Enzyme inhibitors

N-Methylhydroxylamine hydrochloride is a catalyst commonly used in transamidation. It has radical scavenger abilities as a bacterial growth inhibitor.

It is the oxidised and highly fluorescent analogue of Antibiotic UCN-01 and UCN-02. It is a potent inhibitor of protein kinase C and formation of cellular blebs induced by phorbols. It inhibits the cell cycle at the G2 stage with the accumulation of 4C DNA cells and possesses comparable activity against tumour cells lines to UCN-01.

It is the minor component of a bioactive pigment isolated from Bipolaris cynodontis and Cochliobolus miyabeanus. It is an NADH-ubiquinone reductase inhibitor. It is also a phytotoxic agent inhibiting root growth. It is closely related to cochlioquinone A which inhibits diacylglycerol acyltransferase and exhibits anti-angiogenic and nematocidal activity. It is an antagonist of the human chemokine receptor, CCR5, in HIV-1.

It is an inhibitor of the protease Calpain produced by the strain of Streptomyces sp. SC433. It is a small molecular weight monoketopiperazine formed non-ribosomally by the fusion of phenylalanine and valin.

It is an acid degradation product produced by selective hydrolysis of the terminal saccharide unit of avermectin. It is a potent inhibitor of nematode larval development. It has no paralytic activity.

It is an acid degradation product produced by hydrolysis of the disaccharide unit of avermectin. It is an inhibitor of nematode larval development. It has no paralytic activity. It is an anthelmintic in animal health.

It is a selective inhibitor of type II fatty acid synthesis (FASII) with IC50 values of 11.4 and 35.3 μg/ml in the S. Aureus and E. Coli FASII assays, respectively, with comparable antibacterial activities. It is essential to bacterial cell viability and is a promising target for the development of novel antibiotics. It inhibits agonist binding to liver X receptors (LXR).

It is a 12-membered macrocyclic lactone incorporating a resorcinyl moiety, produced by a number of fungal species including curvularia, penicillium and alternaria. It inhibits cell division by disrupting mitotic spindle formation and acts as a developmental regulator by inhibiting self-sporulation in alternaria alternata.

It is an acid degradation product produced by selective hydrolysis of the terminal saccharide unit of doramectin. It is a potent inhibitor of nematode larval development and an anthelmintic in animal health.

It is an acid degradation product produced by hydrolysis of the disaccharide unit of doramectin. It is an inhibitor of nematode larval development and an anthelmintic in animal health. It has no paralytic activity.

It is a minor isomer of equisetin and a potent inhibitor of HIV-integrase produced by a number of species of Fusarium. It has comparable phytotoxicity to equisetin.

It is an amphoteric, 13-member, linear peptide featuring 3,5-dihydroxyphenylalanine and a terminal dicarboxylate amino acid. It is isolated from Streptomyces sp. DSM 11171. It is a potent antiviral agent with antibacterial activity, including MRSA. It specifically inhibits the enzymes mura and murc. It inhibits cell-to-cell transfer between HIV-infected T cells, uninfected CD4+ T cells, and the DC-SIGN-mediated viral transfer to CD4+ T cells.

It is an unusual pentacyclic metabolite related to equisetin isolated from Fusarium. It is identified from a natural product screen using a three-dimensional matrigel-induced bioassay to study acinar morphogenesis. It is the first inhibitor of acini reported in the literature.

It is one of a family of three butyrolactones isolated from aspergillus fumigatus. It exhibits antitumor activity and inhibits the cell cycle at the G1/S and G2/M transitions. It is a selective inhibitor of cyclin-dependent kinases CDK1/cyclin B, CDK2 and CDK5.

It is a dimeric calcium complex of the major analogue of tetronic acid complex isolated from streptomyces. It inhibits protein tyrosine phosphatases, phospoholipase A2, heparinase and HIV-1 protease.

It is a macrocyclic lactone structurally related to gloeosporone. It is a self-germination inhibitor produced by colletotrichum gloeosporioides. It exhibits moderate antifungal activity.

It is a member of the macrotetrolide complex produced by a range of streptomyces sp. It is a monovalent cation ionophore with high selectivity for ammonium and potassium. Unlike the other macrotetrolides, tetranactin exhibits potent insecticidal activity. It is a glycoprotein transportation inhibitor, an immunosuppressant, an antiproliferative and an antiallergic agent.

A macrocyclic lactone related to hygrolidin but produced by a different streptomyces species. TS155-2 is an inhibitor of calcium entry into the cell induced by thrombin stimulation. It has antihypertensive, antiplatelet, antiischemia and anti-inflammatory activities.

It is a cyclic peptide antifungal metabolite first isolated from the fungus didymocladium ternatum. It is a potent inhibitor of fat accumulation in 3T3-L1 murine adipocytes.

A semi-synthetic macrocyclic lactone prepared from rapamycin by selective alkylation of the 42-hydroxy group. It is one of the most hydrophobic tacrolimus analogues. It binds to the cytosolic FK-binding protein 12 (FKBP12) to inhibit the mammalian target of rapamycin (mTOR) pathway.