seven transmembrane g protein coupled receptors gpcrs

... Class C G- protein- coupled receptors ligand binding This led to the demonstration that most GPCRs can oligomerize as shown by both biochemical and energy transfer technologies [3] In recent ... intracellular loops of class C GPCRs as well as the C-terminal tail are involved in G- protein coupling For various class C GPCRs, including the mGlu5, GABAB2 and CaS receptors, the HD can fold correctly ... occurs in the GABAB receptor, GABA binding in the GABAB1 VFT leading to activation of the GABAB2 HD Although GABAB1 VFT binds the agonist and the GABAB2 HD couples to G- protein, a chimeric construct...

Ngày tải lên: 07/03/2014, 21:20

... very high GPCR-GFP ⁄ GPCR-Rluc ratios (B) BRET2 measurements performed in cells expressing increasing concentrations of GPCR– Rluc and GPCR–GFP2 while maintaining a constant GPCR–GFP2 : GPCR–Rluc ... O’Dowd BF & Lee SP (2002) G- proteincoupled receptor oligomerization and its potential for drug discovery Nature Rev Drug Discovery 1, 808–820 12 Milligan G (2004) G protein- coupled receptor dimerization: ... in ‘single point’ assays In these, single amounts of Renilla luciferase and fluorescent protein- tagged forms of a single GPCR, to study homodimerization ⁄ oligomerization, or pairs of GPCRs, to...

Ngày tải lên: 16/03/2014, 22:20

... KA: Functionalized congener approach to the design of ligands for G protein- coupled receptors (GPCRs) Bioconjugate Chem 2009, 20:1816-1835 10 Kim Y, Hechler B, Klutz AM, Gachet C, Jacobson KA: ... Toward multivalent signaling across G protein- coupled receptors from poly(amidoamine) dendrimers Bioconjugate Chem 2008, 19:406-411 11 Klutz KM, Gao ZG, Lloyd J, Shainberg A, Jacobson KA: Enhanced ... Multivalent effect in G protein- coupled receptor recognition Bioconjugate Chem 2009, 20:1650-1659 13 Jacobson KA, Gao Z -G: Adenosine receptors as therapeutic targets Nature Rev Drug Discovery 2006,...

Ngày tải lên: 11/08/2014, 00:22

... and actin polymerization [40] strongly suggest a physiologic role for G1 2/13 signaling in ASM Regulation of GPCR signaling Signaling by GPCRs is a highly regulated process One critical way in ... [39,226–231] Gs Gq RLXN, Cyt, GI CXN CLT1R ET-A/B EDG 1–7 EP2 H1 histamine IP Prostacyclin [232–236] [237–242] [38,243–245] [20,246,247] [248,249] [41,250] Gq Gq Gq, Gi, G1 2/13 Gs Gq Gs CXN, GP CXN, GP GS, ... recently discovered RGS (regulators of G protein signaling) proteins [107] Experimental manipulation of RGS protein expression can alter GPCR signaling, but the physiologic role of RGS proteins is unclear...

Ngày tải lên: 13/08/2014, 13:20

... modeling of GPCRs at different activation states, and docking odorant ligands II WEB-BASED SERVER FOR AUTOMATICALLY HOMOLOGY MODELING AND LIGAND DOCKING Homology modeling is process consisting of ... choice for identifying and aligning templates for homology modeling [14] These 44 TP DUY, A GIORGETTI, NHH CHUONG, P CARLONI, H ZUNG methods are used by many of the best protein structure prediction ... of GPCRs through the use of bioand chemo- informatics tools The server will play the role for doing homology modeling massively for the unknown 3D GPCRs based on the experimentally known 3D GPCRs...

Ngày tải lên: 31/10/2015, 10:39

... following primers: M2-goa1-s, 5¢-CATTATAAGA ACATAGGCGCTACAAGGATGGGTTGTACCATGTC ACAGGAAG-3¢; M2-goa1-PstI-as, 5¢-CCAATGCATTGG TTCTGCAGTTAATACAAGCCGCATCCACGAAGA-3¢ (An engineered PstI recognition ... conditions Human GPCR activates nematode G protein construct, pPAK-M2–Gai1 [25], as a template with the following primers: M2-myc-EcoRI-s, 5¢-CAGAATTCatg gagcagaagctgatctccgaggaggacctgctgGTGAACAACTCCAC ... 1986 [23] Although Gb and Gc are essential for Ga activation by GPCR [10], GPCR can activate Ga without Gb and Gc in some GPCR::Ga fusion proteins [24] Muscarinic-agonist-dependent Ga activation...

Ngày tải lên: 07/03/2014, 11:20

... (nucleotides 1–26, sense, initiating ATG underlined) in combination with antisense primers introducing a stop codon sequence: mGRK6-A M2: P2, 5¢-CTAGTCGC TGGAGTTCCCAGAGGAATCTTGGCG-3¢ (nucleotides 1677–1706, ... P2, 5¢-ACTGTCGCTGGAGTTCCCAGAGGAATCTTGG CG-3¢ (nucleotides 1677–1709, antisense) Complementary DNAs encoding the C-terminal mGRK6-A mutants M2 and M3 were prepared either from the mGRK6-A mutant ... (Stratagene, La Jolla, CA) (18 cycles: 94 °C for min, 55 °C for min, 72 °C for min, followed by a single incubation at 72 °C for 10 min) using primer P1, 5¢-CGCCA AGATTCCTCTGGGAACTCCAGCGACAGT-3¢...

Ngày tải lên: 07/03/2014, 12:20

... 35, 231–235 Regulation of Akt signaling pathways by GPCRs New DC & Wong YH (2007) Molecular mechanisms mediating the G protein- coupled regulation of cell cycle progression J Mol Signal 2, Stambolic ... either through matrix metalloproteinases (Gi ⁄ o-, Gq-, and Gs -coupled receptors) or through Rho ⁄ Rho-associated kinase (Rock)-mediated expression of RTK ligands (G1 2 ⁄ 13 -coupled receptors) ... activation G1 2 ⁄ 13-, Gi ⁄ o-, Gq-, and Gs -coupled receptors are all known to activate the phosphoinositide 3-kinase (PI3K) ⁄ Akt pathway through either Ga or Gbc subunits Gaq and Gas subunits...

Ngày tải lên: 16/03/2014, 05:20

... following primers were used for cloning at the pLEGFP-N1 vector: GPR30-forward 5¢-TAATAAGTCGACGGGTC TCTTCCT-3¢ and GPR30-reverse 5¢-ATTATTGGATC CTACACGGCACTGC-3¢ Viruses capable of introducing pLEGFP-N1, ... primer 5¢-ATCTCCAAGGCAA GATCA-3¢ and reverse primer 5¢-GTGCCATCAGA CAAGGAA-3¢ were used Primer pair resulted in a PCR product of 216 bp Additionally, forward primer 5¢-GAGCCCCAAGAAGAAAGA-3¢ and reverse ... glucocorticoid The role of GPR in glucocorticoid-mediated signaling was suggested by Schmidt and coworkers [12] b2-adrenergic receptors were able to modulate GR transactivation by stimulating...

Ngày tải lên: 16/03/2014, 18:20

... activate a G- protein, leaving their coupling efficacy unchanged For instance, b2-adrenergic receptors, which are coupled with stimulatory G- proteins, and d-opioid and j-opioid receptors, which are coupled ... may form hetero-oligomers [5] The same phenomenon has been shown to occur in hetero-oligomers formed by Gi -coupled and Gq -coupled receptors [6] and by Gs -coupled and Gq -coupled receptors [7] One ... of hetero-oligomers A B H GPCR GPCR H GPCR H H β-arrestin H GPCR H H GPCR GPCR H GPCR GPCR β-arrestin No effect No effect H GPCR H GPCR H GPCR β-arrestin β-arrestin H GPCR β-arrestin ERK activation...

Ngày tải lên: 16/03/2014, 22:20

... Vriend G (2003) Sequence analysis reveals how G protein- coupled receptors transduce the signal to the G protein Proteins 52, 553–560 Madabushi S, Gross AK, Philippi A, Meng EC, Wensel TG & Lichtarge ... Dimerization of G- protein- coupled receptors J Med Chem 44, 4595–4614 Moller S, Vilo J & Croning MD (2001) Prediction of the coupling specificity of G protein coupled receptors to their G proteins Bioinformatics ... structure of G- protein- coupled receptors J Med Chem 40, 3871–3886 Gouldson PR, Snell CR, Bywater RP, Higgs C & Reynolds CA (1998) Domain swapping in G- protein coupled receptor dimers Prot Eng 11, 1181–1193...

Ngày tải lên: 16/03/2014, 22:20

... venom, mimics receptors by activating GTP-binding regulatory proteins (G proteins) J Biol Chem 263, 6491–6494 19 Haga, K., Ogawa, H., Haga, T & Murofushi, H (1998) GTPbinding -protein- coupled receptor ... EQSGYHVEQEKENKLLCEDLPGTEDFVGHQGTVPSDNIDSQGRNCSTNDSLL-OH EPAPAGPRDTDALDLEESSSSDHAERPPGPRRPERGPRGKGKARA EEKESSNDSTSVSAVASNMRDDEITQDENTVSTSLGHSKDENSK KSWKPSAEQMDQDHSSSDSWNNNDAAASLENSASSDEEDIGSETR ... suggested to mediate the internalization of b-adrenergic receptors [45] The GRK-mediated phosphorylation of tubulin may affect physiological processes including GPCRs, and the interaction of GRK2...

Ngày tải lên: 17/03/2014, 09:20

... following primers (Amersham Pharmacia Biotech) were used for PCR: GPR30-forward, 5¢-AGTCGG ATGTGAGGTTCAG-3¢; GPR30-reverse, 5¢-TCTGTGT GAGGAGTGCAAG-3¢; TBP-forward, 5¢-TTTGGAAG AGCAACAAAGG-3¢; ... correlated with growth inhibition The potential importance of the G- proteins in progestin-mediated signaling is also highlighted by a study showing that half of the progesteroneregulated genes were ... AGCAACAAAGG-3¢; TBP-reverse, 5¢-AAGGGTGCAG TTGTGAGAG-3¢ TBP was used to normalize the RNA samples These primer pairs result in PCR products of 240 bp (GPR30) and 243 bp (TBP) LightCycler data were quantitatively...

Ngày tải lên: 24/03/2014, 00:21

... and EcoRI digested pcDNA3 (Invitrogen) using T4 DNA Ligase (Invitrogen) pBABE-GFP and pBABE-GFP-vGPCR were propagated in Escherichia coli strain STBL2 (Invitrogen), whereas pcDNA3-vGPCR, pcDNA3, ... Baltimore, MD) by BglII and EcoRI digestion [12] The digested vGPCR fragment was separated by gel electrophoresis, purified using QIAquick PCR Purification Kit (Qiagen, Page of (page number not for ... KSHV G- protein- coupled receptor (vGPCR) is a constitutively active lytic phase protein with significant homology to the human interleukin-8 (IL-8) receptor and has angiogenic and tumorigenic...

Ngày tải lên: 18/06/2014, 18:20

... and EcoRI digested pcDNA3 (Invitrogen) using T4 DNA Ligase (Invitrogen) pBABE-GFP and pBABE-GFP-vGPCR were propagated in Escherichia coli strain STBL2 (Invitrogen), whereas pcDNA3-vGPCR, pcDNA3, ... Baltimore, MD) by BglII and EcoRI digestion [12] The digested vGPCR fragment was separated by gel electrophoresis, purified using QIAquick PCR Purification Kit (Qiagen, Page of (page number not for ... KSHV G- protein- coupled receptor (vGPCR) is a constitutively active lytic phase protein with significant homology to the human interleukin-8 (IL-8) receptor and has angiogenic and tumorigenic...

Ngày tải lên: 20/06/2014, 01:20

... TPIAESIAVYVFGALIYASKIPERWYPGCFDYFGGSHNLWHLAVLGGIVFHYIAMQE GLSASGFLPIFQIWLTRGGMSVWEHY SPILESLFVYFLGALVYASKVPERWCPGMFDYVGGSHNLWHMAVLGGILFHYNAMQE GLGASLFLPLAHGLSVLGWKRLDAAMGLESFLGLAAINFSGSAVYAMRIPERWFPGTFDLIGQSHNWMHVLVLTGALVRLNGLIR ... EFSFWGQIYGYLSAILYLGSRLPQLLLNFRRKSTEGVSMLFFLFACLGNLTYVLSILAYDGS -SECAAGPGDCEDGEPGQ -EFNILGQVFGWLCAVLYLGSRVPQILLNYRRKSTEGVSMLFFLFACLGNLTYVLSIFAFEPRCRDKHSGIGPHAGGCVGGEAGR SQEPQAVIGMILGYFSAVCYLCARIPQIIKNYREKSCEGLALLFFLLSLTGNLTYGASVIAY ... GLGASLFLPLAHGLSVLGWKRLDAAMGLESFLGLAAINFSGSAVYAMRIPERWFPGTFDLIGQSHNWMHVLVLTGALVRLNGLIR GLGLSGVVPTMHFTIAEGFVKATTVGQMGWFFLMAVMYITGAGLYAARIPERFFPGKFDIWFQSHQIFHVLVVAAAFVHFYGVSN GLGLSGVVPVVHAVGEDGFAALDERMGLKWVMLQGAMYIFGAFIYAARWPERSFPGKFDIWCSSHQIFHIFVLLAAASHLYGMIK...

Ngày tải lên: 14/08/2014, 14:21

... At 3g0 1550 At 1g2 1460* At 3g2 8007* At 5g1 3170* At 2g0 1070 At 5g3 7310 At 1g1 6560 At 3g0 6470 At 1g4 8270 (GCR1) At 5g3 8380 At 3g2 2942 (AGG2) At 2g3 1440 At 2g4 7115 At 3g0 4970 At 5g4 2090 At 1g1 1200 At 3g6 3420 (AGG1) ... Biology 2006, 7:R96 * At 1g1 4530 At 1g1 0660 At 2g0 2180 At 1g5 7680 At 4g3 6830 At 4g0 2690 At 4g2 5010* At 5g5 0800* At 5g6 2960 At 2g4 1610 At 2g3 5710a At 2g3 5710b At 2g1 6970 At 3g1 6690* At 3g4 8740* At 5g2 3660* At 1g4 9470 ... At 3g6 3420 (AGG1) At 4g3 4440 (AGB1) At 5g6 2130 At 1g6 3110 At 4g2 1790 At 3g0 9570 At 3g5 9090 At 1g7 7220 At 3g1 9260 At 4g2 0310 At 5g2 7210 At 2g2 6300 (GPA1) At 3g2 6090 (RGS1) At 3g6 3310 At 5g1 9870 At 1g7 1960 Color scale...

Ngày tải lên: 14/08/2014, 17:22

... stimulation (followed by aggregation) of platelets by ADP and thrombin, implicating this adaptor in signalling pathways of the relevant G- protein coupled receptors [130] Platelet aggregation induced by ... Furthermore, Gab2 (constitutively associating with Gads ⁄ Grb2) is recruited to membrane rafts by LAT upon TCR ligation Gab2 may inhibit signalling by competing with SLP-76 for Gads ⁄ Grb2 binding and ... of important signalling molecules, membrane rafts have been implicated in signalling through a wide range of receptors, including immunoreceptors, and also in many other biologically important...

Ngày tải lên: 18/02/2014, 04:20

... muRGS1 5¢-TCTGCTAGCCCAAAGGATTC-3¢ (sense), 5¢TTCACGTCCATTCCAAAAGTC-3¢ (anti-sense); muRGS2 5¢-GAGAAAATGAAGCGGACACTCT-3¢ (sense), 5¢-TTG CCAGTTTTGGGCTTC-3¢ (antisense); muHPRT as housekeeping gene ... control A Stimulation h Gene Control relative fluorescence LPS relative fluorescence (fold) RGS1 RGS2 RGS3 RGS4a RGS5 RGS6a RGS7a RGS9a RGS10 RGS11a RGS14 RGS16 RGS17a RGS18 RGS19 RGS20a 168 1532 153 ... dominant-negative Gai protein constructs [11] G proteins are located downstream of G- protein- coupled receptors (GPCR) [12] GPCR represent a large family of cell-surface proteins mediating the effects...

Ngày tải lên: 18/02/2014, 13:20

... by G protein- gated inwardly rectifying potassium (GIRK) channels Pflugers Arch 456, 1097– 1108 Stringer BK, Cooper AG & Shepard SB (2001) Overexpression of the G- protein inwardly rectifying potassium ... signalling molecules) GIRK1, GIRK4, Gb ⁄ c, PKA, PP2A and protein phosphatase was identified to exist in rat atrial membranes in situ [21], supporting the physiological relevance of this regulation ... heterooligomeric combinations, including not only GIRK1 ⁄ GIRK4, but also the homooligomeric GIRK1 subunit alone, have been identified to be under PKA regulation [18] In addition, the GIRK1 protein...

Ngày tải lên: 07/03/2014, 00:20