Enzyme Modulators

<p>Polmacoxib is a non-steroidal anti-inflammatory drug (NSAID), which is derived through synthetic chemical processes. It functions as a selective cyclooxygenase-2 (COX-2) inhibitor. By selectively inhibiting the COX-2 enzyme, polmacoxib reduces the conversion of arachidonic acid to prostaglandins that mediate inflammation and pain, while sparing the COX-1 enzyme that protects gastric mucosa and maintains platelet function.</p>

<p>Fibroblast growth factor receptor inhibitor</p>

<p>Thalidomide is a piperidinyl isoindole drug that is used to treat various cancers such as myeloma and erythema nodosum leprosum. This drug is immunosuppressive and has anti-angiogenic activity. Thalidomide’s mechanism of action is not fully understood however it is thought to block the activity of tumor necrosis factor-alpha (TNF-α).</p>

<p>A selective VHL inhibitor that stabilizes the hydroxylated form of HIF-α, resulting in upregulation of downstream target genes and proteins. Provides a tool for studying hypoxic signaling pathway.</p>

<p>A small molecule inhibitor with high selectivity for CDK8 over CDK19. Increases IL-10 production in stimulated human and murine macrophages and dendritic cells. Modulatory action on inflammatory responses has therapeutic potential.</p>

<p>Ibandronate is a bisphosphate used in the treatment of osteoporosis in postmenopausal women. This drug slows down the activity of osteoclasts resulting in a slower process of bone breakdown. This drug also inhibits farnesyl diphosphate and induces apoptosis of hematopoietic tumor cells.</p>

<p>Bestatin is a competitive protease inhibitor. It inhibits aminopeptidase N and is being studied for the use and treatment for acute myelocytic leukemia.</p>

<p>Benserazide is a drug that is used for the treatment of Parkinson’s disease and restless leg syndrome. This drug is a decarboxylase inhibitor and is usually used in combination with Levodopa.</p>

<p>Dutasteride is an androgenic compound and a 5α-reductase inhibitor that is used to treat benign prostatic hyperplasia (BPH) and male pattern baldness. Dutasteride reduces prostate volume and improves symptoms of BPH by inhibiting the enzyme 5α-reductase, which converts testosterone to dihydrotestosterone.</p>

<p>Diclofenac is a non-steroidal anti-inflammatory drug that is used to treat the signs and symptoms of arthritis and osteoarthritis. This drug inhibits COX-1 and COX-2 enzymes. As a result, it reduces pain and inflammation in joints. Diclofenac is usually used as a first line therapy for acute and chronic pain.</p>

<p>HMG-CoA reductase inhibitor</p>

<p>Vardenafil is a phosphodiesterase type 5 inhibitor that binds to intracellular targets and competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis thus increasing cGMP levels. Vardenafil can be used for the research of erectile dysfunction, hepatitis and diabetes.</p>

<p>AKTide-2T is a 14-mer peptide which has the ability to bind to the substrate binding domain of Akt1 with a Ki of 12mM. AKt1 is part of the Akt kinase family which are serine/threonine kinase and it is ubiquitously expressed. AKt1 performs roles such as promoting endothelial neoplasms and through phosphorylating angiogenic substrates AKt1 plays a role in angiogenesis. AKT kinases as a whole perform functional roles in cell proliferation, cell growth, survival and intermediary metabolism.During peptide library screening, AKTide-2T was found to contain the optimal motif for successful binding to AKT. When phosphoamino acid analysis of AKTide-2T was carried out it was observed that although AKTide-2T contained two potential AKT phosphorylation sites: serine or threonine, AKT only phosphorylated the serine site. Furthermore it was found that AKTide-2T exhibits properties of being a competitive inhibitor for example it competitively inhibits histone H2B from being phosphorylated by AKT.</p>

<p>PAC 1 is a small-molecule apoptosis inducer, derived from synthetic sources, with a unique mode of action targeting the apoptotic pathways in cancer cells. PAC 1 functions by selectively activating procaspase-3, an inactive precursor of the caspase enzymes, which play a crucial role in the execution phase of cell apoptosis. By facilitating the conversion of procaspase-3 to its active form, PAC 1 enhances the apoptotic response in cancer cells, promoting cell death and offering potential therapeutic advantages.</p>

<p>Inhibitor of PDE4 enzyme; anti-inflammatory</p>

<p>A cell permeable inhibitor of oligosaccharyltransferase that interferes with the transfer of mature glycan precursors to recipient proteins. Causes reduced proliferation, G1 arrest and senescence in EGFR- and FGFR-dependent non-small-cell lung carcinoma (NSCLC) cells.</p>

<p>Proteosome inhibitor; antineoplastic</p>

<p>Pamidronic acid is a bisphosphate used in the treatment of Paget’s disease, osteolytic bone lesions and in the treatment of hypercalcemia of malignancy. This drug inhibits farnesyl diphosphate and induces apoptosis of hematopoietic tumor cells.</p>

<p>Inhibitor of EGFR transmembrane receptor</p>

<p>Inhibitor of cytochrome P450; inhibitor of prostaglandin synthesis</p>