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Topic: 7TM receptor

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	Methods related to a single nucleotide polymorphism of the g protein coupled receptor, gpr40 patent invention (Site not responding. Last check: 2007-11-05)
		[0006] The G-protein coupled receptors (GPCRs) are a superfamily of membrane proteins characterized by the presence of seven transmembrane.alpha.-helix segments (designated TM1 to TM7) connecting alternating intracellular and extracellular loops.
		In a further preferred embodiment, the methods further comprise comparing the competitive inhibition of binding by said compound of said first receptor and said second receptor.
		In a preferred embodiment, the amino acid number 211 of said second receptor is arginine.
	www.freshpatents.com /Methods-related-to-a-single-nucleotide-polymorphism-of-the-g-protein-coupled-receptor-gpr40-dt20060105ptan20060003344.php (3460 words)

	Targeted Deletion of the Epididymal Receptor HE6 Results in Fluid Dysregulation and Male Infertility -- Davies et al. ... (Site not responding. Last check: 2007-11-05)
		the unveiling of the receptor ligand, as is the case with the
		Signal transduction in the ductuli efferentes testis of the rat: inhibition of fluid reabsorption by cyclic adenosine 3',5' monophosphate.
		HE6, a two-subunit heptahelical receptor associated with apical membranes of efferent and epididymal duct epithelia.
	mcb.asm.org /cgi/content/full/24/19/8642 (4896 words)

	GPCRPE home
		The mechanisms by which 7TM receptors are targeted to caveolae are not yet known, but agents that disrupt caveolae prevent internalization of the ET endothelin receptors and VIP receptors.
		The beta-arrestin-2 translocates more readily to this receptor than does beta-arrestin-1, and the association of either beta-arrestin with receptor is more transient, ending shortly after the receptor is internalized at or near the cell surface.
		In the case of the slowly recycling receptors, such as the V2 vasopressin receptor, both beta-arrestin-1 and beta-arrestin-2 translocate to the receptors, and the receptors and beta-arrestins remain associated for much longer (up to 4h) in large endosomes before the receptors are finally recycled.
	nlp.postech.ac.kr /Research/POSBIOTM/content/internal.html (979 words)

	A Library of 7TM Receptor C-terminal Tails: INTERACTIONS WITH THE PROPOSED POST-ENDOCYTIC SORTING PROTEINS ERM-BINDING ...
		and the tachykinin NK receptor, the ligand dissociates in the
		The relative binding of receptor tails to sorting proteins in GST pull-down experiments are shown as the mean and mean ± S.E. Band intensities were normalized to the band intensity of a reference lane so that 100% binding corresponded to the retention of all of the added radioactive sorting protein (see Fig.
		the OT receptor; the AT receptor; the DOP receptor; PAR1 and
	www.jbc.org /cgi/content/full/279/52/54291 (7237 words)

	NK1 Receptor Fused to beta -Arrestin Displays a Single-Component, High-Affinity Molecular Phenotype -- Martini et al. ... (Site not responding. Last check: 2007-11-05)
		The receptors were expressed transiently in COS-7 cells, and the binding experiments were performed in whole cells in duplicates as described in the text.
		One of the basic tenets of 7TM receptors is that high-affinity agonist binding is dependent on G protein interaction.
		Hastrup H and Schwartz TW (1996) Septide and neurokinin A are high-affinity ligands on the NK-1 receptor: evidence from homologous versus heterologous binding analysis.
	molpharm.aspetjournals.org /cgi/content/full/62/1/30 (5330 words)

	Company Profile: 7TM PHARMA A/S (Site not responding. Last check: 2007-11-05)
		7TM Pharma A/S is a privately held company, incorporated in 2000 as spin out from University of Copenhagen by internationally recognized pioneers in 7TM receptor research, Professor Thue W. Schwartz and Dr. Christian E. Elling alongside with industry-experienced Mette Kirstine Agger (CEO) and Peter Moldt.
		Highly validated 7TM receptor targets are selected for the generation of new drugs, combining fast-to-clinic peptide projects and classical small molecule projects with a primary focus on metablic disorders.
		A cornerstone in 7TM Pharma’s rapid pipeline growth is an in-house group focusing on the selection of new targets and their maturation into full drug discovery projects.
	mediconvalley.dimachosting.net /profiles/9 (559 words)

	7TM Pharma A/S closes USD 15 million Series-A funding (Index Ventures) - Pressi.com (Site not responding. Last check: 2007-11-05)
		7TM receptors, which also are referred to as G-Protein Coupled Receptors (GPCRs) are the prime targets for many pharmaceutical companies and close to 70% of all drugs sold today target this protein class.
		While many 7TM receptors have proven to be "refractory" to lead isolation using traditional screening methods, the Company's proprietary platform should enable the isolation of high affinity leads to all 7TM receptors, even those that have proven "refractory" to traditional approaches.
		7TM receptors are membrane receptors whose stimulation or inhibition regulates very important molecular pathways involved in the development of many common diseases.
	www.pressi.com /ch/release/37606.html (821 words)

	GPCRDB fragments (Site not responding. Last check: 2007-11-05)
		Q8HXM5_CRORS (395 AA) Alpha adrenergic receptor 2B (Fragment).
		Q9GL13_MACRU (379 AA) Alpha adrenergic receptor 2B (Fragment).
		O73641_FUGRU (156 AA) Metabotropic glutamate receptor 1 homologue (Fragment).
	www.gpcr.org /7tm/seq/fragments/DRfrag.html (2434 words)

	7tm Pharma
		Thus, TM30339 mimics a natural satiety signal from the gastrointestinal tract involved in the regulation of food intake in man. In pre-clinical studies in obese mice, the Y4 receptor selective TM30339 was highly efficacious with respect to long term body weight reduction.
		7TM Pharma is a discovery and development biopharmaceutical company which focuses on new pharmaceutical drugs targeting 7TM receptors – a large group of highly valuable drug targets with ample room for exploitation.
		The core therapeutic focus of 7TM Pharma is metabolic disorders, including obesity, an area of obvious unmet medical need and increasing prevalence globally.
	www.7tm.com /news/press_releases/7tm_pharma_advances_the_next_first-in-class_obesity_compound_into_clinical_development.aspx (544 words)

	[Full text] The GAPs, GEFs, and GDIs of heterotrimeric G-protein alpha subunits (Site not responding. Last check: 2007-11-05)
		Ligand-occupied, 7TM cell-surface receptors stimulate signal onset by acting as guanine nucleotide exchange factors (GEFs) for Gα subunits, facilitating GDP release, subsequent binding of GTP, and release of the Gβγ dimer.
		Although the GoLoco motif was first discovered in the context of 7TM receptor signaling, a central role is emerging for GoLoco motif-containing proteins in an unexpected arena: the control of mitotic spindle organization, microtubule (MT) dynamics, and the act of chromosomal segregation during cell division.
		The GEF activity of rat Ric-8A was found to have characteristics distinct from those of 7TM receptors; specifically, Ric-8A appears to interact preferentially with isolated Gα·GDP subunits to accelerate the release of GDP by Gα, the rate limiting step in the G-protein cycle [135].
	www.biolsci.org /v01p0051.htm (9955 words)

	Rhodopsin (Site not responding. Last check: 2007-11-05)
		Rhodopsin belongs to the class of G-protein coupled receptors, and consists of two building blocks, an opsin protein called scotopsin and a reversibly covalently bound cofactor; the protein opsin which is linked to 11-cis retinal a prosthetic group while retinal (retinaldehyde) is the light absorbing pigment molecule.
		Rhodopsin opsin is a member of the 7TM receptor family.
		The eyes' detection of color is a function of the three types of cone cells present within the retina covering the visible spectrum because each type is sensitive to a different range of wavelengths with maximums corresponding to red, the longer, green, the medium, or blue, the short among them.
	www.vitaminsdiary.com /rhodopsin.htm (692 words)

	CHI's Molecular Med Monthly Articles (Site not responding. Last check: 2007-11-05)
		In this article, Peter Moldt, Senior Executive Vice President, Research and Development at 7TM Pharma, discusses his company’s approach to understanding of the structure and function of 7TM, or G protein-coupled receptors, as well as the molecular mechanism of action of ligands on these receptors.
		7TM Pharma’s unique approach to drug discovery is based on an unparalleled understanding of the structure and function of 7TM receptors, as well as the molecular mechanism of action of ligands on these receptors.
		7TM Pharma is combining a number of different tools in conducting structural analyses of the binding pockets of receptor targets of interest, in order to identify key elements necessary to form anchor points for small molecule binding.
	www.healthtech.com /newsarticles/issue32_2.asp (938 words)

	High Constitutive Signaling of the Ghrelin Receptor--Identification of a Potent Inverse Agonist -- Holst et al. 17 ...
		The position in the extracellular loop 2 of an unusually long insertion of 39 amino acids in the motilin receptor, which is not found in the ghrelin receptor, is shown by an arrow.
		A, Gene-dosing experiments with the ghrelin receptor in transiently transfected COS-7 cells: basal constitutive activity (full square), constitutive activity after incubation for 30 min with adenosine deaminase (ADA) (open square) compared with the ghrelin agonist-stimulated activity (full triangle) and the activity in cells transfected with the empty vector pcDNA3 (full circles).
		of an inverse agonist for the ghrelin receptor as an antiobesity
	mend.endojournals.org /cgi/content/full/17/11/2201 (5777 words)

	SIDEROVSKI LAB @ UNC-Chapel Hill - WELCOME PAGE
		2); this PDZ domain is capable of binding peptides derived from the C‑termini of 7TM receptors, including from one of the interleukin-8 receptors (CXCR2) [56, 57].
		An obvious molecular mechanism for engendering such receptor selectivity would be direct interaction between a 7TM receptor and an RGS protein.
		It must be emphasized that no report has yet demonstrated interaction between a full-length 7TM receptor and a full-length RGS protein in cells.
	www.unc.edu /~dsiderov/page3.htm (971 words)

	Select Conferences \| Screening Europe 2007 \| Agenda
		A series of examples will be given clearly demonstrating that it is not advisable to rely on single assay technologies but rather on a repertoire of assays covering both G protein-dependent and –independent signals.
		The use of this assay compared to other assays will be discussed and examples from several screening campaigns described.
		Using a new cellular detection system we have developed a novel sensitive homogeneous assay which enables us to investigate the effect of antibodyreceptor complexes and facilitate selection of therapeutic antibody candidates.
	www.selectbiosciences.com /conferences/ScreeningEurope2007/Agenda.aspx (1817 words)

	Positive Allosteric Modulators for gamma -Aminobutyric AcidB Receptors Open New Routes for the Development of Drugs ... (Site not responding. Last check: 2007-11-05)
		receptor, as observed with the benzodiazepines on the GABA
		receptors: involvement of serine 269 of the GABA
		Romano C, Yang W-L and O'Malley KL (1996) Metabotropic glutamate receptor 5 is a disulfide-linked dimer.
	molpharm.aspetjournals.org /cgi/content/full/60/5/881 (2947 words)

	Constitutive Activity of Glucagon Receptor Mutants -- Hjorth et al. 12 (1): 78 -- Molecular Endocrinology
		In the PTH, the VIP, and the glucagon receptors,
		Carruthers CJL, Unson CG, Kim HN, Sakmar TP 1994 Synthesis and expression of a gene for the rat glucagon receptor.
		Kudo M, Osuga Y, Kobilka BK, Hsueh AJW 1996 Transmembrane regions V and VI of the human luteinizing hormone receptor are required for constitutive activation by a mutation in the third intracellular loop.
	mend.endojournals.org /cgi/content/full/12/1/78 (4811 words)

	Steric Hindrance Mutagenesis versus Alanine Scan in Mapping of Ligand Binding Sites in the Tachykinin NK1 Receptor -- ... (Site not responding. Last check: 2007-11-05)
		In G protein-coupled receptors with 7TM, a main ligand-binding crevice is believed to be located between the loops and the
		Among 7TM receptors, one of the most thoroughly studied peptide systems is the tachykinin NK receptor.
		receptor involved in binding of the nonpeptide antagonist CP 96,345.
	intl-molpharm.aspetjournals.org /cgi/content/full/53/1/166 (6426 words)

	The Carboxyl Terminus of Human Cytomegalovirus-encoded 7 Transmembrane Receptor US28 Camouflages Agonism by Mediating ...
		C-terminal tails of the US28, NK, and ORF74 receptor chimeras beginning with the conserved NPXXY motif Receptor chimeras were generated by exchanging the cytoplasmic tails 8 residues proximal to the NPXXY motif at the end of TM7.
		HEK293 cells were transiently transfected with wild type NK receptor (A and B) or NK -US28ctail receptor DNAs (C and D).
		An antibody feeding experiment was performed with HA antibody for 30 min, and cells were fixed, permeabilized, and stained with a FITC-conjugated secondary antibody and imaged by fluorescence microscopy.
	www.jbc.org /cgi/content/full/278/21/19473 (6346 words)

	The Human Cytomegalovirus US28 Protein Is Located in Endocytic Vesicles and Undergoes Constitutive Endocytosis and ...
		Chemokine receptors are a subgroup of the superfamily of seven transmembrane domain (7TM) G-protein-coupled receptors (GPCRs)
		Davis-Poynter, N.J., Lynch, D.M., Vally, H., Shellam, G.R., Rawlinson, W.D., Barrell, B.G., and Farrell, H.E. Identification and characterization of a G protein-coupled receptor homolog encoded by murine cytomegalovirus.
		Margulies, B.J., Browne, H., and Gibson, W. Identification of the human cytomegalovirus G protein-coupled receptor homologue encoded by UL33 in infected cells and enveloped virus particles.
	www.molbiolcell.org /cgi/content/full/12/6/1737 (7814 words)

	A Library of 7TM Receptor C-terminal Tails: INTERACTIONS WITH THE PROPOSED POST-ENDOCYTIC SORTING PROTEINS ERM-BINDING ...
		mainly with the C-terminal intracellular tails of the receptors.
		family of seven-transmembrane receptors was probed as glutathione
		receptors for recycling to the cell membrane, which is the route
	www.jbc.org /cgi/content/abstract/279/52/54291 (525 words)

	SIDEROVSKI LAB @ UNC-Chapel Hill - WELCOME PAGE
		In the conventional model of heterotrimeric G-protein activation, the ligand/7TM receptor interaction catalyzes guanine nucleotide exchange on the Gbeta/gamma-complexed (and GDP-bound) Galpha subunit (Fig.
		Based on this cycle, the duration of heterotrimeric G-protein signaling is thought to be controlled by the lifetime of the Galpha subunit in its GTP-bound state.
		Ligand-occupied, 7TM cell-surface receptors stimulate signal onset by acting as guanine nucleotide exchange factors (GEFs) for Galpha subunits, facilitating GDP release, subsequent binding of GTP, and release of the Gbeta/gamma dimer.
	www.unc.edu /~dsiderov/intro.htm (443 words)

	Gordon Research Conference on LIGAND RECOGNITION & MOLECULAR GATING
		Surface expression of 7TM receptors through 1TM-7TM and 7TM-7TM heterodimerization.
		Ligand-induced homo- and hetero-dimerization of growth factor receptor tyrosine kinases.
		Receptor side chains and backbone in ligand recognition and gating of the nicotinic receptor
	www.grc.uri.edu /programs/1999/ligand.htm (321 words)

	Cell Biology Promotion (Site not responding. Last check: 2007-11-05)
		The receptor and the effector: one and the same, or are they separate entities?
		A switch in receptor signalling: activation of ERK by 7TM receptors
		The IgE receptor and a signal for exocytosis
	www.cellbiol.net /bodyTRcontents.htm (667 words)

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