Modulateurs d'enzymes

<p>Inhibitor of ADAM10 metalloprotease</p>

<p>Inhibitor of ALK4, ALK5, and ALK7 receptors</p>

<p>Inhibitor of calpain and cathepsin B</p>

<p>Inhibitor of B-Raf mutant (V600E); anti-neoplastic</p>

<p>Cyclin-dependent kinase 8 (CDK8) and CDK19 inhibitor</p>

<p>Inositol monophosphatase (IMPase) inhibitor</p>

<p>N-alpha-Benzoyl-L-argininamide is a synthetic compound that is used as an enzyme inhibitor. It binds to the active site of proteases, thereby inhibiting their activity. This drug has been shown to inhibit the activities of phosphodiesterase and phosphatase enzymes in vitro. N-alpha-Benzoyl-L-argininamide also inhibits the proteolytic degradation of hippuric acid and casein in vitro. The binding affinity for this drug is due to its structural similarity with substrates such as glutamate and rhizosphere exudates.</p>

<p>Methotrexate is a drug that suppresses the immune system by inhibiting the production of white blood cells. It is used in the treatment of a number of diseases, including some cancers and autoimmune diseases such as rheumatoid arthritis and psoriasis. Methotrexate is metabolized to its active form, methotrexate, by an enzyme called dihydrofolate reductase (DHFR). The DHFR inhibitor activity of methotrexate blocks the synthesis of folate-dependent enzymes and prevents DNA synthesis in rapidly dividing cells. Methotrexate has been used in combination with other drugs to treat cancer. Methotrexate has also been shown to have antifungal properties against opportunistic fungal infections.</p>

<p>Antagonist of Aurora A serine/threonine protein kinase; antineoplastic</p>

<p>TDZD 8 is a selective, non-ATP competitive inhibitor of the glycogen synthase kinase GSK3β. TDZD 8 inhibits GSK3β with IC50 of 2 μM and was reported to not significantly affect Cdk-1/cyclin B, casein kinase CK-II, protein kinase A and C (PKA, PKC) activities. TDZD 8 was also identified as an inhibitor of the main protease in coronaviruses. In an in vitro study, TDZD 8 was characterised as an aggregate-based inhibitor as the presence of Triton-X decreased the inhibitory potency to Mpro protease of the SARS-CoV-2 virus (IC50 without Triton-X: 2.15 μM).</p>

<p>BIBF 1202 is a potent inhibitor of phospholipase A2, prostaglandin synthase and cyclooxygenase-2. It inhibits the production of arachidonic acid from membrane phospholipids and is used in cancer research. BIBF 1202 has been shown to have anti-tumour activity in a number of animal models, including human liver cancer cells. This molecule has also been shown to inhibit the activation of nuclear factor kappa B (NF-κB), which is involved in carcinogenesis.</p>

<p>H-9 hydrochloride is a selective protein kinase inhibitor, which is synthetically derived. It primarily inhibits cyclic nucleotide-dependent protein kinases, including protein kinase A (PKA) and protein kinase G (PKG), along with myosin light chain kinase (MLCK). The mode of action involves competitive inhibition at the ATP binding site of these kinases, thereby impacting phosphorylation pathways crucial for multiple physiological functions. The selective inhibition by H-9 hydrochloride allows for detailed exploration of kinase-mediated signaling pathways in cellular biology. Moreover, it is extensively utilized in studies involving cell motility, smooth muscle contraction, and signal transduction. The relevance of H-9 hydrochloride in academic research lies in its ability to provide insights into kinase activity modulation and its ensuing effects on cellular dynamics. This compound serves as an invaluable tool for scientists aiming to elucidate the complex role of protein kinases in health and disease, enabling the development of innovative therapeutic strategies.</p>

<p>Rosuvastatin is a synthetic lipid-lowering agent, which is a product of pharmaceutical manufacturing derived from extensive research in cardiovascular pharmacology. It functions as an HMG-CoA reductase inhibitor, effectively blocking the enzyme responsible for cholesterol biosynthesis in the liver. By inhibiting this enzyme, Rosuvastatin reduces the production of cholesterol, especially low-density lipoprotein (LDL) cholesterol, which is known to contribute to atherosclerosis.</p>

<p>Odevixibat is a pharmacological agent that functions as an ileal bile acid transport inhibitor, which is synthesized through complex organic chemistry methods to create a specific molecular structure targeting bile acid transport mechanisms. It works by inhibiting the apical sodium-dependent bile acid transporter (ASBT) in the terminal ileum. This action reduces the reabsorption of bile acids from the small intestine back into the liver, thereby reducing overall bile acid levels in the body.</p>

<p>Cyclosporine U is a cyclic polypeptide immunosuppressant, which is a derivative of the natural product Cyclosporine A, produced by the fermentation process involving the filamentous fungus *Tolypocladium inflatum*. It primarily acts by inhibiting the activity of calcineurin, a phosphatase enzyme, which in turn blocks the transcription of interleukin-2 and other cytokines. This mechanism suppresses the activation of T-lymphocytes, a crucial component in the immune response.</p>

<p>Inhibitor of GSK3β kinase</p>

<p>Anti-parasitic; pyruvate ferredoxin oxidoreductase inhibitor</p>

<p>Inhibitor of EGFR, HER2 and HER4 tyrosine kinases</p>

<p>Glucokinase activator</p>

<p>Cyclosporin G is an immunosuppressive agent, which is derived from fungal sources with a specific mode of action that involves inhibiting calcineurin. The source of Cyclosporin G is primarily from the fermentation of the fungus *Tolypocladium inflatum*. Its mode of action involves binding to the cytosolic protein cyclophilin in T-lymphocytes, which subsequently inhibits the phosphatase activity of calcineurin. This inhibition prevents the dephosphorylation and nuclear translocation of the nuclear factor of activated T-cells (NFAT), thereby reducing the transcription of interleukin-2 and other cytokines critical for T-cell activation.</p>