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Receptor-binding

Not long ago. an a-melanotropin peptide analogue, cyclized through Tc coordination, was synthesized while retaining high affinity for receptors present on melanoma cells. In vivo the complex revealed selective accumulation in a murine melanoma tumor [246a], [Pg.412]

Ascorbic acid can block a variety of membrane-bound receptor proteins, the mechanisms of which are primarily explained by its antioxidant/prooxidant properties, rather than its direct binding to the receptors. [Pg.298]

Quinone conjugation to proteins occurs readily in vivo, and thus, autooxidation of DOPAC and other endogenous catechol-containing compounds could be an important component of protein modification. Indeed, the DOPAC quinone produced from autooxidation is responsible for the irreversible inhibition of [ H] spiperone binding to neuronal dopamine D2 receptors. Ascorbic acid and dithiothreitol can prevent this inhibition (Cammack et al, 1991b). [Pg.298]

Several lines of evidence have suggested the interactions of ascorbic acid with dopaminergic systems. Like the dopamine antagonist haloperidol, intraventricular or intrastriatal infusions of ascorbic acid (White et al, 1988, 1990) have been shown to attenuate the behavioral response to amphetamine, indicating that at some level ascorbic acid antagonizes the synaptic action of dopamine. Ascorbic acid also has been shown to mimic haloperidol in producing behavioral supersensitivity to [Pg.298]

Ascorbic acid has also been noted to be a potent inhibitor of opioid binding to guinea pig brain homogenate (Dunlap et aL, 1979 Leslie et aL, 1980). This effect is again due to ascorbic acid-induced lipid peroxidation, since it is prevented by removal of oxygen or by the presence of reducing agents. [Pg.299]

Redox phenomena seem to modulate activity of the NMDA subtype of glutamate receptors. Ascorbic acid inhibits binding of [ H]glutamate to the NMDA-receptor complex and impedes NMDA-gated currents in isolated neurons, whereas dithiothreitol-like reductants enhance NMDA-induced currents (Majewska et aL, 1990). The ability of reductants to alter function of the NMDA receptors is prevented by oxidation. This inhibitory effect of ascorbic acid on NMDA receptors may act to protect against excitotoxic insults to the neurons (Section 6). [Pg.299]


To understand the estimation of average drug-receptor binding energies... [Pg.319]

After an alignment of a set of molecules known to bind to the same receptor a comparative molecular field analysis CoMFA) makes it possible to determine and visuahze molecular interaction regions involved in hgand-receptor binding [51]. Further on, statistical methods such as partial least squares regression PLS) are applied to search for a correlation between CoMFA descriptors and biological activity. The CoMFA descriptors have been one of the most widely used set of descriptors. However, their apex has been reached. [Pg.428]

Other filters used for prefiltering account for lead- [22, 23] or drug-likeness [24-26], an appropriate ADMET profile [27-30], or favorable properties concerning receptor binding [31, 32]. [Pg.607]

Desjarlais R L, R P Sheridan, G L Seibel, J S Dixon, ID Kuntz and R Venkataraghavan 1988. Using Shap Complementarity as an Initial Screen in Designing Ligands for a Receptor Binding Site of Know Three-Dimensional Structure. Journal of Medicinal Chemistry 31 722-729. [Pg.737]

Fig. 4. FSH receptor-binding potencies of equine FSH ( ), eCG purified from pregnant mate s semm (O), and endometrial cups (A). Receptor-binding in ceU membrane fractions, B/Bq from (a) horse, (b) calf, and (c) rodent testes (40). Courtesy of Butterworth-Heinemaim. Fig. 4. FSH receptor-binding potencies of equine FSH ( ), eCG purified from pregnant mate s semm (O), and endometrial cups (A). Receptor-binding in ceU membrane fractions, B/Bq from (a) horse, (b) calf, and (c) rodent testes (40). Courtesy of Butterworth-Heinemaim.
Quantitative Structure—Activity Relationships. Many quantitative stmcture—activity relationship (QSAR) studies of progestins have appeared in the Hterature and an extensive review of this work is available (174). QSAR studies attempt to correlate electronic, steric, and/or hydrophobic properties to progestational activity or receptor binding affinity. A review focusing on the problems associated with QSAR of steroids has been pubUshed (175). [Pg.220]

Fig. 9. Sweetener receptor binding sites postulated by Tinti and Nofre, where 5 is an anionic group, eg, CO 2y or CN a hydrogen bond donor... Fig. 9. Sweetener receptor binding sites postulated by Tinti and Nofre, where 5 is an anionic group, eg, CO 2y or CN a hydrogen bond donor...
J) At position 1, an acidic side chain two or three carbons long should be present. The natural L-alanyl side chain reduces receptor binding but enhances in vivo activity by increasing access to the receptor and by retarding metaboHsm and excretion. The enantiomeric D-analogues retain considerable activity in contrast to other bioactive substances (17). [Pg.50]

More subtle modes of action are also possible since the response to hormone receptor binding is complex and could be affected by chemical interference with receptor-related proteins, DNA methylation or histone acetylation. Dioxin (TCDD), for example, reduces the ability of the oestrogen-receptor complex to bind to the oestrogen response element of DNA, reducing gene transcription. ... [Pg.12]

Oestrogen receptor binding/Reporter gene assay. [Pg.18]


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5-Receptor affinity binding properties

8-Opioid receptor binding sites

AMPA receptor binding

AMPA receptor binding protein

Accessory binding sites, receptor

Acetylcholine cholinergic receptor binding

Acetylcholine receptor binding

Acetylcholine receptor toxin-binding site

Acetylcholine receptors nerve agent binding

Acetylcholinesterase receptor binding

Acetylcholine—structure, SAR, and receptor binding

Adenosine receptor radioligand binding studies

Adenosine receptors binding site models

Adenosine receptors binding sites

Adrenaline 32-adrenergic receptor binding

Ah Receptor Binding

Amino acids receptor binding

Androgen receptor binding

Androgen receptor, pesticide binding

Anion binding amide-based receptors

Anion binding by neutral ferrocene-amide receptors

Anion receptors containing ammonium binding sites

Anion receptors containing guanidinium binding sites

Antagonist receptor binding

Apolipoprotein receptor-binding region

Apomorphine receptor binding

Auxins receptors/binding proteins

Avian DNA-binding receptor proteins

Benzodiazepine receptor binding

Benzodiazepine receptors binding sites

Benzodiazepines GABAa receptor binding

Bicuculline GABAa receptor binding

Binding interactions, drug receptor

Binding modes, receptors

Binding theory receptor occupancy

Binding to acetylcholine receptor

Binding to glycine receptor

Binding to muscarinic acetylcholine receptor

Binding to receptors

Binding, antagonist/receptor effectiveness

Binding, drug-receptor distribution affected

Binding, drug-receptor interactions based

Binding, receptor/ligand autocrine growth factor

Binding, receptor/ligand diffusion

Binding, receptor/ligand membrane-associated molecules

Botulinum toxin causes skeletal muscle paralysis by binding to acetylcholine receptors on the motor end plate

Bungarotoxins nicotinic acetylcholine receptor binding

Buprenorphine receptor, binding

CAMP response element binding receptors

Cadherin receptor binding

Cannabinoid receptor binding

Cell cycle protein modulation ligand receptor binding

Cell membrane, receptor/ligand binding

Cell surface, receptor/ligand binding

Chemical detection molecule-receptor binding

Chemokine receptors promiscuous binding

Cobaltocenium based receptors chloride binding

Complementarity receptor-substrate binding

Corticosteroid-Binding Globulin receptor

DNA Binding Elements of Nuclear Receptors, HREs

Decorative receptors, membrane-binding

Decoy receptors, membrane-binding

Definitions of Drug-Receptor Binding Interactions

Diastereomers receptor binding

Dibenzofuran receptor binding affinity

Dopamine receptor binding imaging

Drug-Receptor Binding Energies

Drug-receptor binding

Drug-receptor interactions cooperative binding

Enkephalin analogs receptor binding affinities

Epidermal growth factor receptor ligand binding

Estrogen receptor binding

Estrogen receptor binding activity

Estrogen receptor binding assays

Estrogen receptor competitive binding

Estrogen receptor competitive binding assays

Estrogen receptor estradiol binding

Estrogen receptor pesticide binding

Excitatory amino acids receptor binding

Experimental Quantification of Drug-Receptor Binding Interactions

Ferrocene based anion receptors binding

Fibrinogen receptor binding

Fitting of Binding Data and Search for Receptor Databases

Fluorescence methods ligand-receptor binding

Formyl peptide receptor ligand binding

GABA receptor binding

GABA receptors benzodiazepine binding

GABA receptors binding sites

GABAa receptor binding, alterations

GABAa receptors, activation barbiturate binding site

GABAa receptors, activation benzodiazepine binding site

GABAa receptors, activation binding affinities

GTP-binding proteins coupled receptors

Glucocorticoid receptor binding

Glucocorticoid receptor ligand-binding domain

Glucocorticoid receptor, DNA binding domain

Glycine (Gly drugs binding to receptors

Glycoproteins receptor binding

Growth hormone receptor binding domains

Hormone Receptor Binding Sites

Hormone receptor binding

Hormone receptor drug binding

Hormone receptor ligand-binding domains

Hormones binding to receptors

Hydrogen bonding receptor binding

Hydrophilic interactions receptor binding

Hydrophobic interactions receptor binding

Imidacloprid receptor binding studies

In vitro receptor- binding assays

Inhibition of receptor binding

Inhibitor, receptor binding

Insecticides that Bind to Nicotinic Acetylcholine Receptor

Ionotropic glutamate receptors binding

Ionotropic glutamate receptors ligand binding

Kainic acid-binding glutamate receptors

Kinetics receptor/ligand binding

Ligand affinity agonist-receptor binding, dissociation

Ligand affinity receptor protein, binding site

Ligand binding adrenergic receptors

Ligand binding histamine receptors

Ligand binding muscarinic receptors

Ligand binding neuropeptide receptors

Ligand binding nicotinic receptors

Ligand binding receptor spheres

Ligand binding receptor-based

Ligand receptor binding studies

Ligand-binding domains receptor tyrosine kinases

Ligand-receptor Binding Surface

Ligands receptor/ligand binding

Lipoprotein receptors, binding affinity

Melatonin receptor binding

Membranes acetylcholine-receptor binding

Meperidine opioid receptor binding

Models receptor/ligand binding kinetics

Molecular Interactions and Binding Modes of CCR5 Receptor Antagonists

Molecular ligand-receptor binding

Molecular modelling receptor binding

Molecule-receptor binding

Molecule-receptor binding controlled synthesis

Molecule-receptor binding defense

Molecule-receptor binding events

Molecule-receptor binding methods

Molecule-receptor binding protein stabilization

Molecule-receptor binding sensor components

Molecule-receptor binding transducers

Morphine opioid receptor binding

Mouse vas deferens activity in receptor binding assa

Muscarinic receptor binding

Muscarinic receptors organophosphate binding

NAChR receptor ligand binding domains

Naloxone opioid receptor binding

Nervous system nicotinic acetylcholine receptor binding

Neuroleptics ligand receptor binding studies

Neurotransmitter receptor binding agents

Nicotinic acetylcholine receptors organophosphate binding

Nicotinic receptors acetylcholine binding with

Nuclear hormone receptors drug binding

Nuclear hormone receptors ligand-binding domains

Nuclear receptor Ligand binding domain

Nuclear receptor-binding site

Oestrogen receptor binding

Opiate receptors affinity binding

Opioid receptor binding

Opioid receptor binding of pentapeptides

Opioid receptors agonist binding

Opioid receptors ligand binding model

Oxytocin receptor binding affinities

Oxytocin receptors, binding

P-Opioid receptor binding affinities

P-Opioid receptor radioligand binding assay

P-Receptor affinity binding properties

Palindromic sequences glucocorticoid receptor binding

Peroxisome proliferator activated receptor binding protein

Picrotoxin GABAa receptor binding

Polymerization process, receptor binding

Progesterone receptor binding agents

Prostacyclin receptors PGI2 binding

Protein receptor interactions, binding

Quantitative structure-activity relationship estrogen receptor binding affinity

Radioligand binding studies receptor preparations

Radioligand-receptor binding

Receptor Binding Affinity of Dibenzofurans

Receptor Determination DHP Binding Sites on Surface Membranes

Receptor agonist binding

Receptor androgen, binding affinity

Receptor binding ability

Receptor binding affinities

Receptor binding assay activity

Receptor binding assay mouse vas deferens

Receptor binding assays

Receptor binding assays fundamentals

Receptor binding assays saturability

Receptor binding assays specificity

Receptor binding cavity

Receptor binding characteristics

Receptor binding characteristics initiate responses

Receptor binding conformational flexibility

Receptor binding domain

Receptor binding drug design

Receptor binding empirical approach

Receptor binding experimental approaches

Receptor binding models thyroid hormones

Receptor binding peptide ligands

Receptor binding properties

Receptor binding properties of Tyr-D-Ala-Phe-Asp-Val-ValThr -Gly

Receptor binding properties ofTyr-D-Ala-Phe- Tyr-Pro-Ser

Receptor binding proteins

Receptor binding site models

Receptor binding site-specific mutation

Receptor binding sites

Receptor binding studies

Receptor binding thermodynamics

Receptor binding, enhancement

Receptor binding, estrogens nuclear

Receptor binding, estrogens transmembrane

Receptor binding, irreversible

Receptor binding, toxicolog

Receptor chloramphenicol binding

Receptor superfamilies extracellular ligand binding domains

Receptor-analyte binding

Receptor-binding and Translocation

Receptor-binding epitopes, chemokines

Receptor-binding kinetics model

Receptor-binding regions

Receptor-ligand binding

Receptor-ligand binding assay

Receptor-ligand binding interactions

Receptor-ligand binding interactions equilibrium thermodynamics

Receptor-ligand binding parameters

Receptor-ligand binding reactions

Receptor-ligand binding specific

Receptor-ligand-binding process

Receptor-substrate binding, enzymes

Receptors binding constant

Receptors chemical binding

Receptors ethylene-binding

Receptors neurotransmitter binding

Receptors with Different Binding Sites

Retinoic acid receptor bind response elements

Retinoic acid receptor binding domains

Retinoic acid receptor ligand binding domain

Retinoid receptors ligand-binding assay

Retinoid receptors ligand-binding pocket

Role of GTP-binding proteins in receptor-response coupling

Ryanodine receptors, FKBP12-binding

Scoring Functions - Methods to Estimate Ligand-Receptor Binding

Seven-transmembrane domain receptors nucleotide-binding proteins

Signaling pathways binding, cell surface receptors

Simultaneous binding, cations ditopic receptors

Solution, receptor/ligand binding

Soman muscarinic receptor binding

Spiperone specific binding receptors

Stereoisomers receptor binding

Steroid-receptor binding

Structural Determinants of Ligand Binding and Receptor Activation by CC Chemokines

Structural Requirements for Receptor Binding

Sulpiride receptor binding

Taste receptor binding

The Binding of Chemokines to Chemokine Receptors

The Distinction between Agonist Binding and Receptor Activation

The Law of Mass Action, binding sites and receptors—understanding why specific, potent biological activity is a rare property for any one chemical to possess

Those Binding to the Steroid Hormone Receptors

Thyroid hormone receptor binding

Thyroid hormone receptor binding assay

Toll-Like Receptors and Effects of Binding by Fungal PAMPs

Transport mechanism, receptor/ligand binding

Type Lectin-Like Receptors and Effects of Binding by Fungal PAMPs

Water receptor binding thermodynamics

Y-Aminobutyric acid receptor inhibition of EBOB binding

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