
	Where results make sense

Topic: GPCR

In the News (Tue 14 Feb 12)

EXECUTIVE POWER

Iran

ANALYSIS

Pakistan

Family compact

	GPCR activation -Bourne lab-
		We inferred that: (a) these GPCRs (and, by extension, all seven-helix GPCRs) share a common 3D structure and switch mechanism; (b) all ligands activate the switch by somehow causing a separation or shift in orientation between the cytoplasmic ends of helices III and VI.
		Tom devised a quite different approach, using a mammalian GPCR (the C5a receptor) and a human G-alpha subunit expressed in the budding yeast, S. cerevisiae.
		Based on biochemical effects of G protein mutations in inherited endocrine disorders, 3D crystal structures of G protein trimers, and suggestive biochemical experiments, the model proposed that the GPCR uses both G-betagamma and the carboxy terminus of G-alpha to open the nucleotide-binding pocket.
	www.cmpharm.ucsf.edu /bourne/lab_science/activation.html (678 words)

	The Role of Gas-Phase Chemical Reduction in the Treatment of Sydney Tar Ponds Sediment - April 3, 2003
		GPCR is a non-incineration technology that uses hydrogen to reduce the contaminants down to their basic components.
		Contaminants are conveyed to the GPCR reactor, which has a hydrogen atmosphere, and is heated to a temperature of about 875°C. The combination of heat, hydrogen and steam breaks down the contaminants into methane and hydrochloric acid.
		GPCR has three outputs: treated solids (if indeed solids are being treated), water from the scrubbing system, and stack gas from the use of methane gas as fuel.
	www.safecleanup.com /jag/gpcr/gpcr_2.htm (1955 words)

	GPCR Expression and Purification Services - GenWay
		The GPCRs are the largest protein family known, comprised of an estimated 600-1,000 members, which are involved in all types of stimulus-response pathways, from intercellular communication to physiological senses.
		The GPCR family of receptors is well-established as the premier target family for drug development: about half of the drugs on the market today are targeted towards GPCRs, generating annual sales well in excess of $40 billion.
		GPCR proteins are purified from the plasma membranes using multiple detergent screening followed by detergent selection and physical extraction of the GPCR proteins.
	www.genwaybio.com /gw_services_gpcr_expression_and_purification_services.php (346 words)

	Current Environmental Solutions Home Page
		The GPCR process passes high-voltage electrical fields through a packed bed of dielectric pellets to form non thermal plasma in the void spaces between the pellets.
		The typical GPCR device is a coaxial cylinder with an inner metal electrode, an outer tube made of quartz, and dielectric pellets filling the annular gap, as shown in Figure 2.
		The portable GPCR device is powered by a linear amplifier connected to a high-voltage transformer sized for 500 W operation at up to 1500 VA. The applied voltage (0 to 20 kV) and power frequency (600 to 1200 Hz) are adjusted using a digital waveform generator connected to the amplifier.
	www.cesiweb.com /gpcr.htm (825 words)

	Mechanisms of GPCR Signal Transduction
		The smallest GPCR family is Family C, which are receptors for small molecules such as GABA, glutamate or calcium.
		Although it is well recognised that GPCRs may couple to multiple G proteins, and thus to multiple signal transduction pathways, the full spectrum of potential interactions for an individual receptor has not been well explored.
		GPCR signaling promiscuity and trafficking of receptor stimulus
	www.med.monash.edu.au /pharmacology/research/gpcr-link.html (965 words)

	Genetic Variations in Human G Protein-Coupled Receptors: Implications for Drug Therapy
		GPCRs comprise a large class of membrane proteins that are encoded by approximately 600 human genes with broadly diverse functions.
		Whereas SMO is a member of the 7-TMD GPCR class, PTCH is an integral membrane protein with approximately 9 TMDs unrelated in sequence to the GPCRs.
		The presence of endogenous GPCR antagonists is a rare observation; yet, we have found that the opioid peptide dynorphin also serves as an endogenous antagonist, which may regulate melanocortin function under physiological conditions.
	www.aapspharmsci.org /view.asp?art=ps030322 (6781 words)

	GPCR Frequently Asked Questions : Arena Pharmaceuticals
		GPCRs — shorthand for G protein-coupled receptors — are transmembrane proteins on a cell’s surface that can interact with both the environment outside and inside the cell.
		Molecules called ligands bind to the portion of the GPCR on the outside of the cell, activating the GPCR by allowing it to bind with a G protein and setting off a series of events within the cell.
		Melanophore provides a broadly applicable, high-throughput screen for GPCRs that uses frog skin cells to visually signal when GPCRs couple with their G protein or proteins, allowing researchers to assess when a receptor has been inhibited or stimulated.
	www.arenapharm.com /wt/page/gpcr_faq (625 words)

	Gpr151 - Probable G-protein coupled receptor 151 protein
		G2A is an orphan G protein- coupled receptor (GPCR), expressed predominantly in T and B cells and homologous to a small group of GPCRs of unknown function expressed in lymphoid tissues.
		A special type of GPCR is the gonadotropin-releasing hormone (GnRH) receptor, which uses primarily the Gq protein for its downstream signaling.
		We conclude that (1) osteoblastic cell lines differentially express the enzymes and protein co-factors that modulate GPCR responsiveness and (2) expression of both GRK2 and beta-arrestins is temporally regulated during osteoblast development.
	www.pdg.cnb.uam.es /UniPub/iHOP/gg/155016.html (1816 words)

	It’s a GPCR world
		When the matching natural ligand—which for the range of GPCRs could be an amine, ion, nucleoside, lipid, peptide, protein, or, for optical receptors, light—comes along, it binds to a receptor’s active site and causes a conformational change in the protein to form its active state.
		All GPCRs are known to have a common motif of seven transmembrane helical structures, but the only GPCR crystal structure published at atomic resolution is of the inactive conformation of rhodopsin, the optical receptor protein solved in 2000 by University of Washington chemistry and ophthalmology professor Krzysztof Palczewski (3).
		Obtaining high-quantity and high-purity GPCR proteins is very challenging, because membrane proteins are typically produced in a heterogeneous manner by cells with substantial variability in glycosylation, Ballesteros explains.
	pubs.acs.org /subscribe/journals/mdd/v07/i11/html/1104feature_filmore.html (2317 words)

	Millipore accelerate drug R&D with GPCR screening service
		GPCRs are a protein family of seven transmembrane surface receptors that transduce an extra cellular signal (ligand binding) into an intracellular signal (G protein activation).
		Because of the diversity of their functions, GPCRs are an ideal target class that comprise more than 40 per cent of drug screening programs and are targets for more than 50 per cent of today's commercially available pharmaceuticals.
		An important aspect of the early drug discovery process is the design and implementation of high-throughput GPCR functional assays that allow the cost-effective screening of large compound libraries to identify novel drug candidates.
	www.drugresearcher.com /news/ng.asp?n=71304-millipore-gpcr-screening (527 words)

	United States Patent Application: 0040091863
		GPCRs (also known as 7TM receptors) have been characterized as including these seven conserved hydrophobic stretches of about 20 to 30 amino acids, connecting at least eight divergent hydrophilic loops.
		For example, compounds which activate a GPCR may be employed for therapeutic purposes, such as the treatment of asthma, Parkinson's disease, acute heart failure, urinary retention, and osteoporosis.
		Compounds which inhibit GPCRs also are useful in reversing endogenous anorexia, in the control of bulimia, and in treating various cardiovascular ailments such as caused by excessive pulmonary blood flow or hypotension.
	appft1.uspto.gov /netacgi/nph-Parser?Sect1=PTO1&Sect2=HITOFF&d=PG01&p=1&u=/netahtml/PTO/srchnum.html&r=1&f=G&l=50&s1="20040091863".PGNR.&OS=DN/20040091863&RS=DN/20040091863 (17363 words)

	BioCarta - Charting Pathways of Life
		One method to attenuate GPCR signaling is by removal of the stimulus from the extracellular fluid.
		GRKs attenuate GPCR signaling in concert with arrestins, proteins that bind GRK-phosphorylated GPCRs to disrupt interaction with G-protein and to terminate signaling.
		Endocytosis of activated GPCRs appears to be stimulated by GRKs and arrestins.
	www.biocarta.com /pathfiles/h_agpcrPathway.asp (368 words)

	BioMed Central \| Full text \| Evolution of secretin family GPCR members in the metazoa
		The putative invertebrate receptors identified share the general characteristics of family 2 GPCR members with the presence of conserved cysteine residues [27,28] and several highly conserved amino acids and protein motifs at the N-terminal domain which is involved in ligand binding [22].
		Family 2 GPCR members have been identified in the majority of vertebrate genomes [17,20] and searches carried out on the amphibian and chicken genomes identified an equivalent number of gene family members (data not shown) to that found in the human genome.
		The evolution of family 2 GPCR receptor genes in protostomes and deuterostomes is probably the result of a combination of species-specific gene duplications and gene or genome duplication events in ancestral gene precursors (Figure 6).
	www.biomedcentral.com /1471-2148/6/108 (5822 words)

	Open Biosystems: Clone Resources - BioTrack™ Collections - BioTrack^TM Collection - GPCR (Site not responding. Last check: 2007-10-26)
		G protein-coupled receptors (GPCRs) belong to one of the largest super family of proteins, often playing a remarkable role in a large number of physiological conditions of a cell.
		GPCRs consist of a chain of transmembrane helices.
		Thus, GPCRs are pharmacologically important proteins that are encoded by hundreds of genes.
	www.openbiosystems.com /biotrack_collection_gpcr.php (397 words)

	Tutorial : Casting a New Light on GPCR Targets Genetic Engineering News - Biotechnology from Bench to Business
		GPCRs are transmembrane receptors coupled to an internal cell machinery just underneath the cell membrane, thus carrying extracellular signals to the cytoplasm.
		GPCR activation operates mainly through two major pathways (depending on which particular species of G-protein is involved).
		About 50% of all GPCRs work through this pathway, so it is essential to find a suitable assay to detect their activation.
	www.genengnews.com /articles/chtitem.aspx?tid=1082 (1508 words)

	GPCR SARfari - Inpharmatica (Site not responding. Last check: 2007-10-26)
		The GPCR family of receptors is well established as the premier target family for drug development: over 40% of the drugs on the market today are targeted towards GPCRs, generating annual sales well in excess of $40 billion.
		GPCR SARfari has been designed to provide one essential data resource for GPCR pharmaceutical research: from protein sequence and 3D structure through to corresponding natural ligand and focused compound information, this fully searchable, easy to use, web accessible resource will considerably enhance in-house knowledge to further GPCR Drug Discovery programmes.
		GPCR SARfari is available by subscription either as a stand alone product or as part of a collaborative programme.
	www.inpharmatica.com /gpcr (229 words)

	GPCR Ligands - ActiTarg-G Library - Screening Compounds, bulding blocks, targeted libraries
		The ActiTarg-G Collection is a pre-plated screening set of molecules that contain chemical lattices present in compounds reported in the technical or patent literature to possess GPCR-ligand properties.
		The potential for this super family of receptors to reveal small molecule modulators of a significant biological function has been responsible the focus of intense drug discovery efforts.
		Compounds with structural features and molecular lattices that are present in a large number molecules described in both the patent and technical literature that possess GPCR activity have been identified, and assembled as indicated below.
	www.timtec.net /actitarg-g-gpcr-ligands.html (257 words)

	CMT : GPCR PROFILING
		Ligand binding to GPCRs triggers desensitization, a process mediated by the recruitment of intracellular arrestin proteins to the activated receptor.
		As a result, the ligand-induced activation of GPCRs may be assayed by monitoring the interaction of arrestin with the test GPCR.
		The target GPCR is fused at its intracellular C-terminus to an exogenous transcription factor.
	www.cmt-inc.net /p_gpcrprofiling.html (643 words)

	New tools: GPCR Research Reagents
		G protein-coupled receptors (GPCR) are so named because of their regulation of an intracellular heterotrimeric complex made up of Ga, and Gbg subunits.
		GPCRs make up the largest family of integral membrane proteins and account for approximately 5% of all genes found in the human genome.
		R, is a GPCR with homology to the formyl peptide receptor (FPR1) and is activated by formyl-methionyl-leucyl-phenylalanine (fMLP).
	www.rndsystems.com /cb_detail_objectname_SP06_NT_gpcr.aspx (283 words)

	A generalised fit more beneficial to drug design
		When a hormone binds to its designated GPCR on the outside of a cell, a specific G-protein is activated within the cell, initiating a cascade of biochemical events leading to the appropriate cellular response to that hormone.
		Ã¢â¬Å“GPCRs are the targets of roughly a third of medicines sold today, so if this finding for TRH holds for other GPCR targets, it could have significant implications for drug development,Ã¢â¬Â said Marvin Gershengorn, director of NIDDKÃ¢â¬â¢s Division of Intramural Research and senior author of the paper.
		As to why this would be the case, the researchers suggest that a loose connection between hormone and GPCR may allow a hormone to repetitively dock to and undock from its associated GPCR, activating a succession of G-proteins, and firing signal after signal.
	www.drugresearcher.com /news/ng.asp?n=67696-gpcr-trh-zantac (678 words)

	Transfluor Technology GPCR Assays
		Transfluor is an advanced, cell-based screening technology applicable to all known and orphan GPCRs.
		In contrast to current methods of screening GPCRs, the Transfluor technology is based on the mechanism for termination of GPCR signaling, known as receptor desensitization.
		A proprietary technique to assist in validating orphan GPCR screens, called LITe™ (Ligand Independent Translocation), is an agonist-independent assay used to verify the translocation of ß arrestin-GFP in orphan GPCRs.
	www.moleculardevices.com /pages/reagents/transfluor_gpcr.html (196 words)

	Sex and sugar in yeast: two distinct GPCR systems
		Although eukaryotic G-protein coupled receptor (GPCR) systems are well known for their ability to detect and mediate rapid responses to extracellular signals, the full range of stimuli to which they respond may not yet have been identified.
		The importance of GPCR systems is illustrated by the fact that 30% of all clinically prescribed drugs function as GPCR agonists or antagonists (Stadel et al., 1997).
		If nutrient sensing GPCR systems are a wide-spread phenomenon in eukaryotes, in particular if the GPCRs also act on pivotal effectors like adenylate cyclase, it might have a dramatic impact on the field of signal transduction in that it would add a novel layer of regulation.
	www.nature.com /cgi-taf/DynaPage.taf?file=/embor/journal/v2/n7/full/embor385.html (4231 words)

	TACE cleavage of proamphiregulin regulates GPCR-induced proliferation and motility of cancer cells -- Gschwind et al. ... (Site not responding. Last check: 2007-10-26)
		GPCR agonists stimulate proteolytic cleavage and release of AR
		GPCR stimulation results in metalloprotease-dependent cleavage and release of AR at the cell surface.
		cleaved in response to physiologically abundant GPCR ligands.
	embojournal.npgjournals.com /cgi/content/full/22/10/2411 (6036 words)

	Welcome to Jubilant Biosys ...
		G Protein-Coupled Receptor (GPCR) family emerged as prominent drug targets within pharmaceutical research, since approximately 60% of marketed prescription drugs act by selectively addressing representatives of that class of transmembrane signal transduction systems.
		The database is the integrated chemical and biological information of known GPCR agonists and antagonists from Patents and Journal articles.
		Covers 200 GPCR Targets, which includes 3 classes (A,B,C) The GPCR ligand centric database integrates structure and bioactivity data in a user-friendly format.
	www.jubilantbiosys.com /gpcr.htm (149 words)

	Weill Cornell Research
		Inferences from these bioinformatics tools are used to construct first-generation molecular models of GPCR dimers, which in turn can serve to generate valuable hypotheses of interaction that can be tested experimentally, and help refine the proposed dimeric/oligomeric models.
		The correct nature and geometry of the interface(s) of GPCR homo- and heteromers is essential for understanding of the role and implications of these phenomena in the functional mechanisms of these receptors.
		To provide new and deeper insights into the basis of protein-protein interaction in GPCR dimers/oligomers, and the dynamic properties that may relate to their functional mechanisms, we are currently carrying out detailed MD simulations of the interfaces of activated and inactive GPCR dimers using discrete representations of the membrane and water environment.
	www.med.cornell.edu /research/mafilizola (395 words)

	Analysis of GPCR Signaling Events Using HCS Technology - 040701162044
		Upon GPCR stimulation the β-arrestin translocates from the cytosol to the GPCR at the plasma membrane and promotes the desensitization and internalization of the GPCR into coated pits and endosomal vesicles.
		The GPCR software module measures β-arrestin translocation which is used to measure GPCR activation.
		Samples were all acquired and analyzed using Discovery-1 software with the new GPCR software module.
	www.sbsonline.org /sbscon/2004/posters/040701162044.htm (198 words)

Try your search on: Qwika (all wikis)