Intracellular therapeutic target drug

Mechanisms of drug action. To mediate a response the drug can bind to the desired therapeutic target or to other molecular targets such as G-protein-coupled receptors (GPCRs), ion channels, or transporters on the cell membrane, or to intracellular targets such as enzymes and nuclear hormone receptors. 

Efficacy of therapeutically active drugs known to act on intracellular targets can be enhanced by specific delivery to the site of action. Triphenylphosphoniiun cations can be used to create subcellular targeted Hposomes that efficiently deliver drugs to mitochondria, thus enhancing their therapeutic action. 

The efflux transporter P-glycoprotein (P-gp) has been proposed as a potential therapeutic target for AD [439]. Approximately 10-35 % decrease in 125I-Ap(i 0) intracellular accumulation was observed in cells treated with rifampicin, dexamethasone, caffeine, verapamil, hyperforin, p-estradiol, and pentylenetetrazole, drugs known to induce P-gp expression [439],... 

The human malaria parasite Plasmodium falciparum expresses two neutral zinc-aminopeptidases, PfA-Ml and PfA-M17, which function in regulating the intracellular pool of amino acids required for parasite growth and development inside the red blood cell. These enzymes are essential for parasite viability and are validated therapeutic targets. As a result of the rapid emergence of drug-resistant parasites, blocking these peptidases with potent inhibitors has been proposed as a potential new antimalarial therapy. The simple phosphinic dipeptide 61 (Table 1) was reported to inhibit PfA-M17 with a Ki value of 80 nM [130]. 

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