9780521516358book.pdf

Partial agonists: These ligands also increase the activity of the receptors but do not produce the maximal response shown by fu ...

Partial inverse agonists: These agonists decrease the activity of constitutively active receptors but not to their inactive sta ...

100 50 0 Response (% maximum) 10 –9 10 –8 10 –7 10 –6 10 –5 Concentration of agonist (log scale) (b) Full agonist Full agonist a ...

receptors. It primarily relates to G-protein-coupled receptors that can bind to two or more G-proteins. Potency: This is a meas ...

membrane or within the cell cytoplasm, that terminate in the final target cell response. Examples of second messengers are Ca^2 ...

agonismis a behaviour characteristic of a particular ligand and can be demonstrated in the absence of any other ligand for the ...

they have several distinct conformational states and that these states can be switched with distinct kinetics by the various cla ...

its own in the absence of the agonist or antagonist. Allosteric enhancers are a subgroup of these allosteric modulators; Ago-al ...

wherekþ 1 is the association rate constant andk 1 is the dissociation rate constant. Therefore: k 1 kþ 1 ¼Kd¼ 1 Ka ¼ ð½RtŠ½RL ...

In this case, a plot ofr/[L] againstrwill again be linear with a slope of1/Kdbut in this case the intercept on thex-axis will b ...

and secondly that there is cooperativity in binding within a single population. In both cases the Scatchard plot will be curvili ...

The association rate constant,kþ 1 (units: M^1 time^1 ), is best estimated by the approach to equilibrium methodby which the e ...

Example 1(cont.) Answer To address this problem it is first necessary to calculate the specific binding of the ligand to the rec ...

large, it actually represents a small fraction of the total membrane protein. This partly explains why receptor proteins are som ...

Quantitative characterisation of competitive antagonists The ability of a competitive antagonist to reduce the response of a rec ...

To carry out a Schildt plot, the receptor response to increasing concentrations of agonist for a series of fixed concentrations ...

17.3 Ligand-binding and cell-signalling studies 17.3.1 Selection of ligand and receptor preparation Receptor preparations Prepar ...

17.3.2 Experimental procedures for ligand-binding studies The general experimental approach for studying the kinetics of recepto ...

series of ligand concentrations to cover 10–90% of maximum binding at a fixed receptor concentration. The binding data are then ...

Experimental techniques for the study of the binding of a ligand to a membrane receptor Equations 17.1 to 17.11 allow the calcul ...