Enzyme inhibitors

It is produced by the strain of Streptomyces californicus KS-619-1. KS-619-1 inhibited Ca2+ and CAM-PDE in bovine brain and heart with an IC50 of 2.0 and 1.5 μmol/L.

L-681176 is originally isolated from Streptomyces sp. MA 5143a. It has the activity of inhibiting angiotensin transferase.

L 687781, an inhibitor of β-1,3-D-glucan synthase, is originally isolated from Dictyochaeta simplex. It also has anti-Candida fungal activity and has some effects on Pneumocystis carinii.

L-696474 is extracted from Hypoxylon fragiforme MF5511. It can competitively inhibit the action of HIV-1 protease with an IC50 of 3 μmol/L.

Mer-N5075A, an HIV-1 protease inhibitor, is originally isolated from Streptomyces chromofuscus. Its IC50 of inhibiting HIV-1 protease was 17.8 μmol/L.

Mer NF5003B is extracted from Stachybotrys sp. Mer-NF-5003. It has the activity of inhibiting avian myeloblastic leukemia virus (AMV) protease.

It has the activity of inhibiting HMG-CoA reductase, and it is produced by the strain of Penicillum citrinum SANK.

MLR-52, extracted from Streptomyces sp. AB 1869R-359, is an immunosuppressive protein kinase C inhibitor. And the IC50 (nmol/L) of the mixed lymphocyte response test was 1.9±0.2.

MR-387-A is an AP-N inhibitor produced by the strain of Streptomyces neyagawaensis SL-387. It is used to inhibit AP-N activity in cells derived from porcine kidney microsomes, human fibrosarcoma HT-1080 and human myeloid leukemia K562.

MR-387-B is an AP-N inhibitor produced by the strain of Streptomyces neyagawaensis SL-387. It is used to inhibit AP-N activity in cells derived from porcine kidney microsomes, human fibrosarcoma HT-1080 and human myeloid leukemia K562.

It is produced by the strain of Trichoderma harzianus KCTC 0114BP. MR-566A inhibited mushroom enzyminase and melanin biosynthesis in B16 melanoma cells with IC50 (μmol/L) of 1.72 and 0.1, respectively.

It is produced by the strain of Trichoderma harzianus KCTC 0114BP. MR-566B inhibited mushroom enzyminase and melanin biosynthesis in B16 melanoma cells with IC50 (μmol/L) of 47 and 2.2, respectively.

MS-282a is produced by the strain of Streptomyces tauricus. It inhibits calmodulin-dependent MLCK with an IC50 of 3.8 μmol/L. It has anti-gram-positive bacteria activity.

MS-282b is produced by the strain of Streptomyces tauricus. It inhibits calmodulin-dependent MLCK with an IC50 of 5.2 μmol/L. It has anti-gram-positive bacteria activity.

MS-444, originally isolated from Micromonospora sp. KY7123, is a myosin light chain kinase (MLCK) inhibitor.

MS-681a, originally isolated from Myrothecium sp. KY6568, is a myosin light chain kinase (MLCK) inhibitor (IC50=0.11 μmol/L).

FR-901537, a naphthothiazin compound, has been found to be an aromatase inhibitor that could be used as a cytostatic antibiotic and was once studied in breast cancer.

It is originally isolated from Aspergillus fumigatus F93. GERI-BP002-A inhibits ACTC with an IC50 of 50 μmol/L.

A staurosporine analogue isolated from a nocardiopsis strain; a potent inhibitor of protein kinase C. K-252b exhibits potent antitumour activity but shows no antimicrobial activity in vitro, or in vivo toxicity in rodents; also active against other kinases, notably myosin light chain kinase, camp-dependent protein kinase (PKA), protein kinase C (PKC) and cgmp-dependent protein kinase (PKG).

K252c, a metabolite product of Nocardiopsis Sp., has been found to be a protein kinase C inhibitor and exhibit antiviral activities against GCV-sensitive and-resistant strains at some extent.