In Vitro Pharmacological Screening for Potency Selectivity

In Vivo Target Directed

Broad Based In Vivo Screening

Pharmacological Screening

Pharmacokinetics/Pharmacodynamics

Disease Models

ADME

Antisense/siRNA

Cardiovascular

Transgenic Animals

Toxicology

/

Optimized Lead as Potential Human Therapeutic

Optimized Lead as Potential Human Therapeutic

FIGURE 3.2 Flowchart of GPCR drug discovery research.

of GPCRs. Family C shares structural similarity to the metabotropic glutamate receptor and is characterized by an extracellular ligand-binding domain. It is comprised of 11 liganded and about 5 orphan GPCRs and is represented by the metabotropic glutamate and GABAb receptors. The most recently described and less characterized Family F/S is composed of frizzled and smoothened receptors that play a role in cellular development.6 A comprehensive description of GPCR classification is provided in Chapter 10.

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