interactions predicting receptor ligand pairings

... dynamic specific ligand recognition pocket in the extracellular loops of the TP receptor and the ligand/ receptor recognition mechanism, which may also apply to other prostanoid receptors Materials ... [53] Other GPCRs Thyrotropin-releasing hormone receptor Human P2Y1 receptor A1/A3 adenosine receptor Human A2a adenosine receptor a1-Adrenergic receptor eLP2 eLP2 [54] [55] Ó FEBS 2004 3008 K.-H ... structural information about the ligand recognition pocket of the TP receptor The structural information revealed several critical molecular mechanisms of the specific ligand /receptor interaction, which...

Ngày tải lên: 16/03/2014, 18:20

... estrogen receptor ligand binding domain in its dimeric noncovalently bound form Craig et al [25] analyzed by microESI-MS the binding of the human vitamin D receptor and the retinoid X receptor- a ... of ligands on this equilibrium Ligand modulation of HD–CoRNR ternary complexes In order to monitor the effect of different types of ligands on the recruitment of two CoRNR peptides, various ligands ... protein ligand complexes Combining rapidity, sensitivity and accuracy, it will play an increasingly important role not only for the analysis of nuclear receptor action and (orphan) receptor ligand...

Ngày tải lên: 23/03/2014, 13:20

... Oxford University Press, New York De Schamphelaere K A C and Janssen C R (2002) A Biotic Ligand Model predicting acute copper toxicity for Daphnia magna: The effects of calcium, magnesium, sodium, ... non-competitive interactions: Implications for an algal BLM, Aquat Toxicol., 84, 123-132 Hatano A and Shoji R (2008) Toxicity of Copper and Cadmium in Combinations to Duckweed Analyzed by the Biotic Ligand ... Toxicol., 23, 372-378 Heijerick D G., De Schamphelaere K A C and Janssen C R (2002) Biotic ligand model development predicting Zn toxicity to the alga Pseudokirchneriella subcapitata: possibilities and...

Ngày tải lên: 05/09/2013, 10:15

... necessary, alongside HSPGs, for PTPr interactions Results Nucleolin is a PTPr-binding protein We have shown previously that PTPr binds to an unidentified ligand, or ligand complex, in developing muscle ... blockade of PTPr interactions with other known ligand sites, in particular those of HSPGs in retinal basement membranes It is not clear what this means at present, as the basement membrane interactions ... (1996) Inhibition of FGF receptor activity in retinal ganglion cell axons causes errors in target recognition Neuron 17, 245–254 Doherty P & Walsh FS (1996) CAM–FGF receptor interactions: a model...

Ngày tải lên: 19/02/2014, 05:20

... 0.95 A) The notable uorescence changes upon ligand binding here described show that the P-pyridoxyl group is a useful probe to monitor ligand binding and ligand- induced conformational changes in ... upon ligand binding in solution Analysis of the uorescent characteristics of the reduced Schiff base allowed us to obtain binding constants for the interaction of several substrates and ligands, ... ẳ Sfisi, where fi is the amplitude fraction The effect of ligands was analyzed by monitoring the change of uorescence intensity upon ligand addition to protein solutions OAA solutions were prepared...

Ngày tải lên: 21/02/2014, 01:21

... C-terminus of the A2A receptor are involved in heterodimerization between the adenosine A2A receptor and the dopamine D2 receptor [43] A similar interaction has also been shown for D1–NMDA receptor heterodimers ... monitor the physical interactions between receptor proteins [51,52] Results Radioligand binding assay As shown in Table 1, the binding parameters obtained for dopamine D1 receptor and its mutant ... or D2 receptors, which were tagged with YFP As seen in Fig 4, the FRET phenomenon takes place only when the D1 receptor is co-expressed with as or D2 receptor is co-expressed with The interactions...

Ngày tải lên: 07/03/2014, 03:20

... the result of specific protein–protein interactions between the receptors, rather than nonspecific diffusive lateral motion or clustering of overexpressed receptors First, the lifetime of an excited ... Krogsgaard-Larsen, P (2000) Ligands for glutamate receptors: design and therapeutic prospects J Med Chem 43, 2609–2645 Nakanishi, S (1994) Metabotropic glutamate receptors: synaptic transmission, ... purification of the extracellular ligand binding region of metabotropic glutamate receptor subtype J Biol Chem 273, 13089–13096 16 Han, G & Hampson, D.R (1999) Ligand binding to the aminoterminal...

Ngày tải lên: 08/03/2014, 09:20

... heterogeneous ligand- binding model and the bivalent analyte model – both supplemented with the BIAevalution Wizard The heterogeneous ligand- binding model assumes that two parallel and independent interactions ... The neonatal Fc receptor (FcRn), which plays a central role in prolonging the half-life of IgG and albumin [1–3], is a major histocompatibility complex (MHC) class I-related receptor consisting ... assumes that two parallel and independent interactions (KD1 and KD2) take place between the ligand and the receptor, and the derived affinities were determined to be 6.7 ± 0.1 · 10)9 m (KD1) and 219.0...

Ngày tải lên: 16/03/2014, 06:20

... vertebrate hormone receptors [2024] It is generally accepted that ligand- free AhR molecules are mainly cytoplasmic, and that binding to the ligand triggers the translocation of the receptorligand complex ... [32,33] It is also required for liganddependent activation mediated in yeast by several vertebrate receptors, including the glucocorticoid, estrogen and retinoic acid receptors [3436] Carbaryl (1-naphthyl-N-methylcarbamate) ... biomarker of ectopic activation of the AhR receptor by exogenous ligands present in the environment [11,39] However, carbaryl differs structurally from typical AhR ligands, which are aromatic compounds...

Ngày tải lên: 16/03/2014, 10:20

... target receptor In fact, it is well-established in the nuclear receptor field that the development of useful synthetic agonists ⁄ antagonists can occur before the endogenous ligand( s) of the receptor ... competitively displace a quenching ligand (JH III) from the receptor, so as to relieve the receptor quenching caused by JH III That is, if the nonfluorescence-suppressing ligand can actually bind, then ... for understanding how farnesoids fit into the USP ligand- binding pocket The natural ligands for nuclear receptors not fully occupy the cavity of the ligand- binding pocket For example, 53–67% occupancy...

Ngày tải lên: 16/03/2014, 12:20

... physiological relevance of the many interactions It remains to be established whether all interactions take place in living cells under physiological conditions, whether interactions with different proteins ... described for other nuclear receptors ERa ligand- dependent direct N/C interaction has been demonstrated, which was disrupted by amino acid substitutions that affect receptor function [52,53] The ... nuclear receptor coactivator interactions Genes Dev 12, 3343–3356 Onate, S.A., Boonyaratanakornkit, V., Spencer, T.E., Tsai, S.Y., Tsai, M.J., Edwards, D.P & O’Malley, B.W (1998) The steroid receptor...

Ngày tải lên: 17/03/2014, 10:20

... role of the hinge region for liganddependent effects and ligand binding remains a matter of conjecture (compare [36] with the alignment in [37]) The induction by ligand of heterodimerization ... though ligand binding to EcR–LBD was low, it was significant and has been observed before with full-length EcR [20,43–45] There exists a clear positive correlation between ligand binding and ligand ... gene encodes an ecdysone receptor, a new member of the steroid receptor superfamily Cell 67, 59–77 Lezzi, M., Bergman, T., Mouillet, J.-F & Henrich, V.C (1999) The ecdysone receptor puzzle Arch Insect...

Ngày tải lên: 18/03/2014, 01:20

... Two water molecules also make hydrogen bonds with the ligand; several other residues contribute hydrophobic interactions (Fig 2) Most of these interactions have been identified previously in complexes ... galactose chemoreceptor protein Science 242, 1290– 1295 ˚ 25 Flocco MM & Mowbray SL (1994) The 1.9 A X-ray structure of a closed unliganded form of the periplasmic glucose ⁄ galactose receptor from ... (marked with red ovals in Fig 2B): B Fig Interactions in the binding site (A) Stereoview of bound GGal showing GBP residues making hydrogen-bonding and aromatic interactions (B) Schematic diagram of...

Ngày tải lên: 23/03/2014, 04:21

... receptor and analysis of the receptor- ligand interaction J Med Chem 36, 820–825 21 Ruan KH, Wu J, So SP, Jenkins LA & Ruan CH (2004) NMR structure of the thromboxane A2 receptor ligand recognition pocket ... mapping of the residues that are important for receptor ligand recognition in the eLP2 region of human IP A profile of the IP eLP2 residues involved in the receptor agonist recognition is revealed Results ... are involved in the configuration of a general ligand recognition pocket for the receptors, but the residues are less important for determining the receptor selectivities in binding to the different...

Ngày tải lên: 23/03/2014, 07:20

... noncovalent interactions with the type I receptor (Fig 2) Although the noncanonical loop conformation of BMP-6 seems not to be able to form a stable ligand receptor interface using the type I receptor ... high degree of promiscuity in the BMP ligand receptor interaction, as it allows the ligand as well as the receptor surfaces to adapt to the binding partner Receptor binding and activity of BMP-6 ... determinants for type I receptor recognition in BMP-2 [23] and GDF-5 [17] Structure analysis of receptor ligand complexes of BMP-2 [23,24] and BMP-7 [25] suggested that receptor binding and recognition...

Ngày tải lên: 23/03/2014, 07:20

... LA-7 Interaction with ligand- binding domain Induction of conformational change Interaction with ligand- binding domain Interaction with ligand- binding domain Interaction with ligand- binding domain ... Fig Hybrid receptors and relative amount of pH-dependent ligand dissociation (A) Schematic models of the hybrid receptors LDLR domains are depicted in gray and LpR domains in black Each receptor ... possibility that differences in ligand binding were caused by differences in receptor expression, binding of antibody to the receptor was used as a measure for the amount of receptor on the plasma membrane...

Ngày tải lên: 23/03/2014, 07:20

... low affinity receptor pool that is conformationally responsive to ligand J Biol Chem 270, 28740–28750 24 Newham, P., Craig, S.E., Clark, K., Mould, A.P & Humphries, M.J (1998) Analysis of ligand- induced ... a cleft for ligand binding Binding sites involving two consecutive IgSF domains were already observed in other IgSF proteins, not involved in integrin binding, such as the cytokine receptor family ... largely involve the site, play a key role in ligand recognition Aspartate or ABED sheet of D1 domain However, in the cell adhesion glutamate residues of ligands form part of the coordination assay...

Ngày tải lên: 23/03/2014, 13:20

... ecdysone receptor in hormone signaling Nuclear hormone receptors play key roles in metazoan development, metabolic homeostasis, and response to xenobiotics Some of these nuclear receptors bind ligands ... these receptors on gene transcription, while other receptors are apparently constituitively active and unregulated by dynamic equilibrium with ligand [1] For example, the retinoic acid receptor ... above ligand- binding receptors and their close relatives functions as a heterodimer with the (also homodimer-forming) retinoid-X -receptor (RXR), which itself can be activated by the RAR ligand...

Ngày tải lên: 23/03/2014, 13:20

... higher-affinity ligands for USP The molecular interactions between a receptor and a synthetic activating ligand have previously provided insight to the molecular basis by which agonist ligand( s) activates ... the C472A/H475L mutations on the ligand- binding activity of USP Some models of nuclear hormone receptor action include the component that binding of ligand to the ligand- binding pocket induces a ... the ligand binding pocket of the estrogen receptor (450–500 A3 [46,47]), Yet, b-estradiol is nonetheless able to bind to and activate the estrogen receptor Thus, PPARc and the estrogen receptor...

Ngày tải lên: 23/03/2014, 21:20

... that recognizes activated ERK specifically RESULTS Ligand- binding abilities of the chimeric receptors The ligand- binding abilities of the chimeric receptors were measured (Fig 2) After the incubation ... the chimeric receptors ErbB-1, ErbB-4, and the chimeric receptors were tested for autophosphorylation (Fig 3) In response to the ligand binding to the ectodomains, the dimerized receptors phosphorylate ... cognate receptors, which suggests a common mechanism for both homodimerization and heterodimerization of the ErbBfamily receptors Nevertheless, the interaction of the ligand with the receptor...

Ngày tải lên: 24/03/2014, 03:21