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Chimeric small molecule therapeutics are a class of drugs designed with multiple active domains to operate outside of the typical protein inhibition model. While most small molecule drugs inhibit target proteins by binding their active site, chimerics form protein-protein ternary structures to induce degradation or, less frequently, other protein modifications.
Image illustrates DNA, RNA, and protein synthesis. The first two are nucleic acids. A nucleic acid inhibitor is a type of antibacterial that acts by inhibiting the production of nucleic acids. There are two major classes: DNA inhibitors and RNA inhibitors. [1] The antifungal flucytosine acts in a similar manner.
The structure of paclitaxel, a widely used mitotic inhibitor. A mitotic inhibitor, microtubule inhibitor, or tubulin inhibitor, is a drug that inhibits mitosis, or cell division, and is used in treating cancer, gout, and nail fungus. These drugs disrupt microtubules, which are structures that pull the chromosomes apart when
A protein kinase inhibitor (PKI) is a type of enzyme inhibitor that blocks the action of one or more protein kinases. [1] Protein kinases are enzymes that phosphorylate (add a phosphate, or PO 4, group) to a protein and can modulate its function. [2] The phosphate groups are usually added to serine, threonine, or tyrosine amino acids on the
Compared to traditional inhibitors, PROTACs display multiple benefits that make them desirable drug candidates. Due to their catalytic mechanism, PROTACs can be administered at lower doses compared to their inhibitor analogues, [ 20 ] though care needs to be taken in achieving oral bioavailability if administered by that route. [ 24 ]
Irreversible inhibitors are generally specific for one class of enzyme and do not inactivate all proteins; they do not function by destroying protein structure but by specifically altering the active site of their target. For example, extremes of pH or temperature usually cause denaturation of all protein structure, but this is a non-specific ...
Kunitz domains are the active domains of proteins that inhibit the function of protein degrading enzymes or, more specifically, domains of Kunitz-type are protease inhibitors. They are relatively small with a length of about 50 to 60 amino acids and a molecular weight of 6 kDa .
Pharmacological myostatin inhibitors can therefore be considered exercise mimetics. [7] Creatine, a popular workout supplement, has shown some myostatin inhibitory effects in preclinical studies. [6] Many drugs in development as myostatin inhibitors also reduce the activity of related proteins such as GDF11, activins, and bone morphogenetic ...