Medicinal Chemistry
regulation, respectively, but they are also probably different in a morphological sense: the neuromodulatory receptors are assum ...
antagonists are very similar in structure, but if one considers the relationship between the endogenous peptide opiates known as ...
being composed of more than one protein; facilitatory and inhibitory interactions exist between these subunits and may alter the ...
R or T state), signaling subsequent links in the receptor–effector chain that ultimately trigger the biological effect. Besides ...
multipotential association. However, it is probably true that a recognition site that operates an ion gate is more permanently a ...
the number of available receptors (as in the case of the insulin receptor). Heterospecific regulation is shown, for instance, by ...
transported to the interior of the cell. Perhaps the most important role of internalization is the removal of receptors from the ...
produced by bacteria such as Staphylococcus aureus respond to antibiotics such as penicillin. Penicillin binds to “exogenous rec ...
mapped by Gilman and his group. This chain of reactions is shown in figure 2.4. Membrane receptors that operate through adenylat ...
and molecular modeling studies of these proteins. Early work suggested that there were three types of heterotrimeric G protein: ...
Inositol triphosphate is water soluble and therefore diffuses into the cytoplasm, where it mobilizes calcium from its stores in ...
2.11.1 Disease-Centered Receptor Selection In this approach, several possible receptors for a single disease entity (e.g., Alzhe ...
systems (cardiac, respiratory, gastrointestinal, genitourinary) and structural systems (musculosketelal, dermatological). The co ...
2.11.4.1 Targets 1–3 The first three categories target endogenous messengers. An endogenous messenger is a molecule synthesized ...
targets have to be considered. Like the messenger target, these nonmessenger targets can be divided into three logical groups. T ...
always be kept in mind. The drug molecule must be able to withstand the pharmaceutical and pharmacokinetic phases of drug action ...
interactions between two co-administered drugs, and are a common clinical problem. Table 2.2 shows a partial listing of drugs wi ...
c. M—Metabolism competition (competition for same enzymes in liver). d. E—Elimination competition (similar structures are compet ...
P. M. Laduron (1982). Towards a unitary concept of opiate receptor. Trends Pharmacol. Sci. 3: 351–352. K. E. Light (1984). Analy ...
Molecular Structure of Receptors A. A. Abdel-Latif (1986). Calcium-mobilizing receptors, polyphosphoinositides, and the generati ...
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