세포내 섭취; generation of precursor metabolites and energy; activation of adenylate cyclase activity; 식사 유발성 열생산; norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressure; adenylate cyclase-activating adrenergic receptor signaling pathway; heat generation; brown fat cell differentiation; response to cold; energy reserve metabolic process; temperature homeostasis; desensitization of G protein-coupled receptor signaling pathway by arrestin; positive regulation of MAPK cascade; 신호전달; 탄수화물 대사; G protein-coupled receptor signaling pathway; positive regulation of cold-induced thermogenesis;
	출처: Amigo / QuickGO
동원체
	155
	11556
	ENSG00000188778
	ENSMUSG00000031489
	P13945
	P25962
	NM_000025
	NM_013462
	NP_000016
	NP_038490
	위키데이터
인간 보기/편집	쥐 보기/편집

베타-3 아드레날린 수용체 (β₃ 아드레날린 수용체)는 ADRB3으로도 알려져 있는데, 베타 아드레날린 수용체의 일종으로 이를 인코딩하는 인간 유전자를 지칭하기도 한다.^[5]

작용

β ₃ 수용체의 작용에는 다음이 포함된다.

지방 조직의 지방 분해 증진.^[6]
골격근에서의 열발생^[7]

주로 지방 조직에 위치하며 지방 분해 및 열 발생 조절에 관여한다. 일부 β ₃ 작용제는 항 스트레스 효과가 동물 실험에서 밝혀졌는데, 이는 중추 신경계 (CNS)에서도 역할을 한다는 점을 암시한다. β ₃ 수용체는 담낭, 방광 및 갈색 지방 조직에서 발견된다. 담낭 생리학에서 그들의 역할은 알려지지 않았지만 갈색 지방에서 지방 분해 및 열 발생에 역할을하는 것으로 생각된다. 방광에서는 방광의 이완과 배뇨 방지를 유발하는 것으로 알려져 있다.^[8]

작용 메커니즘

베타 아드레날린 수용체는 Gs 유형의 G 단백질의 작용을 통하여 에피네프린 또는 노르에피네프린에 의하여 유도되는 아데닐레이트 사이클라제의 활성화에 관련되어 있다.^[5]

리간드

작용제

Amibegron (SR-58611A)^[9]^[10]
BRL-37344^[11]
CL-316,243^[12]
L-742,791^[13]
L-796,568^[14]
LY-368,842
Mirabegron (YM-178),^[15] 일본, 미국, 영국, 캐나다, 중국 및 인도에서 과민성 방광 치료로 승인됨.
Nebivolol^[16] 선택적 베타 (1) 차단제 및 베타 (3) 작용제.
Ro40-2148
솔라베그론 (GW-427,353)^[17]
Vibegron (MK-4618)^[18]

길항제

L-748,328^[13]
L-748,337^[13]
SR 59230A는 원래 선택적 β ₃ 길항제로 생각되었는데,^[19] 그 후, α₁ 수용체의 길항제인 것으로 밝혀졌다.^[20]

상호 작용

베타-3 아드레날린 수용체는 Src와 상호 작용하는 것으로 밝혀졌다.^[21]

같이 보기

기타 아드레날린 수용체

각주

↑ ^가 ^나 ^다 GRCh38: Ensembl release 89: ENSG00000188778 - 앙상블, May 2017
↑ ^가 ^나 ^다 GRCm38: Ensembl release 89: ENSMUSG00000031489 - 앙상블, May 2017
↑ “Human PubMed Reference:”. 《National Center for Biotechnology Information, U.S. National Library of Medicine》.
↑ “Mouse PubMed Reference:”. 《National Center for Biotechnology Information, U.S. National Library of Medicine》.
↑ ^가 ^나 “Entrez Gene: ADRB3 adrenergic, beta-3-, receptor”.
↑ “Combined effects of oleoyl-estrone and a β₃-adrenergic agonist (CL316,243) on lipid stores of diet-induced overweight male Wistar rats”. 《Life Sciences》 77 (16): 2051–8. September 2005. doi:10.1016/j.lfs.2005.04.008. PMID 15935402.
↑ Rang, H. P. (2003). 《Pharmacology》. Edinburgh: Churchill Livingstone. ISBN 0-443-07145-4.
↑ “Recent Developments in the Design of Orally Bioavailable β3-Adrenergic Receptor Agonists”. 《Current Medicinal Chemistry》 13 (1): 25–37. 2006. doi:10.2174/092986706775198006. PMID 16457637.
↑ “Behavioral effects of the β₃ adrenoceptor agonist SR58611A: is it the putative prototype of a new class of antidepressant/anxiolytic drugs?”. 《European Journal of Pharmacology》 573 (1–3): 139–47. November 2007. doi:10.1016/j.ejphar.2007.06.048. PMID 17669397.
↑ “Confirmation of antidepressant potential of the selective β₃ adrenoceptor agonist amibegron in an animal model of depression”. 《Pharmacology Biochemistry and Behavior》 89 (4): 623–6. June 2008. doi:10.1016/j.pbb.2008.02.020. PMID 18358519.
↑ “BRL37344 stimulates GLUT4 translocation and glucose uptake in skeletal muscle via β2-adrenoceptors without causing classical receptor desensitization”. 《American Journal of Physiology. Regulatory, Integrative and Comparative Physiology》 316 (5): R666–R677. May 2019. doi:10.1152/ajpregu.00285.2018. PMID 30892909.
↑ “The effects of beta(3)-adrenoceptor agonist CL-316,243 on adiponectin, adiponectin receptors and tumor necrosis factor-alpha expressions in adipose tissues of obese diabetic KKAy mice”. 《European Journal of Pharmacology》 584 (1): 202–6. 2008. doi:10.1016/j.ejphar.2008.01.028. PMID 18304529.
↑ ^가 ^나 ^다 “Potent and selective human beta(3)-adrenergic receptor antagonists.”. 《The Journal of Pharmacology and Experimental Therapeutics》 290 (2): 649–55. Aug 1999. PMID 10411574.
↑ “Effect of a 28-d treatment with L-796568, a novel β₃-adrenergic receptor agonist, on energy expenditure and body composition in obese men”. 《The American Journal of Clinical Nutrition》 76 (4): 780–8. 2002. doi:10.1093/ajcn/76.4.780. PMID 12324291.
↑ “Mirabegron for the treatment of overactive bladder”. 《Drugs of Today》 48 (1): 25–32. 2012. doi:10.1358/dot.2012.48.1.1738056. PMID 22384458.
↑ “Nebivolol, a vasodilating selective beta(1)-blocker, is a beta(3)-adrenoceptor agonist in the nonfailing transplanted human heart”. 《J Am Coll Cardiol》 53 (17): 1532–8. doi:10.1016/j.jacc.2008.11.057. PMID 19389564.
↑ “GW427353 (solabegron), a novel, selective beta3-adrenergic receptor agonist, evokes bladder relaxation and increases micturition reflex threshold in the dog”. 《The Journal of Pharmacology and Experimental Therapeutics》 323 (1): 202–9. October 2007. doi:10.1124/jpet.107.125757. PMID 17626794.
↑ “Discovery of Vibegron: A Potent and Selective β3 Adrenergic Receptor Agonist for the Treatment of Overactive Bladder.”. 《Journal of Medicinal Chemistry》 59 (2): 609–23. January 2016. doi:10.1021/acs.jmedchem.5b01372. PMID 26709102.
↑ “Functional studies of the first selective β₃-adrenergic receptor antagonist SR 59230A in rat brown adipocytes”. 《Mol. Pharmacol.》 49 (1): 7–14. 1996. PMID 8569714.
↑ “Role of α1- and β3-adrenoceptors in the modulation by SR59230A of the effects of MDMA on body temperature in the mouse”. 《British Journal of Pharmacology》 158 (1): 259–66. April 2009. doi:10.1111/j.1476-5381.2009.00186.x. PMC 2795232. PMID 19422394.
↑ “Direct binding of activated c-Src to the beta 3-adrenergic receptor is required for MAP kinase activation”. 《J. Biol. Chem.》 275 (49): 38131–4. 2000. doi:10.1074/jbc.C000592200. PMID 11013230.

추가 자료

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Nahmias C, Blin N, Elalouf JM, Mattei MG, Strosberg AD, Emorine LJ (1991). “Molecular characterization of the mouse beta 3-adrenergic receptor: relationship with the atypical receptor of adipocytes”. 《EMBO J.》 10 (12): 3721–7. doi:10.1002/j.1460-2075.1991.tb04940.x. PMC 453106. PMID 1718744.
Emorine LJ, Marullo S, Briend-Sutren MM, Patey G, Tate K, Delavier-Klutchko C, Strosberg AD (1989). “Molecular characterization of the human beta 3-adrenergic receptor”. 《Science》 245 (4922): 1118–21. doi:10.1126/science.2570461. PMID 2570461.
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Dib A, Adélaïde J, Chaffanet M, Imbert A, Le Paslier D, Jacquemier J, Gaudray P, Theillet C, Birnbaum D, Pébusque MJ (1995). “Characterization of the region of the short arm of chromosome 8 amplified in breast carcinoma”. 《Oncogene》 10 (5): 995–1001. PMID 7898940.
Mahmoudian M (1994). “The complex of human Gs protein with the beta 3 adrenergic receptor: a computer-aided molecular modeling study”. 《Journal of Molecular Graphics》 12 (1): 22–8, 34. doi:10.1016/0263-7855(94)80004-9. PMID 8011597.
Wilkie TM, Chen Y, Gilbert DJ, Moore KJ, Yu L, Simon MI, Copeland NG, Jenkins NA (1994). “Identification, chromosomal location, and genome organization of mammalian G-protein-coupled receptors”. 《Genomics》 18 (2): 175–84. doi:10.1006/geno.1993.1452. PMID 8288218.
Krief S, Lönnqvist F, Raimbault S, Baude B, Van Spronsen A, Arner P, Strosberg AD, Ricquier D, Emorine LJ (1993). “Tissue distribution of beta 3-adrenergic receptor mRNA in man”. 《J. Clin. Invest.》 91 (1): 344–9. doi:10.1172/JCI116191. PMC 330032. PMID 8380813.
van Spronsen A, Nahmias C, Krief S, Briend-Sutren MM, Strosberg AD, Emorine LJ (1993). “The promoter and intron/exon structure of the human and mouse beta 3-adrenergic-receptor genes”. 《Eur. J. Biochem.》 213 (3): 1117–24. doi:10.1111/j.1432-1033.1993.tb17861.x. PMID 8389293.
Lelias JM, Kaghad M, Rodriguez M, Chalon P, Bonnin J, Dupre I, Delpech B, Bensaid M, LeFur G, Ferrara P (1993). “Molecular cloning of a human beta 3-adrenergic receptor cDNA”. 《FEBS Lett.》 324 (2): 127–30. doi:10.1016/0014-5793(93)81377-C. PMID 8389717.
Candelore MR, Deng L, Tota LM, Kelly LJ, Cascieri MA, Strader CD (1996). “Pharmacological characterization of a recently described human beta 3-adrenergic receptor mutant”. 《Endocrinology》 137 (6): 2638–41. doi:10.1210/en.137.6.2638. PMID 8641219.
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Cao W, Luttrell LM, Medvedev AV, Pierce KL, Daniel KW, Dixon TM, Lefkowitz RJ, Collins S (2001). “Direct binding of activated c-Src to the beta 3-adrenergic receptor is required for MAP kinase activation”. 《J. Biol. Chem.》 275 (49): 38131–4. doi:10.1074/jbc.C000592200. PMID 11013230.
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외부 링크

“β₃-adrenoceptor”. 《IUPHAR Database of Receptors and Ion Channels》. International Union of Basic and Clinical Pharmacology. 2014년 12월 30일에 원본 문서에서 보존된 문서. 2021년 3월 25일에 확인함.
인간 ADRB3 게놈 위치와 ADRB3 유전자의 상세한 설명은 UCSC 게놈 브라우저에 있습니다.

[refGRCh38Ensembl-1] 가 ^나 ^다 GRCh38: Ensembl release 89: ENSG00000188778 - 앙상블, May 2017

[refGRCm38Ensembl-2] 가 ^나 ^다 GRCm38: Ensembl release 89: ENSMUSG00000031489 - 앙상블, May 2017

[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》.

[entrez-5] 가 ^나 “Entrez Gene: ADRB3 adrenergic, beta-3-, receptor”.

[pmid15935402-6] “Combined effects of oleoyl-estrone and a β₃-adrenergic agonist (CL316,243) on lipid stores of diet-induced overweight male Wistar rats”. 《Life Sciences》 77 (16): 2051–8. September 2005. doi:10.1016/j.lfs.2005.04.008. PMID 15935402.

[Rang163-7] Rang, H. P. (2003). 《Pharmacology》. Edinburgh: Churchill Livingstone. ISBN 0-443-07145-4.

[pmid16457637-8] “Recent Developments in the Design of Orally Bioavailable β3-Adrenergic Receptor Agonists”. 《Current Medicinal Chemistry》 13 (1): 25–37. 2006. doi:10.2174/092986706775198006. PMID 16457637.

[pmid17669397-9] “Behavioral effects of the β₃ adrenoceptor agonist SR58611A: is it the putative prototype of a new class of antidepressant/anxiolytic drugs?”. 《European Journal of Pharmacology》 573 (1–3): 139–47. November 2007. doi:10.1016/j.ejphar.2007.06.048. PMID 17669397.

[pmid18358519-10] “Confirmation of antidepressant potential of the selective β₃ adrenoceptor agonist amibegron in an animal model of depression”. 《Pharmacology Biochemistry and Behavior》 89 (4): 623–6. June 2008. doi:10.1016/j.pbb.2008.02.020. PMID 18358519.

[pmid30892909-11] “BRL37344 stimulates GLUT4 translocation and glucose uptake in skeletal muscle via β2-adrenoceptors without causing classical receptor desensitization”. 《American Journal of Physiology. Regulatory, Integrative and Comparative Physiology》 316 (5): R666–R677. May 2019. doi:10.1152/ajpregu.00285.2018. PMID 30892909.

[12] “The effects of beta(3)-adrenoceptor agonist CL-316,243 on adiponectin, adiponectin receptors and tumor necrosis factor-alpha expressions in adipose tissues of obese diabetic KKAy mice”. 《European Journal of Pharmacology》 584 (1): 202–6. 2008. doi:10.1016/j.ejphar.2008.01.028. PMID 18304529.

[pmid10411574-13] 가 ^나 ^다 “Potent and selective human beta(3)-adrenergic receptor antagonists.”. 《The Journal of Pharmacology and Experimental Therapeutics》 290 (2): 649–55. Aug 1999. PMID 10411574.

[pmid12324291-14] “Effect of a 28-d treatment with L-796568, a novel β₃-adrenergic receptor agonist, on energy expenditure and body composition in obese men”. 《The American Journal of Clinical Nutrition》 76 (4): 780–8. 2002. doi:10.1093/ajcn/76.4.780. PMID 12324291.

[15] “Mirabegron for the treatment of overactive bladder”. 《Drugs of Today》 48 (1): 25–32. 2012. doi:10.1358/dot.2012.48.1.1738056. PMID 22384458.

[16] “Nebivolol, a vasodilating selective beta(1)-blocker, is a beta(3)-adrenoceptor agonist in the nonfailing transplanted human heart”. 《J Am Coll Cardiol》 53 (17): 1532–8. doi:10.1016/j.jacc.2008.11.057. PMID 19389564.

[pmid17626794-17] “GW427353 (solabegron), a novel, selective beta3-adrenergic receptor agonist, evokes bladder relaxation and increases micturition reflex threshold in the dog”. 《The Journal of Pharmacology and Experimental Therapeutics》 323 (1): 202–9. October 2007. doi:10.1124/jpet.107.125757. PMID 17626794.

[pmid17626795-18] “Discovery of Vibegron: A Potent and Selective β3 Adrenergic Receptor Agonist for the Treatment of Overactive Bladder.”. 《Journal of Medicinal Chemistry》 59 (2): 609–23. January 2016. doi:10.1021/acs.jmedchem.5b01372. PMID 26709102.

[pmid8569714-19] “Functional studies of the first selective β₃-adrenergic receptor antagonist SR 59230A in rat brown adipocytes”. 《Mol. Pharmacol.》 49 (1): 7–14. 1996. PMID 8569714.

[pmid19422394-20] “Role of α1- and β3-adrenoceptors in the modulation by SR59230A of the effects of MDMA on body temperature in the mouse”. 《British Journal of Pharmacology》 158 (1): 259–66. April 2009. doi:10.1111/j.1476-5381.2009.00186.x. PMC 2795232. PMID 19422394.

[pmid11013230-21] “Direct binding of activated c-Src to the beta 3-adrenergic receptor is required for MAP kinase activation”. 《J. Biol. Chem.》 275 (49): 38131–4. 2000. doi:10.1074/jbc.C000592200. PMID 11013230.

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