Modulateurs d'enzymes

Inhibitor of dipeptidyl peptidase IV; anti-diabetic agent

Inhibitor of dopamine-?-hydroxylase

Zoledronic acid is a drug that is used for the treatment of malignancy associated with hypercalcemia and bone metastasis from tumors. This drug induces apoptosis pf hematopoietic tumor cells by inhibiting farnesyl diphosphate. Zoledronic acid is a bisphosphate that inhibits osteoclast function and bone resorption.

Inhibitor of fibroblast growth factor receptors (FGFR1, FGFR2 and FGFR3). Demonstrated anti-tumor effects in pre-clinical models of FGFR-driven tumors. AZD 4547 resulted in tumor progression when applied on a patient-derived model of FGFR1-amplified squamous cell lung disease. Antineoplastic effects also observed in FGFR2-amplified gastric cancer.

Ibuprofen is a non-steroidal anti-inflammatory drug (NSAID) used to reduce inflammation, relieve pain and reduce fever. The mechanism of action of ibuprofen has not been fully elucidated, but it may be due to inhibiting the enzyme cyclooxygenase and thus decreasing the synthesis of prostaglandins allowing a reduction of pain and inflammation.

Dasatinib is a potent inhibitor of tyrosine kinases and is used in the treatment of chronic myelogenous leukemia, gastrointestinal stromal tumors, and other types of cancer. It also inhibits many SRC- family kinases. Dasatinib has been shown to inhibit the proliferation of cancer cells, leading to cell lysis. Additionally, it has anti-angiogenic effects in vivo, inhibiting the development of new blood vessels in solid tumours.

Inhibitor of BCR-ABL1 kinase

Sunitinib is a tyrosine kinase inhibitor drug. It is a drug that is used as a treatment for renal cell carcinoma, gastrointestinal stromal tumor, and other solid tumors. This drug inhibits tyrosine kinases such as VEGFRs, this prevents tumour growth and pathologic angiogenesis.

PD 168393 is a potent and selective irreversible inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase. It is synthesized through advanced chemical processes, designed to specifically target and covalently modify the ATP-binding site of EGFR. The mode of action involves the irreversible binding to the cysteine residue in the ATP-binding pocket, leading to the inhibition of EGFR autophosphorylation and subsequent downstream signaling pathways.

Inhibitor of glutaminase; glutamine analogue

Potent and selective GSK3-β inhibitor, with IC50 value of 48 nM. Increases Nanog expression and regulates self-renewal in murine embryonic stem cells (ESCs). Induces reprograming of induced pluripotent stem cells (iPSCs) to derive cells from specific lineages.

Nintedanib is an anti-inflammatory and anti-cancer drug. It is used for treatment of idiopathic pulmonary fibrosis. Nintedanib is a prodrug that is rapidly converted to the active form nintedanib, which inhibits angiogenesis by interfering with the activation of vascular endothelial growth factor receptor 1 (VEGFR1). 
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Arbutin or alpha-arbutin is a natural product. It is a hydroquinone glucoside with antioxidant properties. It is widely used in cosmetics as depigmenting agent, acting as an inhibitor of tyrosinase in melanocytes. Arbutin acts by supressing the enzymes that stimulate these melanocytes without killing or fully inhibiting them. As a consequence, melanin production is decreased to avoid hyperpigmentation that might be caused by an excess of UV radiation or a higher activity of tyrosinases.

Inhibitor of panPI3K/mTOR

HIF prolyl-hydroxylase inhibitor for treatment of anaemia

Inhibitor of LRRK2 kinase

Inhibits VEGFR1, VEGFR2, VEGFR3, c-kit and PDGFR tyrosine kinases

A potent ATP-competitive inhibitor of tropomyosin-related kinases (TRK1, TRK2 and TRK3), members of the receptor tyrosine kinase family of neurotrophin receptors. Tumors with oncogenic TRK fusions are sensitive to larotrectinib, leading to reduced proliferation and tumor growth in patients with soft tissue sarcoma, triple-negative breast cancer and lung cancer.

Vildagliptin is an antihyperglycemic agent that is used for the management of type 2 diabetes mellitus. This drug is a dipeptidyl peptidase 4 inhibitor and prevents the degradation of glucagon-like peptide 1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). This leads to improved glycemic control.

Inhibitor of CK2 protein kinase; anti-proliferative