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wikidata:Q8054 owl:Thing dbo:Protein wikidata:Q206229 dbo:Biomolecule
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Receptor spřažený s G proteinem Receptor acoplado à proteína G Récepteur couplé aux protéines G G-proteïnegekoppelde receptor G蛋白偶联受体 Receptor acoplado a proteínas G Reseptor terhubung protein G Receptor acoblat a proteïnes G G-білокспряжені рецептори G protein-coupled receptor G 단백질 연결 수용체 مستقبل مقترن بالبروتين ج G proteinei loturiko hartzaile Recettori accoppiati a proteine G Receptory sprzężone z białkami G G-proteinkopplade receptorer Υποδοχέας συζευγμένος με πρωτεΐνη G G-Protein-gekoppelte Rezeptoren Gタンパク質共役受容体 GPCR
rdfs:comment
Рецепторы, сопряжённые с G-белком, (англ. G-protein-coupled receptors, GPCRs), также известные как семиспиральные рецепторы или серпантинные рецепторы, составляют большое семейство трансмембранных рецепторов. GPCR выполняют функцию активаторов внутриклеточных путей передачи сигнала, приводящими в итоге к клеточному ответу. Рецепторы этого семейства обнаружены только в клетках эукариот: у дрожжей, растений, хоанофлагеллят и животных. Эндогенные лиганды-агонисты, которые связываются и активируют эти рецепторы, включают гормоны, нейромедиаторы, светочувствительные вещества, пахучие вещества, феромоны и варьируются в своих размерах от небольших молекул и пептидов до белков. Нарушение работы GPCR приводит к возникновению множества различных заболеваний, а сами рецепторы являются мишенью до 40 % I recettori accoppiati alle proteine G (o GPCR) sono una famiglia di recettori biologici che comprende i recettori colinergici muscarinici, i recettori adrenergici, dopaminergici, serotoninergici, i recettori cannabinoidi e i recettori degli oppiacei e delle purine. Gタンパク質共役受容体(ジータンパクしつきょうやくじゅようたい、英: G protein-coupled receptor、GPCR)は、生体に存在する受容体の形式の1つである。様々な機能を持ったGタンパク質共役受容体が見られ、既知のタンパク質の中では最大のスーパーファミリーを形成している。別名としてGタンパク質結合受容体、あるいは細胞膜を7回貫通する特徴的な構造から7回膜貫通型受容体(ななかいまくかんつうがたじゅようたい)と呼ばれることもある。細胞外の神経伝達物質やホルモンを受容してそのシグナルを細胞内に伝えるが、その際Gタンパク質と呼ばれる三量体タンパクを介してシグナル伝達が行われる。Gタンパク質共役受容体には様々な種類が存在し、多くの疾患に関与しているため、市販薬の数割がGタンパク質共役受容体のうちのいずれかを標的としている。 G蛋白偶联受体(G protein-coupled receptor,GPCRs),是一大类膜蛋白受体的统称。 这类受体的共同点是其立体结构中都有七个跨膜α螺旋,且其肽链的C端和连接第5和第6个跨膜螺旋的胞内环上都有G蛋白(鸟苷酸结合蛋白)的结合位点。 目前为止,只在真核生物中发现G蛋白偶联受体。它们参与很多细胞信号转导过程。在这些过程中,G蛋白偶联受体能结合细胞周围环境中的化学物质并激活细胞内的一系列信号通路,最终引起细胞状态的改变。已知的与G蛋白偶联受体结合的配体包括气味分子、费洛蒙、荷尔蒙、神经递质、趋化因子等等。这些受体可以是小分子的糖类、脂质、多肽,也可以是蛋白质等生物大分子。一些特殊的G蛋白偶联受体也可以被非化学性的刺激源激活,例如在感光细胞中的视紫红质可以被光所激活。与G蛋白偶联受体相关的疾病为数众多,并且大约40%的现代药物都以G蛋白偶联受体作为靶点。 G-proteinkopplade receptorer är en grupp transmembranproteiner som fungerar som receptorer, vilka uppfattar molekyler utanför cellen och möjliggör signaltransduktion i cellen, och därmed möjliggör cellulära responser. Ligander som fäster vid, och aktiverar, receptorerna innefattar odörer, feromoner, hormoner och signalsubstanser – dessa varierar i storlek från små molekyler till större peptider till stora proteiner. Några exempel på G-proteinkopplade receptorer är G-білокспряжені рецептори (GPCR, англ. G protein-coupled receptors) також відомі як рецептори, спряжені з G-білками чи 7TM-рецептори (сім-трансмембран, англ. 7 transmembrane) належать до найбільшої групи трансмембранних рецепторів. Це білки, які у відповідь на різноманітні сигнали, включаючи фотони світла, гормони, білки та ліпіди, активують поєднані з ними G-білків і передають сигнал всередину клітини. Приблизно 30-40 % фармакологічних препаратів діють на G-білокспряжені рецептори, включаючи β-блокатори, опіоїдні агоністи, антигістаміни та блокатори ангіотензинових рецепторів. Receptory sprzężone z białkami G (GPCR – z ang. G Protein-Coupled Receptor; receptory siedmiotransbłonowe, 7TM) – rodzaj transmembranowych receptorów metabotropowych, które reagują na sygnały docierające do komórki za pośrednictwem neuroprzekaźników aktywując białko G związane z receptorem po drugiej stronie błony komórkowej. G proteinei loturiko hartzaileak (ingelesez: G protein-coupled receptor; GPCR siglekin ezaguna) seinaleztapenean berebiziko funtzioa betetzen duten mintzean zeharreko 7 domeinuz osatutako proteina eukariotikoak dira; izan ere, giza familiarik handiena osatzen dute, 800 GPCR inguru identifikatu direlarik. Horrez gain, familia handi hori 5 talde nagusitan sailkatu da, GRAFS siglez adierazten direnak: Glutamate (Glutamato), Rhodopsin (Errodopsina), Adhesion (Atxikidura), Frizzled eta Secretin. GPCR talde nagusi horiek azpitaldetan ere sailkatzen dira, sekuentzien arteko antzekotasunetan oinarrituta. G protein-coupled receptors (GPCRs), also known as seven-(pass)-transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptors, and G protein-linked receptors (GPLR), form a large group of evolutionarily-related proteins that are cell surface receptors that detect molecules outside the cell and activate cellular responses. Coupling with G proteins, they are called seven-transmembrane receptors because they pass through the cell membrane seven times. Ligands can bind either to extracellular N-terminus and loops (e.g. glutamate receptors) or to the binding site within transmembrane helices (Rhodopsin-like family). They are all activated by agonists although a spontaneous auto-activation of an empty receptor can also be observed. Les récepteurs couplés aux protéines G (RCPG) sont une famille de récepteurs membranaires chez les mammifères. Parmi les nombreux récepteurs qui jouent un rôle dans la communication cellulaire, les récepteurs couplés aux protéines G (RCPG) constituent la plus grande famille de récepteurs membranaires de mammifères puisqu’elle représente 3,4 % du génome. Plus de la moitié des agents pharmacologiques agissent sur les RCPG : ils sont donc une classe de protéines d'importance thérapeutique majeure. G-proteïnegekoppelde receptoren (Engels: G protein-coupled receptor, GPCR) vormen een biologisch belangrijke klasse van metabotrope receptoren. Ze spelen een rol in een groot aantal signaaltransductieprocessen. Een belangrijke karakteristiek van GPCR's is, dat ze zeven zogenaamde hebben. Deze domeinen bestaan uit een α-helix die de celmembraan overspant. De GPCRs zijn geclassificeerd in 6 subfamilies: Ongeveer 40 % van de geneesmiddelen heeft een GPCR als aangrijpingspunt. مستقبل مقترن بالبروتين ج والمعروف - أيضًا - بالمستقبل السباعي عبر الغشاء، مستقبل هيبتاثيليكال، ومستقبل متصل بالبروتين ج. وهي عائلة من البروتينات عبر الغشائية التي تستقبل الحوافز والإشارات الخارجية وتوصلها إلى داخل الخلية. عائلة البروتينات «مستقبل مقترن بالبروتين ج» هي أكبر عائلة بروتينات معروفة، أعضاء هذه العائلة يتشاركون في جميع أنواع الطرق للاستجابة للمحفزات، بدءاً من الاتصالات داخل الخلية وانتهاءً بالحواس الفيزيولوجية. Οι υποδοχείς συζευγμένοι με πρωτεΐνη G (αγγλικά: G protein–coupled receptors: GPCRs), επίσης γνωστοί ως υποδοχείς µε 7 διαµεµβρανικές περιοχές (υποδοχείς 7TM), αποτελούν μια μεγάλη πρωτεϊνική οικογένεια υποδοχέων που ανιχνεύουν μόρια εξωτερικά του κυττάρου, ενεργοποιούν ενδοκυτταρικά σηματοδοτικά μονοπάτια και, τελικά, κυτταρικές αποκρίσεις. Ονομάζονται και υποδοχείς µε 7 διαµεµβρανικές περιοχές (7TM), επειδή διαπερνούν την κυτταρική μεμβράνη επτά φορές. Υπάρχουν δύο κύρια μονοπάτια μεταγωγής σήματος στα οποία εμπλέκονται οι υποδοχείς συζευγμένοι με πρωτεΐνες G: G-Protein-gekoppelte Rezeptoren (englisch G protein-coupled receptor, GPCR) sind biologische Rezeptoren in der Zellmembran und der Membran von Endosomen, die Signale über GTP-bindende Proteine (kurz G-Proteine) in das Zellinnere beziehungsweise das Innere des Endosoms weiterleiten (Signaltransduktion). In der Neurobiologie wird für G-Protein-gekoppelte Rezeptoren häufig der Begriff metabotrope Rezeptoren verwendet, um sie von einem anderen Rezeptortyp, den ligandengesteuerten Ionenkanälen (Ionotroper Rezeptor), zu unterscheiden. Diese Unterscheidung ist jedoch nicht ausreichend trennscharf, denn auch enzym-gekoppelte Rezeptoren gehören zu den metabotropen Rezeptoren. Los receptores acoplados a proteínas G o RAPG (en inglés, GPCR: G protein-coupled receptors), también conocidos como receptores transmembrana de siete dominios, receptores 7TM, receptores heptahelicoidales, receptor serpentina, y receptores ligados a proteínas G, comprenden una gran familia de proteínas de receptores transmembrana que responden a una variedad de estímulos extracelulares que van desde fotones y pequeñas moléculas hasta péptidos y proteínas, tales como hormonas, neurotransmisores y agentes paracrinos los cuales activan las vías de transducción de señales y, finalmente, dan origen a las respuestas celulares específicas. En el ser humano existen más de 800 RAPG diferentes, ubicados en distintos sistemas, que participan en funciones tan variadas como la visión, el olfato, el gu Els receptors acoblats a proteïnes G (GPCR, de l'anglès: G protein-coupled receptors), també coneguts com a receptors transmembrana de set dominis, receptors 7TM, receptors heptahelicoidals, receptor serpentina, i receptors lligats a proteïnes G (GPLR, de l'anglès: G protein-linked receptors), comprenen una gran família de proteïnes de receptors transmembrana que perceben molècules fora de la cèl·lula i activen les vies de transducció de senyals i, finalment, les respostes cel·lulars. Els receptors acoblats a proteïnes G només es troben en organismes eucariotes, incloent els llevats, coanoflagel·lats i animals. Els lligands químics que enllacen i activen aquests receptors inclouen compostos sensibles a la llum, olors, feromones, hormones, i neurotransmissors, i varien des de la mida de mol Receptor spřažený s G proteinem (GPCR – G protein-coupled receptor) je označení pro skupinu receptorů přítomných na cytoplazmatické membráně buněk. Skládají se ze sedmi transmembránových alfa-helixových domén a přiléhajících smyček, které na vnitrobuněčné straně membrány asociují s G-proteinem. G 단백질 연결 수용체(G protein coupled receptor, GPCR)는 7-막관통 수용체(7-Transmembrane receptor, 7TMR)라고도 불린다. 이름에서 알 수 있듯이 [그림 1]에서 살펴보면 이것의 구조는 세포막 혹은 세포 내의 기관의 세포막에서 세포질 면과 세포 외면에 걸쳐있고 막을 7번 통과하는 구조이다. 생체내에서 800~1000개 정도의 수용체의 종류가 존재 하고, 사실상 생체내의 거의 모든 생리적 반응을 촉매한다 이것의 종류는 크게 5 가지로 나뉘며 (type A, B, C, D, E, F), type A에는 빛을 감지하는 로돕신, 냄새를 감지하는 후감각 수용체, 아드레날린 혹은 노르아드레날린을 감지하는 아드레날린 수용체가 있다. Type B에는 가 존재하며, Type C에는 글루타메이트 수용체 그리고 미감각 수용체가 존재한다고 알려져 있다. 이때 수용체에 붙는 물질을 리간드라고 정의하며 리간드는 수용체의 반응을 촉진하는 수용체 작용제와 반응을 촉진하지 않는 수용체 대항제로 나뉘게 된다. Receptores acoplados às proteínas G são uma grande família proteica de receptores transmembranares que captam sinais extracelulares e activam vias de transdução de sinal no interior da célula. Este tipo de receptores apenas é encontrado nos eucariotas, como é o caso das leveduras, plantas, coanoflagelados, e animais. Os ligandos que se ligam e activam estes receptores incluem compostos sensíveis à luz, odores, feromonas, hormonas e neurotransmissores, e variam em tamanho, desde pequenas moléculas, até péptidos, podendo mesmo ser grandes proteínas. Reseptor terhubung protein G (GPCR), juga dikenal sebagai reseptor domain tujuh transmembran, reseptor 7TM, reseptor heptaheliks, reseptor serpentin, dan reseptor terkait protein G (GPLR), merupakan famili protein besar dari reseptor yang mendeteksi molekul di luar sel dan mengaktifkan jalur transduksi sinyal internal dan memberikan respons seluler. Ada dua jalur transduksi sinyal utama yang melibatkan reseptor terhubung protein G yaitu jalur sinyal cAMP dan jalur sinyal fosfatidlinositol.
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Reseptor terhubung protein G (GPCR), juga dikenal sebagai reseptor domain tujuh transmembran, reseptor 7TM, reseptor heptaheliks, reseptor serpentin, dan reseptor terkait protein G (GPLR), merupakan famili protein besar dari reseptor yang mendeteksi molekul di luar sel dan mengaktifkan jalur transduksi sinyal internal dan memberikan respons seluler. Reseptor terhubung protein G hanya ditemukan pada eukariota, termasuk khamir, choanoflagellata, dan hewan. Ligan yang mengikat dan mengaktifkan reseptor ini termasuk senyawa sensitif cahaya, bau, feromon, hormon, dan neurotransmiter, dan bervariasi dalam ukuran dari molekul kecil ke peptida hingga protein besar. Reseptor terhubung protein G terlibat dalam banyak penyakit, dan juga merupakan target sekitar 34% dari semua obat-obatan modern. Ada dua jalur transduksi sinyal utama yang melibatkan reseptor terhubung protein G yaitu jalur sinyal cAMP dan jalur sinyal fosfatidlinositol. Ketika ligan mengikat GPCR, ligan menyebabkan perubahan konformasi pada GPCR, yang memungkinkannya bertindak sebagai faktor pertukaran nukleotida guanin (Guanine nucleotide exchanger factor, GEF). GPCR kemudian dapat mengaktifkan protein G terkait dengan menukar GDP terikat ke protein G dengan GTP. Subunit protein Gα, bersama dengan GTP terikat, kemudian dapat dipisahkan dari subunit β dan γ untuk lebih lanjut memengaruhi protein pensinyalan intraseluler atau menargetkan protein fungsional secara langsung tergantung pada jenis subunit α , , , . :1160 GPCR merupakan target obat yang penting dan sekitar 34% dari semua obat yang disetujui oleh FDA AS menargetkan 108 anggota famili ini. Volume penjualan global untuk obat-obatan ini diperkirakan 180 miliar dolar AS hingga tahun 2018. G-proteinkopplade receptorer är en grupp transmembranproteiner som fungerar som receptorer, vilka uppfattar molekyler utanför cellen och möjliggör signaltransduktion i cellen, och därmed möjliggör cellulära responser. Ligander som fäster vid, och aktiverar, receptorerna innefattar odörer, feromoner, hormoner och signalsubstanser – dessa varierar i storlek från små molekyler till större peptider till stora proteiner. Receptorerna för solljus i ögats sinnesceller är också en form av G-proteinkopplad receptor, fast istället för en löslig ligand binder receptorn rodopsin, som ändrar sin struktur när det träffas av solljus, vilket aktiverar receptorn. De första G-proteinkopplade receptorerna upptäcktes och utforskades av Robert Lefkowitz omkring 1968 då han fann att det fanns adrenerga receptorer på cellytor. Brian Kobilka rekryterades på 1980-talet till dennes forskningsgrupp, och han visade att de beta-adrenerga receptorerna påminde om ljusreceptorerna i ögat. Därmed insåg de att det var fråga om en grupp receptorer med liknande beteende och utseende. Lefkowitz och Kobilka tilldelades Nobelpriset i kemi år 2012. Några exempel på G-proteinkopplade receptorer är * * histaminreceptorer * * dopaminreceptorer * adrenerga receptorer * oxytocinreceptorer * tyrotropinreceptor * TRH-receptor * muskarinreceptorer * glutamatreceptorer I recettori accoppiati alle proteine G (o GPCR) sono una famiglia di recettori biologici che comprende i recettori colinergici muscarinici, i recettori adrenergici, dopaminergici, serotoninergici, i recettori cannabinoidi e i recettori degli oppiacei e delle purine. Gタンパク質共役受容体(ジータンパクしつきょうやくじゅようたい、英: G protein-coupled receptor、GPCR)は、生体に存在する受容体の形式の1つである。様々な機能を持ったGタンパク質共役受容体が見られ、既知のタンパク質の中では最大のスーパーファミリーを形成している。別名としてGタンパク質結合受容体、あるいは細胞膜を7回貫通する特徴的な構造から7回膜貫通型受容体(ななかいまくかんつうがたじゅようたい)と呼ばれることもある。細胞外の神経伝達物質やホルモンを受容してそのシグナルを細胞内に伝えるが、その際Gタンパク質と呼ばれる三量体タンパクを介してシグナル伝達が行われる。Gタンパク質共役受容体には様々な種類が存在し、多くの疾患に関与しているため、市販薬の数割がGタンパク質共役受容体のうちのいずれかを標的としている。 Receptores acoplados às proteínas G são uma grande família proteica de receptores transmembranares que captam sinais extracelulares e activam vias de transdução de sinal no interior da célula. Este tipo de receptores apenas é encontrado nos eucariotas, como é o caso das leveduras, plantas, coanoflagelados, e animais. Os ligandos que se ligam e activam estes receptores incluem compostos sensíveis à luz, odores, feromonas, hormonas e neurotransmissores, e variam em tamanho, desde pequenas moléculas, até péptidos, podendo mesmo ser grandes proteínas. Estes receptores estão envolvidos numa variedade de doenças, mas também são o alvo de cerca de metade das drogas medicinais humanas. G protein-coupled receptors (GPCRs), also known as seven-(pass)-transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptors, and G protein-linked receptors (GPLR), form a large group of evolutionarily-related proteins that are cell surface receptors that detect molecules outside the cell and activate cellular responses. Coupling with G proteins, they are called seven-transmembrane receptors because they pass through the cell membrane seven times. Ligands can bind either to extracellular N-terminus and loops (e.g. glutamate receptors) or to the binding site within transmembrane helices (Rhodopsin-like family). They are all activated by agonists although a spontaneous auto-activation of an empty receptor can also be observed. G protein-coupled receptors are found only in eukaryotes, including yeast, choanoflagellates, and animals. The ligands that bind and activate these receptors include light-sensitive compounds, odors, pheromones, hormones, and neurotransmitters, and vary in size from small molecules to peptides to large proteins. G protein-coupled receptors are involved in many diseases. There are two principal signal transduction pathways involving the G protein-coupled receptors: * the cAMP signal pathway and * the phosphatidylinositol signal pathway. When a ligand binds to the GPCR it causes a conformational change in the GPCR, which allows it to act as a guanine nucleotide exchange factor (GEF). The GPCR can then activate an associated G protein by exchanging the GDP bound to the G protein for a GTP. The G protein's α subunit, together with the bound GTP, can then dissociate from the β and γ subunits to further affect intracellular signaling proteins or target functional proteins directly depending on the α subunit type (Gαs, Gαi/o, Gαq/11, Gα12/13). GPCRs are an important drug target and approximately 34% of all Food and Drug Administration (FDA) approved drugs target 108 members of this family. The global sales volume for these drugs is estimated to be 180 billion US dollars as of 2018. It is estimated that GPCRs are targets for about 50% of drugs currently on the market, mainly due to their involvement in signaling pathways related to many diseases i.e. mental, metabolic including endocrinological disorders, immunological including viral infections, cardiovascular, inflammatory, senses disorders, and cancer. The long ago discovered association between GPCRs and many endogenous and exogenous substances, resulting in e.g. analgesia, is another dynamically developing field of the pharmaceutical research. Los receptores acoplados a proteínas G o RAPG (en inglés, GPCR: G protein-coupled receptors), también conocidos como receptores transmembrana de siete dominios, receptores 7TM, receptores heptahelicoidales, receptor serpentina, y receptores ligados a proteínas G, comprenden una gran familia de proteínas de receptores transmembrana que responden a una variedad de estímulos extracelulares que van desde fotones y pequeñas moléculas hasta péptidos y proteínas, tales como hormonas, neurotransmisores y agentes paracrinos los cuales activan las vías de transducción de señales y, finalmente, dan origen a las respuestas celulares específicas. En el ser humano existen más de 800 RAPG diferentes, ubicados en distintos sistemas, que participan en funciones tan variadas como la visión, el olfato, el gusto; funciones neurológicas, cardiovasculares, endocrinas y reproductivas. Esta ubicuidad convierte a los RAPGs en un objetivo principal del desarrollo farmacológico siendo el blanco de aproximadamente el 40% de todos los fármacos modernos.​​​​​​ Los receptores acoplados a proteínas G solo se encuentran en eukaryotas, incluyendo la levadura, choanomonadas y animales.​ Hay dos vías de transducción de señales principales que involucran a los receptores acoplados a proteínas G: la vía de señal cAMP (Adenosín monofosfato cíclico) y la vía de señal fosfatidilinositol.​ Cuando un ligando se liga al RAPG, este provoca un cambio conformacional en el RAPG, lo que le permite actuar como un factor intercambiador de nucleótido de guanina (GEF). El RAPG puede entonces activar una proteína G asociada mediante el intercambio de su GDP (Guanosín difosfato) enlazado por un GTP (Guanosín trifosdato). Receptor spřažený s G proteinem (GPCR – G protein-coupled receptor) je označení pro skupinu receptorů přítomných na cytoplazmatické membráně buněk. Skládají se ze sedmi transmembránových alfa-helixových domén a přiléhajících smyček, které na vnitrobuněčné straně membrány asociují s G-proteinem. G-Protein-gekoppelte Rezeptoren (englisch G protein-coupled receptor, GPCR) sind biologische Rezeptoren in der Zellmembran und der Membran von Endosomen, die Signale über GTP-bindende Proteine (kurz G-Proteine) in das Zellinnere beziehungsweise das Innere des Endosoms weiterleiten (Signaltransduktion). In der Neurobiologie wird für G-Protein-gekoppelte Rezeptoren häufig der Begriff metabotrope Rezeptoren verwendet, um sie von einem anderen Rezeptortyp, den ligandengesteuerten Ionenkanälen (Ionotroper Rezeptor), zu unterscheiden. Diese Unterscheidung ist jedoch nicht ausreichend trennscharf, denn auch enzym-gekoppelte Rezeptoren gehören zu den metabotropen Rezeptoren. Die Familie der G-Protein-gekoppelten Rezeptoren stellt mit mehr als 1000 verschiedenen Mitgliedern die größte Proteinsuperfamilie dar. G-Protein-gekoppelte Rezeptoren sind für die Verarbeitung von Licht-, Geruchs- und einer Vielzahl von Geschmacksreizen verantwortlich. Sie spielen eine entscheidende Rolle bei Entzündungsprozessen, der gezielten Zellbewegung (Taxis), dem Transport von Stoffen durch die Zellmembran (Endozytose und Exozytose) sowie beim Zellwachstum und bei der Zelldifferenzierung. Sie sind darüber hinaus als Zielstrukturen für die Wirkung von Hormonen, wie Adrenalin oder Glucagon, und Neurotransmittern, wie Serotonin und Acetylcholin, verantwortlich. Auch einige Viren nutzen G-Protein-gekoppelte Rezeptoren als Bindungsstellen für den Eintritt in die Zelle (beispielsweise HIV). G 단백질 연결 수용체(G protein coupled receptor, GPCR)는 7-막관통 수용체(7-Transmembrane receptor, 7TMR)라고도 불린다. 이름에서 알 수 있듯이 [그림 1]에서 살펴보면 이것의 구조는 세포막 혹은 세포 내의 기관의 세포막에서 세포질 면과 세포 외면에 걸쳐있고 막을 7번 통과하는 구조이다. 생체내에서 800~1000개 정도의 수용체의 종류가 존재 하고, 사실상 생체내의 거의 모든 생리적 반응을 촉매한다 이것의 종류는 크게 5 가지로 나뉘며 (type A, B, C, D, E, F), type A에는 빛을 감지하는 로돕신, 냄새를 감지하는 후감각 수용체, 아드레날린 혹은 노르아드레날린을 감지하는 아드레날린 수용체가 있다. Type B에는 가 존재하며, Type C에는 글루타메이트 수용체 그리고 미감각 수용체가 존재한다고 알려져 있다. 이때 수용체에 붙는 물질을 리간드라고 정의하며 리간드는 수용체의 반응을 촉진하는 수용체 작용제와 반응을 촉진하지 않는 수용체 대항제로 나뉘게 된다. مستقبل مقترن بالبروتين ج والمعروف - أيضًا - بالمستقبل السباعي عبر الغشاء، مستقبل هيبتاثيليكال، ومستقبل متصل بالبروتين ج. وهي عائلة من البروتينات عبر الغشائية التي تستقبل الحوافز والإشارات الخارجية وتوصلها إلى داخل الخلية. عائلة البروتينات «مستقبل مقترن بالبروتين ج» هي أكبر عائلة بروتينات معروفة، أعضاء هذه العائلة يتشاركون في جميع أنواع الطرق للاستجابة للمحفزات، بدءاً من الاتصالات داخل الخلية وانتهاءً بالحواس الفيزيولوجية. تنوع الوظائف هو بسبب تنوع المحفزات التي تستقبلها هذه المستقبلات من هذه المجموعة (العائلة)، من فوتونات ضوئية (مثل في مستقبلات الرودوبسين في العين) إلى الجزيئات الصغيرة (مثل مستقبلات الهستامين) إلى بروتينات كبيرة (مثل مستقبلي المحرك الكيميائي). وبسبب هذا التنوع والانشغال في العديد من الوظائف الفيزيولوجية والانخراط في عدة من الوظائف المرضية، فإن 40-50% من الأدوية الحديثة تستهدف التأثير على المستقبلات من أعضاء هذه العائلة. بعد تحليل شامل لما يقارب مئتي تسلسل من مستقبل مقترن بالبروتين ج، أظهرت النتائج أن الطول الإجمالي للمستقبل المقترن بالبروتين ج يتفاوت بين 311 إلى ما يقارب 1490 حمض أميني، وأكبر اختلاف في الطول يوجد في النهايات الأمينية والكربوكسيلية حيث قد يصل طولها إلى 879 و 371 حمض أميني على الترتيب. G蛋白偶联受体(G protein-coupled receptor,GPCRs),是一大类膜蛋白受体的统称。 这类受体的共同点是其立体结构中都有七个跨膜α螺旋,且其肽链的C端和连接第5和第6个跨膜螺旋的胞内环上都有G蛋白(鸟苷酸结合蛋白)的结合位点。 目前为止,只在真核生物中发现G蛋白偶联受体。它们参与很多细胞信号转导过程。在这些过程中,G蛋白偶联受体能结合细胞周围环境中的化学物质并激活细胞内的一系列信号通路,最终引起细胞状态的改变。已知的与G蛋白偶联受体结合的配体包括气味分子、费洛蒙、荷尔蒙、神经递质、趋化因子等等。这些受体可以是小分子的糖类、脂质、多肽,也可以是蛋白质等生物大分子。一些特殊的G蛋白偶联受体也可以被非化学性的刺激源激活,例如在感光细胞中的视紫红质可以被光所激活。与G蛋白偶联受体相关的疾病为数众多,并且大约40%的现代药物都以G蛋白偶联受体作为靶点。 G蛋白偶联受体的下游信号通路有多种。与配体结合的G蛋白偶联受体会发生构象变化,从而表现出(GEF)的特性,通过以三磷酸鸟苷(GTP)交换G蛋白上本来结合着的二磷酸鳥苷(GDP)使G蛋白的α亚基与β、γ亚基分离。这一过程使得G蛋白(特别地,指其与GTP结合着的α亚基)变为激活状态,并参与下一步的信号传递过程。具体的传递通路取决于α亚基的种类(、、、)。其中主要的两个通路分别以由三磷酸腺苷环化产生的环腺苷酸(cAMP)和由(PIP2)水解生成的肌醇三磷酸(IP3)和甘油二酯(DAG)作为第二信使, 详见环腺苷酸信号通路和磷脂酰肌醇信号通路。 G proteinei loturiko hartzaileak (ingelesez: G protein-coupled receptor; GPCR siglekin ezaguna) seinaleztapenean berebiziko funtzioa betetzen duten mintzean zeharreko 7 domeinuz osatutako proteina eukariotikoak dira; izan ere, giza familiarik handiena osatzen dute, 800 GPCR inguru identifikatu direlarik. Horrez gain, familia handi hori 5 talde nagusitan sailkatu da, GRAFS siglez adierazten direnak: Glutamate (Glutamato), Rhodopsin (Errodopsina), Adhesion (Atxikidura), Frizzled eta Secretin. GPCR talde nagusi horiek azpitaldetan ere sailkatzen dira, sekuentzien arteko antzekotasunetan oinarrituta. GPCRak mintzean zeharreko domeinuez osatutako proteinak dira, alegia, zelula-mintzean kokatuta daude eta, zelulaz kanpoko hainbat kinada ezagutzen dituzte, besteak beste, fotoiak, ioiak, usainarekin lotutako molekulak, feromonak, hormonak, lipidoak, peptidoak eta proteinak. Kinada horietako bat jasotzen dutenean, abiarazten dute edo G proteinen bidezko piztuz, erantzun fisiologikoa eragiteko helburuarekin. Gainera, aipatzekoa da GPCRen bidezidorra giza gaixotasun askorekin lotu dela; horregatik, gaur egun erabiltzen diren farmakoen % 30-50ek GPCRak dituzte itu gisa. Οι υποδοχείς συζευγμένοι με πρωτεΐνη G (αγγλικά: G protein–coupled receptors: GPCRs), επίσης γνωστοί ως υποδοχείς µε 7 διαµεµβρανικές περιοχές (υποδοχείς 7TM), αποτελούν μια μεγάλη πρωτεϊνική οικογένεια υποδοχέων που ανιχνεύουν μόρια εξωτερικά του κυττάρου, ενεργοποιούν ενδοκυτταρικά σηματοδοτικά μονοπάτια και, τελικά, κυτταρικές αποκρίσεις. Ονομάζονται και υποδοχείς µε 7 διαµεµβρανικές περιοχές (7TM), επειδή διαπερνούν την κυτταρική μεμβράνη επτά φορές. Οι υποδοχείς συζευγμένοι με πρωτεΐνη G βρίσκονται μόνο σε ευκαρυωτικά κύτταρα, συμπεριλαμβανομένης της μαγιάς, του μαστιγοφόρου πρώτιστου του είδους των choanoflagellates, και των ζώων. Οι προσδέτες που δεσμεύονται και ενεργοποιούν αυτούς τους υποδοχείς περιλαμβάνουν , οσμές, φερομόνες, ορμόνες και νευροδιαβιβαστές και ποικίλουν σε μέγεθος από μικρά μόρια έως πεπτίδια και μεγάλες πρωτεΐνες. Οι GPCRs εμπλέκονται σε πολλές ασθένειες, και είναι επίσης ο στόχος του 34% περίπου όλων των σύγχρονων φαρμάκων. Υπάρχουν δύο κύρια μονοπάτια μεταγωγής σήματος στα οποία εμπλέκονται οι υποδοχείς συζευγμένοι με πρωτεΐνες G: * το σηματοδοτικό μονοπάτι της * το σηματοδοτικό μονοπάτι της . Όταν ένας προσδέτης συνδέεται με τον GPCR προκαλεί μία αλλαγή στην διαμόρφωση αυτού, η οποία επιτρέπει στον υποδοχέα να ενεργήσει ως (GEF). Ο GPCR μπορεί στη συνέχεια να ενεργοποιήσει μια ενωμένη με αυτόν , με την ανταλλαγή του GDP που είναι συνδεδεμένο στην G πρωτεΐνη για . Η α-υπομονάδα της G πρωτεΐνης, μαζί με το δεσμευμένο GTP, μπορεί έπειτα να απομακρυνθεί από τις β- και γ- υπομονάδες και να επηρεάσει περαιτέρω ενδοκυτταρικές σηματοδοτικές πρωτεΐνες ή να στοχοποιήσει λειτουργικές πρωτεΐνες, γεγονός που εξαρτάται άμεσα από τον υπότυπο της α- υπομονάδας (Gαs, Gαi/o, Gαq/11, Gα12/13). Receptory sprzężone z białkami G (GPCR – z ang. G Protein-Coupled Receptor; receptory siedmiotransbłonowe, 7TM) – rodzaj transmembranowych receptorów metabotropowych, które reagują na sygnały docierające do komórki za pośrednictwem neuroprzekaźników aktywując białko G związane z receptorem po drugiej stronie błony komórkowej. Les récepteurs couplés aux protéines G (RCPG) sont une famille de récepteurs membranaires chez les mammifères. Parmi les nombreux récepteurs qui jouent un rôle dans la communication cellulaire, les récepteurs couplés aux protéines G (RCPG) constituent la plus grande famille de récepteurs membranaires de mammifères puisqu’elle représente 3,4 % du génome. Plus de la moitié des agents pharmacologiques agissent sur les RCPG : ils sont donc une classe de protéines d'importance thérapeutique majeure. Ces récepteurs doivent leur appellation à leur capacité de couplage, une fois activés, à des protéines hétérotrimériques liant le GTP (guanosine triphosphate), aussi appelées protéines G. Ces protéines transmettent le signal provenant du récepteur à différents effecteurs intracellulaires permettant la génération d’une réponse cellulaire appropriée. L’isolation puis le clonage des RCPG a permis d’identifier chez l’être humain autour de 900 gènes dont environ 500 correspondent aux récepteurs olfactifs et gustatifs et 400 à des récepteurs capables de lier des ligands endogènes. Ainsi, l’hétérogénéité de ces récepteurs assure une reconnaissance très large de signaux tant externes (odeurs, lumière, molécules du goût) qu'internes (hormones et neurotransmetteurs). Els receptors acoblats a proteïnes G (GPCR, de l'anglès: G protein-coupled receptors), també coneguts com a receptors transmembrana de set dominis, receptors 7TM, receptors heptahelicoidals, receptor serpentina, i receptors lligats a proteïnes G (GPLR, de l'anglès: G protein-linked receptors), comprenen una gran família de proteïnes de receptors transmembrana que perceben molècules fora de la cèl·lula i activen les vies de transducció de senyals i, finalment, les respostes cel·lulars. Els receptors acoblats a proteïnes G només es troben en organismes eucariotes, incloent els llevats, coanoflagel·lats i animals. Els lligands químics que enllacen i activen aquests receptors inclouen compostos sensibles a la llum, olors, feromones, hormones, i neurotransmissors, i varien des de la mida de molècules petites (inclosos ions i protons) a pèptids a grans proteïnes. Els receptors acoblats a proteïnes G están inplicats a moltes malalties, i també són la diana del voltant del 40% dels medicaments moderns. Рецепторы, сопряжённые с G-белком, (англ. G-protein-coupled receptors, GPCRs), также известные как семиспиральные рецепторы или серпантинные рецепторы, составляют большое семейство трансмембранных рецепторов. GPCR выполняют функцию активаторов внутриклеточных путей передачи сигнала, приводящими в итоге к клеточному ответу. Рецепторы этого семейства обнаружены только в клетках эукариот: у дрожжей, растений, хоанофлагеллят и животных. Эндогенные лиганды-агонисты, которые связываются и активируют эти рецепторы, включают гормоны, нейромедиаторы, светочувствительные вещества, пахучие вещества, феромоны и варьируются в своих размерах от небольших молекул и пептидов до белков. Нарушение работы GPCR приводит к возникновению множества различных заболеваний, а сами рецепторы являются мишенью до 40 % выпускаемых лекарств. Точный размер надсемейства GPCR не известен, но почти 800 различных человеческих генов (или около 4 % от всего кодирующего белок генома) были предсказаны из анализа последовательности генома. Несмотря на многочисленные схемы, было предложено разделить надсемейство на три основных класса (a, b и c). G-білокспряжені рецептори (GPCR, англ. G protein-coupled receptors) також відомі як рецептори, спряжені з G-білками чи 7TM-рецептори (сім-трансмембран, англ. 7 transmembrane) належать до найбільшої групи трансмембранних рецепторів. Це білки, які у відповідь на різноманітні сигнали, включаючи фотони світла, гормони, білки та ліпіди, активують поєднані з ними G-білків і передають сигнал всередину клітини. G-білокспряжені рецептори беруть участь у найрізноманітніших фізіологічних процесах, включаючи відчуття смаку, зору та запаху, регуляцію тиску крові, імунологічну відповідь, поведінку та настрій. Приблизно 30-40 % фармакологічних препаратів діють на G-білокспряжені рецептори, включаючи β-блокатори, опіоїдні агоністи, антигістаміни та блокатори ангіотензинових рецепторів. G-proteïnegekoppelde receptoren (Engels: G protein-coupled receptor, GPCR) vormen een biologisch belangrijke klasse van metabotrope receptoren. Ze spelen een rol in een groot aantal signaaltransductieprocessen. Een belangrijke karakteristiek van GPCR's is, dat ze zeven zogenaamde hebben. Deze domeinen bestaan uit een α-helix die de celmembraan overspant. De GPCRs zijn geclassificeerd in 6 subfamilies: * Rhodopsin familie (Klasse A), veruit de grootste familie * Secretin familie (Klasse B) * Glutamaat familie (Klasse C) * Adhesie familie (Klasse D) * Cyclisch AMP (klasse E) * Frizzled familie (Klasse F) In 1999 ontving Marc Parmentier de Francquiprijs voor zijn werk op dit vlak en in 2012 ontvingen Robert Lefkowitz en Brian Kobilka de Nobelprijs voor de Scheikunde voor hun werk aan deze G-eiwit gekoppelde receptoren. Ongeveer 40 % van de geneesmiddelen heeft een GPCR als aangrijpingspunt.
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dbr:G_protein-coupled_receptor
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dbr:Nociceptin_receptor
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dbr:G_protein-coupled_receptor
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dbr:TAS1R2
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dbr:G_protein-coupled_receptor
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dbr:Pepducin
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dbr:G_protein-coupled_receptor
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dbr:Raymond_C._Stevens
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dbr:G_protein-coupled_receptor
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dbr:TAS2R3
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dbr:G_protein-coupled_receptor
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dbr:Oxoeicosanoid_receptor_1
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dbr:P2Y12
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dbr:P2Y_receptor
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dbr:G_protein-coupled_receptor
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dbr:P2_receptor
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dbr:G_protein-coupled_receptor
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dbr:PHLPP
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dbr:G_protein-coupled_receptor
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dbr:PLD2
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dbr:G_protein-coupled_receptor
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dbr:PRKD3
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dbr:G_protein-coupled_receptor
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dbr:Pancreatic_islets
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dbr:G_protein-coupled_receptor
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dbr:Parathyroid_hormone_1_receptor
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dbr:G_protein-coupled_receptor
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dbr:G_protein-coupled_receptor
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dbr:Peter_N._Devreotes
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dbr:G_protein-coupled_receptor
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dbr:Thrombin_receptor
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dbr:G_protein-coupled_receptor
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dbr:Utopia_Documents
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dbr:G_protein-coupled_receptor
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dbr:Rhabdosynochus
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dbr:G_protein-coupled_receptor
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dbr:Thromboxane_receptor
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dbr:G_protein-coupled_receptor
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dbr:TRPM1
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dbr:Walker_motifs
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dbr:G_protein-coupled_receptor
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dbr:RGS7
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dbr:G_protein-coupled_receptor
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dbr:S1PR5
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dbr:SIGLEC6
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dbr:TAS2R14
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dbr:G_protein-coupled_receptor
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dbr:TRPC4
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dbr:Thyrotropin_receptor
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dbr:Target_2035
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dbr:WNT4_deficiency
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dbr:G_protein-coupled_receptor
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dbr:7-transmembrane_G-protein_coupled
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dbr:G_protein-coupled_receptor
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dbr:7-transmembrane_receptor
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dbr:7TM
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dbr:7TM_Receptor
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dbr:7TM_receptor
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dbr:7_transmembrane_receptor
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dbr:Thiamine_transporter_1
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dbr:Gi_coupled_receptor
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dbr:UPF0488
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dbr:Seven-transmembrane_protein
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dbr:Seven_transmembrane_protein
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dbr:Seven_transmembrane_region
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dbr:G-protein-coupled
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dbr:G-protein-coupled_receptors
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dbr:G-protein_coupled
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dbr:G-protein_coupled_membrane_receptors
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dbr:G_protein_coupled_receptors
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dbr:Gpcr
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dbr:Gpcrs
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dbr:Guanine_Nucleotide-Binding_Protein-Coupled_Receptor
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dbr:Receptors,_g-protein-coupled
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dbr:G_protein-coupled_receptor
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dbr:Heptahelical_receptor
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dbr:G_protein-coupled_receptor
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wikipedia-en:G_protein-coupled_receptor
foaf:primaryTopic
dbr:G_protein-coupled_receptor