Enzyme inhibitors

CGP049090 is a novel inhibitor of Wnt/beta-catenin/lef-1 signaling inducing apoptosis in chronic lymphocytic leukemia cells in vitro and in vivo.

Hexadecylpyridinium bromide is a pyridinium salt that has N-hexadecylpyridinium as the cation and bromide as the anion. It has a role as a surfactant, an antiseptic drug and an EC 2.7.11.18 (myosin-light-chain kinase) inhibitor. It is a pyridinium salt and a bromide salt.

A tetrahydropyrimidine used as an oral anthelmintic in the veterinary medicine sector.

Dihydroergocristine Mesylate, an ergotamine derivative, has been found to be a 5-HT receptor antagonist and exhibit protective activities to the brain at some extent.

TAN 1364B is a tetronic acid analogue isolated from Streptomyces species. It can inhibit protein tyrosine phosphatase, phospholipase A2, heparinase and HIV-1 protease.

Paraoxamide A is a mycotoxin derived from the fungus Penicillium. Paraherquamide A is a selective, competitive, cholinergic antagonist that distinguishes subtypes of cholinergic receptors. The structure of parherquamide, a toxic metabolite from Penicillium paraherquei.

Terphenyllin is a naturally abundant p-terphenyl metabolite isolated from the coral derived fungus Aspergillus candidus, has significant α-glucosidase inhibitory activity.

Thiourea B is a fungal metabolite that contains O-substituted salicylic acid. It is a fungal metabolite closely related to thiobactin A. It is an effective inhibitor of phospholipase C, which can inhibit the formation of peptidoglycan and the biosynthesis of prostaglandin.

Altertoxin I, a sort of natural mycotoxin, could be obtained from Alternaria fungi and has been found to restrain human topoisomerase II as well as bacterial gyrase. Altertoxin I (and other altertoxins) inhibit the HIV replication.

Amodiaquine, a 4-aminoquinoquinoline compound, is a histamine N-methyltransferase inhibitor, used as an antimalarial and anti-inflammatory agent for more than 40 years.

Sulbactam is a β-lactamase inhibitor. This drug is given in combination with β-lactam antibiotics to inhibit β-lactamase, an enzyme produced by bacteria that destroys the antibiotics.

Alizarin strongly inhibits P450 isoform CYP1A1, CYP1A2 and CYP1B1 with IC50 of 6.2 μM, 10.0 μM and 2.7 μM, respectively; weakly inhibits CYP2A6 and CYP2E1, and does not inhibit CYP2C19, CYP3A4 and CYP3A5.

Acriflavine Hydrochloride is an inhibitor of HIF-1α. Acriflavine is a topical antiseptic agent and has also been used for the treatment of external fungal infections.

Tazobactam acid is a pharmaceutical drug that inhibits the action of bacterial β-lactamases, especially those belonging to the SHV-1 and TEM groups. It is commonly used as the sodium salt. It is derived from the penicillin nucleus and is a penicillinic acid sulfone. It is used with β-lactam antibiotics to enhance their effect. It has antibacterial activity.

Aranorosin is a fungal metabolite originally isolated from P. roseus and an inhibitor of anti-apoptotic functions regulated by Bcl-2. It has antimicrobial activity against B. subtilis, A. niger, and C. albicans when used at a concentration of 1 mg/ml. Aranorosin also reduces viability in apoptosis-resistant HeLa/Bcl-2 cells. Aranorosin also inhibits enzyme AAC(6')/APH(2'') which plays a role in arbekacin (ABK)-resistance in MRSA.

Aspochalasin D is a potent inhibitor of mammalian tumor cell lines, first isolated from Aspergillus microcysticus. It has antibacterial activity against Gram-positive and Gram-negative bacteria at a concentration of 1 mg/ml. Aspochalasin D was found that it can strongly induce the formation of actin-containing rodlets in the cytoplasm of treated fibroblasts.

Mycophenolate Mofetil is a non-competitive, selective and reversible inhibitor of inosine monophosphate dehydrogenase I/II with IC50 of 39 nM and 27 nM, respectively.

Pseurotin A is a secondary metabolite of Aspergillus. It has effective neurogenesis activity in PC12 pheochromocytoma cells, induces multipolar and branched neurites equivalent to β-NGF (an endogenous neurotrophic factor), and also exhibits chitinase inhibition. And it has a synergistic effect with azole antifungal agents.

Sonolisib, also known as PX-866, is a small-molecule wortmannin analogue inhibitor of the alpha, gamma, and delta isoforms of phosphoinositide 3-kinase (PI3K) with potential antineoplastic activity. PI3K inhibitor PX-866 inhibits the production of the secondary messenger phosphatidylinositol-3,4,5-trisphosphate (PIP3) and activation of the PI3K/Akt signaling pathway, which may result in inhibition of tumor cell growth and survival in susceptible tumor cell populations. Activation of the PI3K/Akt signaling pathway is frequently associated with tumorigenesis and dysregulated PI3K/Akt signaling may contribute to tumor resistance to a variety of antineoplastic agents.

Luzopeptin A is a cyclic depsipeptide antibiotic produced by an actinomycete strain. It has anti-tumor activity. It is a potent inhibitor of HIV-1 reverse transcriptase.