Receptors and genes

Newer pharmacologic approaches targeting receptors and genes... 

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With the catolog of human receptors and genes available, it should be possible to manipulate the expression of the receptor genes in tissue culture, and test the binding affinities of the phenethylamines against the receptors in vitro. Once the distribution of these receptors in the brain is determined, the information would then be in place to complete the "ideal" research program discussed above. 

The observation of dependent variable values (in functional experiments this is cellular response) as they happen (i.e., as the agonist or antagonist binds to the receptor and as the cell responds) is referred to as real time. In contrast, a response chosen at a single point in time is referred to as stop-time experimentation. There are certain experimental formats that must utilize stop-time measurement of responses since the preparation is irreparably altered by the process of measuring response. For example, measurement of gene activation through reporter molecules necessitates lysis of the cell. Therefore, only one... 

Orphan receptor, a gene product that is predicted to be a receptor through structure and spontaneous interaction with G-proteins but for which there is no known endogenous ligand or physiological function. 

Subtype, often refers to a receptor and denotes a variation in the gene product such that the endogenous ligand is the same (i.e., neurotransmitter, hormone) but the function, distribution, and sensitivity of the receptor subtypes differ. Antagonists often can distinguish receptor subtypes. 

The family of apelin peptides is derived from a single gene, activate a single G-protein-coupled receptor and are substrates for the angiotensin converting enzyme-2 (ACE2). Apelins regulate cardiovascular function and fluid homeostasis. The apelin receptor also functions as a co-receptor for infection of CD4-positive cells by human immunodeficiency vims ( HIV). 

Cytokines. Figure 1 Inhibition of cytokine synthesis during activation of the specific immune system. The monoclonal antibodies Muromonab and Basiliximab are specific for the CD3 complex of the T-cell receptor, and for the IL-2 receptor on lymphocytes, respectively. Cyclosporin and Tacrolimus inhibit activation of cytoplasmic NF-AT, a transcription factor essential for activation of the IL-2 gene ( NFAT Family of Transcription Factors). Sirolimus interferes with mTOR signaling and inhibits IL-2 dependent proliferation. Red pharmaka, blue target proteins. 

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