Enzyme inhibitors

Miltefosine inhibits PI3K/Akt activity with ED50 of 17.2 μM and 8.1 μM in carcinoma cell lines A431 and HeLa, first oral drug for Visceral leishmaniasis, effective against both promastigotes and amastigotes.

Atpenin A5 is an inhibitor of SDHB, SDHC and SDHD. It is an antifungal antibiotic produced by Penicillium sp. and an ubiquinone-binding site inhibitor of succinate dehydrogenase with IC50s of 12 nM for nematode and IC50s of 3.7 nM for mammalian mitochondria. Atpenin A5 is the most effective inhibitor against complex II from all the atpenins and has been shown to protect against cardiac-reperfusion injury in rat studies through the stimulation of mitochondrial KATP channels.

Icotinib Hydrochloride is a quinazoline-based inhibitor of epidermal growth factor receptor (EGFR), which is upregulated in a variety of cancer cell types. Icotinib supresses the cancer cell proliferation via EGFR tyrosine kinase inhibition.

Gefitinib is an antineoplastic drug. Gefitinib effectively inhibits all tyrosine phosphorylation sites on EGFR in both the high and low EGFR-expressing cell lines including NR6, NR6M and NR6W cell lines. The phosphorylation sites Tyr1173 and Tyr992 are less sensitive requiring higher concentrations of Gefitinib for inhibition.

Melittin is a polypeptide isolated from the venom of the honey bee (Apis mellifera). It inhibits protein kinase C, Ca2+/calmodulin-dependent protein kinase II, myosin light chain kinase and Na+/K+-ATPase (synaptosomal membrane).

It is produced by the strain of Streptomyces griseus ssp. sulphurus TU 1022 and Str. griseus TU 2437. Bafilomycin A1 is a vacuolar H+-ATPase inhibitor with IC50 of 0.44 nM. It can inhibit the growth of gram-positive bacteria, negative bacteria, fungi, yeast and protozoa, and has the effects of insect killing, nematode killing and immunosuppression.

Temsirolimus is an mTOR inhibitor produced by Streptomyces. Temsirolimus potently inhibits mTOR kinase activity with IC50 of 1.76 μM, similar to that of rapamycin with IC50 of 1.74 μM.

Epirubicin HCl, a semisynthetic L-arabino derivative of doxorubicin, is an antineoplastic agent by inhibiting Topoisomerase.

Mupirocin is an isoleucyl t-RNA synthetase inhibitor, used in the treatment of bacterial skin infections.

Tacrolimus monohydrate is a potent immunosuppressive drug often administered to transplant recipient patients and exhibits a variety of adverse cardiovascular effects.

Pimecrolimus is an immunomodulator of calcineurin inhibitors produced by Streptomyces.

Orlistat is a pancreatic lipase inhibitor acting locally in the gastrointestinal tract to inhibit lipase. It is commonly used as a weight loss agent.

Micafungin Sodium is an inhibitor of 1,3-beta-D-glucan synthesis, used as an antifungal drug.

It is produced by the strain of Penicillum brevicompactum. It has weak anti-fungal activity and can inhibit the key enzyme (3-hydroxy-3-methyl glutaryl coenzyme A(HMGCoA) reductase) in the cholesterol biosynthesis pathway. It has been shown to lower cholesterol in animals and humans. It led the discovery of statins, lipid-lowering drugs. It is now used as a biochemical reagent.

Marizomib is a naturally-occurring salinosporamide, isolated from the marine actinomycete Salinospora tropica, with potential antineoplastic activity. Marizomib irreversibly binds to and inhibits the 20S catalytic core subunit of the proteasome by covalently modifying its active site threonine residues.

Artemisinin is a natural product originally isolated from plants of the genus Artemisia. It effectively kills malarial parasites of the genus Plasmodium. It is usually used in combination therapy for the treatment of malaria. Artemisinin is also used against a wide range of trematodes, including Schistosoma. Artemisinin is an inhibitor of human NOS2 (iNOS) with anticancer activity.

Emodin is an anthraquinone found naturally in the roots and barks of numerous plants. It exerts antiproliferative effects in cancer cells that are regulated by different signaling pathways. It has anti-cancer, anti-depressant and anti-microbial effects.

Embelin, a quinone isolated from the Japanese Ardisia herb, is an inhibitor of X-linked inhibitor of apoptosis (XIAP) with IC50 of 4.1 uM.

Naringenin is an estrogen receptor binding inhibitor produced by Streptomyces graminofaciens BA 14348.

Baicalin is a flavone found in several species in the genus Scutellaria, including Scutellaria baicalensis and Scutellaria lateriflora. Baicalin is a positive allosteric modulator of the benzodiazepine site and/or a non-benzodiazepine site of the GABA receptor. Baicalin can also absorb ultraviolet rays, scavenge oxygen free radicals, and inhibit the production of melanin. Therefore, it can be used in medicine and cosmetics. It is a good functional cosmetic raw material.