balanced cell growth quot anti angiogenic quot g protein coupled receptors

... 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 ... 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 ... complex functioning of these receptors offers a number of possibilities for allosterically regulating 2953 Class C G- protein- coupled receptors their activity using compounds acting at various sites...

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: ... Milligan G (2002) Homo -and hetero-oligomeric interactions between G protein- coupled receptors in living cells monitored by two variants of bioluminesence resonance energy transfer Hetero-oligomers...

Ngày tải lên: 16/03/2014, 22:20

... 47:221-231 28 Kim Y, Hechler B, Gao ZG, Gachet C, Jacobson KA: PEGylated dendritic unimolecular micelles as versatile carriers for ligands of G proteincoupled receptors Bioconjugate Chem 2009, 20:1888-1898 ... 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

... [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, ... of ASM growth (DNA synthesis /cell proliferation); GP – potentiation of growth stimulated by polypeptide growth factors; GS – growth stimulation ; RLXN – relaxation Coupling to Gi is suggested ... to maintain a degree of Gs -coupled receptor signaling in the face of persistent Gi -coupled receptor activation A role for Gi -coupled receptors in modulating growth in ASM is suggested by studies...

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 ... Using Autodock VINA, we dock all these ligands to the built models Fig show the best docked configurations of the ligands The best complexes mostly CHARACTERIZATION OF G PROTEIN COUPLED RECEPTORS...

Ngày tải lên: 31/10/2015, 10:39

... gynaecologic cancers Some breast cancers are responsive to estrogens for growth Estrogens directly increased the growth of breast cancer cells in culture by increasing the number of G0 /G1 cells ... thereby initiating transcription of genes that regulates the growth of breast cancer cells, i.e growth regulation by estrogen in breast cancer (GREB1) With more than 300 co-regulators identified ... localization signal (NLS), allowing ligand bound receptor dimer translocation into the nucleus resulting in transcriptional regulation of target genes Besides genomic pathway, estrogen signaling can also...

Ngày tải lên: 04/10/2015, 17:05

... 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

... initiating ATG underlined) in combination with antisense primers introducing a stop codon sequence: mGRK6-A M2: P2, 5¢-CTAGTCGC TGGAGTTCCCAGAGGAATCTTGGCG-3¢ (nucleotides 1677–1706, antisense, ... 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 ... encoding mGRK6-A, -B and -C Aliquots of the soluble fractions of infected cells containing similar amounts of recombinant mGRK6 proteins were subjected to SDS ⁄ PAGE and immunoblotting using antiserum...

Ngày tải lên: 07/03/2014, 12:20

... (1991) G protein- coupled receptors, phosphoinositide hydrolysis, and cell proliferation Cell Growth Differ 2, 359–364 43 Li S, Huang S & Peng SB (2005) Overexpression of G protein- coupled receptors ... the cell type observed Competing effects on cell cycle progression generated simultaneously by the same extracellular signal have been observed, suggesting that the final outcome of a signaling ... 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) ...

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, ... progestin- as well as estrogen-mediated signaling [30,32,33] Here we sought to establish whether GPR30 inhibits growth by affecting steroid receptor activity or through other cell signaling pathways ... NCL-ER-6F11 (Novocastra) or anti- b-actin (Sigma) Peroxidase-conjugated goat anti- rabbit IgG (Cappel, West Chester, PA, USA) for GR and peroxidase-conjugated goat anti- mouse IgG (Cappel) for PR, ER...

Ngày tải lên: 16/03/2014, 18:20

... coexpressing both receptors, even though they 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 ... 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 ... cotransfected cells is often sufficient to activate a G- protein, leaving their coupling efficacy unchanged For instance, b2-adrenergic receptors, which are coupled with stimulatory G- proteins, and...

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 ... 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 ... Ng GY, Varghese G, Akil H, Mansour A, Nguyen T & George SR (2000) Inhibition of cell surface expression by mutant receptors demonstrates that D2 dopamine receptors exist as oligomers in the cell...

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 ... Phosducin-like protein (rat, 279–301, C-terminal) EQSGYHVEQEKENKLLCEDLPGTEDFVGHQGTVPSDNIDSQGRNCSTNDSLL-OH EPAPAGPRDTDALDLEESSSSDHAERPPGPRRPERGPRGKGKARA EEKESSNDSTSVSAVASNMRDDEITQDENTVSTSLGHSKDENSK ... KSWKPSAEQMDQDHSSSDSWNNNDAAASLENSASSDEEDIGSETR KAFLHWYTGEGMDEMEFTEAESNMNDLVSEYQQYQDATADEEGEMY EDDDEESEAQGPK-OH NEEGAPQEGILEDMPVDPDNEAYEMPSEEGYQDYEPEA-OH PEEVAQEAAEEPLIEPLMEPEGESYEDPPQEEYQEYEPEA-OH EQFAEEFFAADVESFLNEYGLLPEREIHDLGQTNTEDEDIE-OH...

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¢; ... 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 ... [12–14], and some G protein- coupled receptors are known to be involved in growth regulation The regulation of GPR30 expression in MCF-7 cells was progestin specific and was not upregulated by other...

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, ... mM L-glutamine, mM penicillin-streptomycin, and 1% endothelial cell growth supplement (ECGS) (BD Biosciences, Bedford, MA) Phoenix GP retroviral packaging cells (ATCC, Manassas, VA) were grown ... 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...

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, ... mM L-glutamine, mM penicillin-streptomycin, and 1% endothelial cell growth supplement (ECGS) (BD Biosciences, Bedford, MA) Phoenix GP retroviral packaging cells (ATCC, Manassas, VA) were grown ... 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...

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

... dexamethasone; CT: computed tomography Page of Author details Shanghai Institute of Hematology, Shanghai Rui Jin Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai, China 2Inserm, U728, ... International agency for research on cancer, 2008 Ghielmini M, Zucca E: How I treat mantle cell lymphoma Blood 2009, 114:1469-1476 Zhao WL: Targeted therapy in T -cell malignancies: dysregulation of the cellular ... 109:3509-3512 10 Del Bufalo D, Ciuffreda L, Trisciuoglio D, Desideri M, Cognetti F, Zupi G, Milella M: Antiangiogenic potential of the Mammalian target of rapamycin inhibitor temsirolimus Cancer Res...

Ngày tải lên: 10/08/2014, 22:21

... bạch linh 1 0g, sinh khương 2 1g, sơn thù 6g, phòng sâm 6g, hoàng kỳ 5g, cam thảo (chích) 4g Đổ 600ml nước, sắc 200ml, chia nhiều lần cho trẻ uống ngày Chữa thương hàn, giải cảm: 20 lốt già (thái ... rễ tầm gai, đa lông, mã đề vị 1 0g Sắc với 500ml nước 150ml, uống ngày Uống sau bữa ăn trưa thuốc ấm Dùng 3-5 ngày Chữa viêm tinh hoàn: Lá lốt 1 2g, lệ chi 1 2g, bạch truật 1 2g, trần bì 1 0g, bạch ... liên tục - ngày khỏi Chữa đau nhức xương khớp: 20 gr lốt, 12 gr thiên niên kiện, 16 gr gai tầm xoang, sắc với 400 ml nước 100 ml, chia uống ngày Uống liền tuần Chữa viêm nhiễm âm đạo, ngứa, nhiều...

Ngày tải lên: 25/12/2015, 08:07

... GCGGGATCCCTGGACGGGCAGCCGATGAAG ATAAGAATGCGGCCGCTCAAAGCTTGATTTTGAATTCTGT GCGGGATCCCAGCCCATCCTGCTGCGGCTG ATAAGAATGCGGCCGCTCAAAGCTTGATTTTGAATTCTGT GCGGGATCCCAGCCCATCCTGCTGCGGCTG ATAAGAATGCGGCCGCTCAGGGCTGCGTGGTCACAGAGGC ... ATAAGAATGCGGCCGCTCAAGGCAGCTCGCTCTCCTTTTT GCGGGATCCCTCAGCCCATTGGAAGGCACC ATAAGAATGCGGCCGCTCAGCTGTCACTCAGCCGCAGCAG GCGGGATCCAACAAGGAAGAACCCCCC ATAAGAATGCGGCCGCTCAGTCTGAGGTGATAACATTCCC GCGGGATCCCTGGACGGGCAGCCGATGAAG ... GCGGGATCCCGTTTCCCAGCCTGTTGGGCCT AAACTGCAGGATGGCGGACATCTCCCTGGAC AAACTGCAGAAGCTTGATTTTGAATTCTGT AAACTGCAGGATGGCGGACATCTCCCTGGAC AAACTGCAGAAGCTTGATTTTGAATTCTGT GCGAAGCTTCACGATGCCCAAGAAGAAGCCGACGCC GCGGGATCCCGGATGCTGGCAGCGTGGGTTGG...

Ngày tải lên: 19/02/2014, 05:20