Modulateurs d'enzymes

<p>p38α MAP kinase inhibitor; JNK2α2 protein kinase inhibitor</p>

<p>p38 MAP kinase antagonist</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>Inhibitor of CKD1, CDK2, and CDK4 serine/threonine kinases</p>

<p>Glucokinase activator</p>

<p>First generation PI 3-kinase inhibitor</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>Sildenafil is a pharmaceutical compound, which is a synthetic product derived from chemical processes. It functions as a selective inhibitor of the enzyme phosphodiesterase type 5 (PDE5). By inhibiting PDE5, sildenafil increases cyclic guanosine monophosphate (cGMP) levels within the smooth muscle cells of the corpus cavernosum. This leads to smooth muscle relaxation and vasodilation, allowing increased blood flow and facilitating penile erection in the presence of sexual stimulation.</p>

<p>Inhibitor of Janus kinase JAK-1</p>

<p>N-(5-Aminopentyl) methotrexate amide-LC-biotin is a specialized bioconjugate, derived through the conjugation of methotrexate, an established antifolate drug, with an LC-biotin moiety. This product is synthesized by covalently linking methotrexate, which is known for its role in cancer therapy through the inhibition of dihydrofolate reductase (DHFR), to a biotin moiety via a long-chain spacer. The resultant bioconjugate retains the therapeutic effects of methotrexate, particularly in its ability to interrupt nucleotide synthesis, thereby affecting cell division in rapidly proliferating cancer cells.The inclusion of biotin in the structure allows for facile attachment to avidin or streptavidin-labeled systems, facilitating targeted delivery and enhanced detection in molecular and cellular studies. The primary application of N-(5-Aminopentyl) methotrexate amide-LC-biotin lies in the realm of targeted drug delivery and advanced research into methotrexate metabolism. By leveraging the high affinity of biotin-streptavidin interactions, researchers can effectively study the biodistribution and cellular uptake of methotrexate, advancing cancer therapeutic strategies and providing insights into antifolate drug mechanisms at the molecular level.</p>

<p>CAY10727 is a potent biochemical inhibitor, which is derived from synthetic sources with specific action targeting cyclooxygenase-2 (COX-2) enzymes. It functions by selectively blocking the enzymatic activity of COX-2, which plays a critical role in the biosynthesis of prostaglandins involved in inflammatory responses. This targeted inhibition allows the study of COX-2-related pathways without interference from COX-1, which is significant for maintaining gastrointestinal integrity.The use and applications of CAY10727 are primarily in research settings where understanding the pathways involved in inflammation, pain, and cancer progression are critical. This compound is utilized in various in vitro experiments to delineate the role of COX-2 in cellular and molecular contexts, enabling scientists to dissect complex signaling networks. Given its specificity, CAY10727 is instrumental in the development of new therapeutic approaches where selective COX-2 inhibition might offer benefits over non-selective inhibitors.</p>

<p>Inhibitor of cyclin dependend kinases</p>

<p>A potent small-molecule activator of UNC-51-like kinase 1 (ULK1), a serine-threonine kinase involved in autophagy. Promotes cytoprotective autophagy in MPP+-treated SH-SY5Y cells, via the ULK complex. Improves motor dysfunction and reduces loss of dopaminergic neurons, mediated by MPTP, in in vivo models of Parkinson’s disease.</p>