Estimation of competitive antagonist affinity from functional inhibition curves using the Gaddum, Schild and Cheng-Prusoff equations.
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Taking the time to study competitive antagonismHow Natalizumab Binds and Antagonizes 4 IntegrinsFrom 'captive' agonism to insurmountable antagonism: demonstrating the power of analytical pharmacology.Prostanoid receptor antagonists: development strategies and therapeutic applicationsAntagonist selective modulation of adenosine A1 and A3 receptor pharmacology by the food dye Brilliant Black BN: evidence for allosteric interactionsProtein engineering of the N-terminus of NEMO: structure stabilization and rescue of IKKβ binding.Characterization of the muscarinic receptor subtype(s) mediating contraction of the guinea-pig lung strip and inhibition of acetylcholine release in the guinea-pig trachea with the selective muscarinic receptor antagonist tripitramine.Functional characterization of alpha 1-adrenoceptor subtypes in vascular tissues using different experimental approaches: a comparative study.Extracellular nucleotides induce vasodilatation in human arteries via prostaglandins, nitric oxide and endothelium-derived hyperpolarising factor.Differences in agonist and antagonist activities for two indices of metabotropic glutamate receptor-stimulated phosphoinositide turnover.Pharmacological characterization of acetylcholine-stimulated [35S]-GTP gamma S binding mediated by human muscarinic m1-m4 receptors: antagonist studies.Species-specific action of (Pro3)GIP - a full agonist at human GIP receptors, but a partial agonist and competitive antagonist at rat and mouse GIP receptorsN-terminally and C-terminally truncated forms of glucose-dependent insulinotropic polypeptide are high-affinity competitive antagonists of the human GIP receptorIC50-to-Ki: a web-based tool for converting IC50 to Ki values for inhibitors of enzyme activity and ligand bindingKinetic analysis of cytokine-mediated receptor assembly using engineered FC heterodimers.ADN-1184 a monoaminergic ligand with 5-HT(6/7) receptor antagonist activity: pharmacological profile and potential therapeutic utility.Design, synthesis and evaluation in an LPS rodent model of neuroinflammation of a novel 18F-labelled PET tracer targeting P2X7.Rational design of CXCR4 specific antibodies with elongated CDRs.Chemical modification of the M(1) agonist VU0364572 reveals molecular switches in pharmacology and a bitopic binding mode.Quantitative Measure of Receptor Agonist and Modulator Equi-Response and Equi-Occupancy Selectivity.Measuring the contractile response of isolated tissue using an image sensor.Contacts-based prediction of binding affinity in protein-protein complexes.Roles of affinity and lipophilicity in the slow kinetics of prostanoid receptor antagonists on isolated smooth muscle preparations.Probing the acceptor active site organization of the human recombinant β1,4-galactosyltransferase 7 and design of xyloside-based inhibitors.The molecular interaction of the high affinity reversal agent XR9576 with P-glycoprotein.Modulation by central postsynaptic alpha 2-adrenoceptors of the jaw-opening reflex induced by orofacial stimulation in rats.An immunosuppressive antibody-drug conjugate.Inhibition of the constitutive activity of human 5-HT1A receptors by the inverse agonist, spiperone but not the neutral antagonist, WAY 100,635Mechanisms of agonism and inverse agonism at serotonin 5-HT1A receptors.Pharmacological analysis of dopamine stimulation of [35S]-GTP gamma S binding via human D2short and D2long dopamine receptors expressed in recombinant cells.Agonist-stimulated [35S]GTPγS binding.Antagonist inhibition curves and the measurement of dissociation constants.Towards a high-affinity allosteric enhancer at muscarinic M1 receptors.Parameters of drug antagonism: re-examination of two modes of functional competitive drug antagonism on intraocular muscles.Binding free energy predictions of farnesoid X receptor (FXR) agonists using a linear interaction energy (LIE) approach with reliability estimation: application to the D3R Grand Challenge 2.Water-soluble nicotinic acetylcholine receptor formed by alpha7 subunit extracellular domains.Variable Dependence of Signaling Output on Agonist Occupancy of Ste2p, a G Protein-coupled Receptor in Yeast.Analyzing isolated blood vessel contraction in multi-well plates.Practical aspects of radioligand binding.Distinct muscarinic receptor subtypes suppress excitatory and inhibitory synaptic responses in cortical neurons.
P2860
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P2860
Estimation of competitive antagonist affinity from functional inhibition curves using the Gaddum, Schild and Cheng-Prusoff equations.
description
1993 nî lūn-bûn
@nan
1993 թուականի Օգոստոսին հրատարակուած գիտական յօդուած
@hyw
1993 թվականի օգոստոսին հրատարակված գիտական հոդված
@hy
1993年の論文
@ja
1993年論文
@yue
1993年論文
@zh-hant
1993年論文
@zh-hk
1993年論文
@zh-mo
1993年論文
@zh-tw
1993年论文
@wuu
name
Estimation of competitive anta ...... d and Cheng-Prusoff equations.
@ast
Estimation of competitive anta ...... d and Cheng-Prusoff equations.
@en
Estimation of competitive anta ...... d and Cheng-Prusoff equations.
@nl
type
label
Estimation of competitive anta ...... d and Cheng-Prusoff equations.
@ast
Estimation of competitive anta ...... d and Cheng-Prusoff equations.
@en
Estimation of competitive anta ...... d and Cheng-Prusoff equations.
@nl
prefLabel
Estimation of competitive anta ...... d and Cheng-Prusoff equations.
@ast
Estimation of competitive anta ...... d and Cheng-Prusoff equations.
@en
Estimation of competitive anta ...... d and Cheng-Prusoff equations.
@nl
P2860
P1476
Estimation of competitive anta ...... d and Cheng-Prusoff equations.
@en
P2093
Birdsall NJ
Lazareno S
P2860
P304
P356
10.1111/J.1476-5381.1993.TB13737.X
P407
P577
1993-08-01T00:00:00Z