Modulatori enzimatici

<p>A potent Met kinase inhibitor (IC50 = 3.9 nM). Also inhibits Axl, Ron, and Tyro-3 (IC50 = 1.1, 1.8 and 4.3 nM, respectively). Anti-proliferative in Met-driven tumors in vitro and in vivo. Induces polyploidy in breast cancer cells and thereby chemoresistance.</p>

<p>Inhibitor of vacuolar ATP-ases</p>

Inhibitor of ALK4, ALK5, and ALK7 receptors

<p>Inhibits factor Xa; anti-thrombotic</p>

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

<p>Dihydrocyclosporin A is an immunosuppressant, which is a cyclic undecapeptide derived from fungal metabolites, specifically from the soil fungus Tolypocladium inflatum. This compound functions through the inhibition of calcineurin, which is a crucial phosphatase involved in the activation of T-cells. By binding to the intracellular protein cyclophilin, Dihydrocyclosporin A forms a complex that inhibits calcineurin activity, subsequently blocking the transcription of interleukin-2 and other cytokines essential for T-cell proliferation.</p>

<p>JAK2 inhibitor with potential antineoplastic activity</p>

<p>Inhibits MET, VEGFR2, Ron, AXL, Tie-2, Flt-1, Flt-3 and Flt-4 tyrosine kinases</p>

<p>Lifirafenib is a targeted anticancer therapy, which is a small molecule inhibitor sourced through pharmaceutical development processes. Its mode of action involves the selective inhibition of the RAF kinase family, including B-RAF, which plays a critical role in the MAPK/ERK signaling pathway. By targeting these kinases, Lifirafenib effectively disrupts the aberrant signaling that contributes to tumor growth and survival in certain cancers with mutations such as BRAF V600E.</p>

<p>Multi-kinase inhibitor; inhibits epoxide hydrolase; antineoplastic</p>

<p>Spirapril hydrochloride is an antihypertensive agent, which is a synthetic pharmaceutical compound designed to treat high blood pressure. The compound is derived from laboratory synthesis aimed at modulating the renin-angiotensin-aldosterone system. Its mode of action involves the inhibition of angiotensin-converting enzyme (ACE), which is crucial for the conversion of angiotensin I to the vasoconstrictor peptide angiotensin II. Angiotensin II is responsible for the constriction of blood vessels and an increase in blood pressure. By inhibiting this enzyme, Spirapril hydrochloride effectively reduces vascular resistance and lowers blood pressure.</p>

Inhibitor of Polo-like kinase 1

<p>Sorafenib is a drug that belongs to the class of multikinase inhibitors. It inhibits a number of kinases, including the Mcl-1 protein, which is involved in apoptosis along with blocking picolinic acid (PA), an endogenous metabolite involved in apoptosis signal transduction. Sorafenib also binds to epidermal growth factor receptor (EGFR) on the surface of cancer cells, inhibiting the production of proteins that are required for angiogenesis, thus blocking the formation of new blood vessels. Sorafenib may also inhibit P-glycoprotein (Pgp) activity. Overall, these cytotoxic effects give Sorafenib anti-tumor properties, inhibiting angiogenesis and cellular transformation, which are the two main processes of tumor growth and metastasis. Sorafenib has been shown to be effective against a range of solid tumors such as breast, prostate and lung cancers and is also used for the treatment of metastatic colorectal cancer and renal cell carcinoma. A combination therapy group found that sorafenib was more effective when used with interferon alfa-2b for the treatment of advanced renal cell carcinoma. Sorafenib also has the potential for drug interactions with other drugs that are metabolized by cytochrome P450 enzymes.</p>

Inhibitor of B-Raf mutant (V600E); anti-neoplastic

<p>TPPB is a small molecule inhibitor, which is synthetically derived for targeted biochemical studies. It functions by selectively modulating G-protein-coupled receptor (GPCR) signaling pathways through the inhibition of specific protein-protein interactions. This mode of action makes TPPB an insightful tool for dissecting the complex mechanisms by which G-proteins relay extracellular signals to intracellular responses.</p>

<p>Inhibitor of Bruton's tyrosine kinase (BTK)</p>

<p>Synthetic phosphodiesterase inhibitor</p>

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

<p>Pemetrexed is a chemotherapy drug that belongs to the class of drugs called folate antimetabolites. It is used for the treatment of various cancers such as non-small cell lung cancer and pleural mesothelioma. Pemetrexed targets the enzymes thymidylate synthase, dihydrofolate reductase and glycinamide ribonucleotide formyltransferase. The drug works by inhibiting those enzymes so that the formation of DNA and RNA is prevented.</p>

Inhibitor of EGFR (ErbB1) and HER2 (ErbB2) receptor tyrosine kinases. Used for sensitization of HER2-overexpressing cancer cells to radiation as well as chemotherapy to tamoxifen- and trastuzumab-resistant cell lines. The compound blocks signalling via Akt and mitogen-activated protein kinase (MAPK) pathways leading to reduced cell survival. In trastuzumab resistant cancer cells, it inhibits HER2 phosphorylation, prevents receptor ubiquitination and causes accumulation of inactive HER2 dimers on the cell surface.