GPCR & G Protein

G protein-coupled receptors (guanine nucleotide-binding protein-coupled receptors), is a general term of a large class of membrane protein receptors. A common properties of such receptors is that their three-dimensional structures all contain seven transmembrane α helix with its C-terminal of peptide chain as well as the intracellular loop connecting the fifth and sixth transmembrane helices all containing G proteins (Guanosine nucleotide-binding protein) binding site. Their major function is transducing the extracellular signal into intracellular region through interaction with G proteins. G protein-coupled receptor can recognized various kinds of ligands and various stimuli including hormones and neurotransmitters, chemokines, prostaglandins, proteases, biogenic amines, nucleosides, lipids, growth factors, odorants and light. These receptors can act as an intracellular mediator and further participate in regulating complex network pathways. Signaling pathways mediated by G protein-coupled include cAMP / PKA signaling pathway, Ca2 + / PKC signaling pathway, Ca2 + / NFAT signaling pathway, PLC signal pathway, PTK signaling pathway, PKC / MEK signaling pathway, p43 / p44MAPK signaling pathway, p38 MAP signaling pathway, PI3K signaling pathway, NO-cGMP signal pathway, Rho signaling pathway, NF-KappaB signaling pathway and JAK / STAT signaling pathway (Fang Y. et al., 2003).

G proteins are heterotrimers consisting of α, β, γ three subunits. When activated, G protein-coupled receptors can have interaction with their cognate G- protein. G proteins capable of activating adenylate cyclase G protein are collectively called Gs while those having inhibitory effects on this enzyme are collectively called Gi. When Gs is in its non-activated state, it appear as a iso-trimer with the α subunit binding of GDP. In this case, both the cyclase and receptor have no activity; the binding of hormone ligand to the receptor leads to a conformational change of the receptor, causing the exposure of the Gs binding sites, receptor and Gs further diffuse in the membrane and lead to the combination binding of them two; after the formation of the receptor-Gs complex, Gs [alpha] subunit undergoes conformational change, repels the GDP and binds with GTP to be activated. The α can thus be dissociated from the βγ subunit and simultaneously exposing the cyclase binding site; α subunits bind to the cyclase and activate the latter one, utilizing ATP to generate cAMP; after a certain period, the GTPase activity in the α subunit leads to the hydrolysis of GTP into GTP; subunits then restore to the initial conformation, thereby being separated from the cyclase; the activation of cyclase is then terminated. The alpha subunit re-binds to the βγ subunit complex (Fang Y. et al., 2003).

Many G protein-coupled receptor-mediated signaling pathways are controlled by hormones. These pathways are all subject to dynamic adjustment. At the receptor level, it can be adjusted through inhibiting the coupling process between with G protein and the G protein-coupled receptor, redistribution of cell surface receptors and the degradation of the receptors. During the process of regulating these processes, two kinds of protein family -GRKs (G protein-coupled receptor kinase) and inhibitory proteins play a crucial role. GRKs are a cluster of kinases related to the rapid desensitization of the G protein-coupled receptors (GPCRs). Many kinds of GPCRs such as opioid receptors, thromboxane receptor, 52 serotonin receptors and adrenergic receptor are easily subject to a rapid decline of the transducing signals during continuous stimulation from agonist. This regulation mechanism is mainly related with GRKs. GPCR is a pharmacologically important protein family. There are hundreds of drugs related to these receptors pathways including antihistamines, tranquilizers, anti-depressants and anti-hypertensive drugs (Sah VP. Et al., 2003).

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Structure Chemical Name CAS MF
Ramelteon Ramelteon 196597-26-9 C16H21NO2
Bosentan Bosentan 147536-97-8 C27H29N5O6S
Rimonabant Rimonabant 168273-06-1 C22H21Cl3N4O
Tolvaptan Tolvaptan 150683-30-0 C26H25ClN2O3
Bosentan hydrate Bosentan hydrate 157212-55-0 C27H31N5O7S
Ambrisentan Ambrisentan 177036-94-1 C22H22N2O4
Cinacalcet hydrochloride Cinacalcet hydrochloride 364782-34-3 C22H23ClF3N
Plerixafor 8HCl (AMD3100 8HCl) Plerixafor 8HCl (AMD3100 8HCl) 155148-31-5 C28H54N8
Suvorexant Suvorexant 1030377-33-3 C23H23ClN6O2
PLERIXAFOR PLERIXAFOR 110078-46-1 C28H54N8
8-[(E)-2-(3,4-dimethoxyphenyl)ethenyl]-1,3-diethyl-7-methyl-purine-2,6 -dione 8-[(E)-2-(3,4-dimethoxyphenyl)ethenyl]-1,3-diethyl-7-methyl-purine-2,6 -dione 155270-99-8 C20H24N4O4
NPS 2143 NPS 2143 284035-33-2 C24H25ClN2O2
AM 251 AM 251 183232-66-8 C22H21Cl2IN4O
Mozavaptan Mozavaptan 137975-06-5 C27H29N3O2
N1,N4-Di-2-pyridinyl-1,4-benzenedimethanamine N1,N4-Di-2-pyridinyl-1,4-benzenedimethanamine 55778-02-4 C18H18N4
Sitaxentan sodium Sitaxentan sodium 210421-74-2 C18H14ClN2NaO6S2
BML-190 BML-190 2854-32-2 C23H23ClN2O4
SB408124 SB408124 288150-92-5 C19H18F2N4O
CGS 21680A CGS 21680A 124431-80-7 C23H30ClN7O6
N-(2-METHYL-6-BENZOOXAZOLYL)-N''-1,5-NAPHTHYRIDIN-4-YL UREA N-(2-METHYL-6-BENZOOXAZOLYL)-N''-1,5-NAPHTHYRIDIN-4-YL UREA 792173-99-0 C17H13N5O2
SB 225002 SB 225002 182498-32-4 C13H10BrN3O4
SKI II SKI II 312636-16-1 C15H11ClN2OS
CP 945598 hydrochloride CP 945598 hydrochloride 686347-12-6 C25H26Cl3N7O
Zibotentan (ZD4054) Zibotentan (ZD4054) 186497-07-4 C19H16N6O4S
GW 842166X GW 842166X 666260-75-9 C18H17Cl2F3N4O2
(R)-2-((R)-6,7-diMethoxy-1-(4-(trifluoroMethyl)phenethyl)-3,4-dihydroisoquinolin-2(1H)-yl)-N-Methyl-2-phenylacetaMide (R)-2-((R)-6,7-diMethoxy-1-(4-(trifluoroMethyl)phenethyl)-3,4-dihydroisoquinolin-2(1H)-yl)-N-Methyl-2-phenylacetaMide 913358-93-7 C29H31F3N2O3
5-chloro-3-ethyl-1H-indole-2-carboxylic  acid  [2-(4-piperidin-1-yl-phenyl)-ethyl]-amide 5-chloro-3-ethyl-1H-indole-2-carboxylic acid [2-(4-piperidin-1-yl-phenyl)-ethyl]-amide 868273-06-7 C24H28ClN3O
MK 3207 hydrochloride MK 3207 hydrochloride 957116-20-0 C31H30ClF2N5O3
(R,S)-AM1241 (R,S)-AM1241 444912-48-5 C22H22IN3O3
BAF-312(SiponiMod) BAF-312(SiponiMod) 1230487-00-9 C29H35F3N2O3
Ki16198 Ki16198 355025-13-7 C24H25ClN2O5S
PF 543 PF 543 1415562-82-1 C27H31NO4S
KI16425 KI16425 355025-24-0 C23H23ClN2O5S
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