1 |
HIV type 1 integrase |
Acquired immuno-deficiency syndrome |
4000 |
Inhibition of strand transfer activity of HIV-1 integrase |
Mazumder et al. (1997) |
2 |
Tyrosine-protein kinase Lck |
Cancer, autoimmune disorders, chronic inflammatory diseases |
24,000 |
Inhibition of binding to p56 Lck tyrosine kinase SH2 domain |
Park et al. (2003) |
3 |
Matrix metalloproteinase-2 |
Cancer, arthritis, skin aging, blood vessel impairment |
27,200 |
Inhibition of gelatinolytic activity of MMP2 in rat lung homogenate after 40 min by SDS-PAGE preincubated for 30 min |
Murata et al. (2009) |
4 |
Aldose reductase |
Diabetes |
3910 |
Inhibition of aldose reductase |
Koukoulitsa et al. (2010) |
5 |
Tyrosinase |
Skin melanization |
250,000 |
Inhibition of mushroom tyrosinase |
Fujimoto et al. (2010) |
6 |
Transcription factor AP-1 |
Rheumatoid arthritis and cancer |
16,200 |
Inhibition of transcription factor AP-1 binding to oligonucleotide containing TPA-responsive element in TPA-activated human HeLa cells after 1 h |
Chen et al. (2014) |
7 |
Interstitial collagenase |
Rheumatoid arthritis, fibrotic disease |
5600 |
Inhibition of human recombinant MMP1 catalytic domain using Dnp-Pro-beta-cyclohexyl-Ala-Gly-Cys(Me)-His-Lys-(Nma)-NH2 as substrate pre-incubated |
Yuan et al. (2013) |
8 |
Proto-oncogene tyrosine-protein kinase Src |
Cancer |
26,000 |
Inhibition of c-SRC SH2 domain |
Sperl et al. (2009) |
9 |
Estradiol 17-beta-dehydrogenase 2 |
Osteoporosis |
3720 |
Inhibition of human 17beta-HSD2 expressed in HEK293 cell lysates incubated for 10 min using [2,4,6,7-3H]-estradiol and NAD + by scintillation |
Vuorinen et al. (2017) |
10 |
Beta amyloid A4 protein |
Alzheimer’s disease |
71,900 |
Inhibition of amyloid beta (1 to 42 residues) (unknown origin) aggregation after 24 h by thioflavin T assay |
Kwon et al. (2015) |
11 |
Reverse transcriptase |
Acquired immuno-deficiency syndrome |
100,000 |
Inhibition of HIV1 reverse transcriptase |
Dubois et al. (2008) |
12 |
Integrase |
Acquired immuno-deficiency syndrome |
63,500 |
Inhibition of HIV1 integrase using labelled oligonucleotide substrate in presence of bovine serum albumin by ELISA |
Dubois et al. (2008) |
13 |
Aldose reductase |
Diabetes complications |
3890 |
Inhibition of Rattus norvegicus (rat) lens aldose reductase |
Jain et al. (2012) |
14 |
Tyrosine-protein kinase Fyn |
Neurodegenerative disease |
1300 |
Inhibition of human Fyn expressed in Sf9 cells after 20 min by ELISA in presence of 1 umol/L ATP |
Jelić et al. (2007) |
15 |
Lipoxygenase |
Cancer, asthma, inflammatory disease |
1,150,000 |
Inhibition of soybean lipoxygenase in vitro. Binding energy and IC-50 calculated to detect inhibitory activity |
Koukoulitsa et al. (2007) |
16 |
MARK-4 |
Cancer |
6200 |
Inhibition of MARK-4 validated in cell-free and cell-based enzyme assay. Increased apoptosis in MARK-4 overexpressing cancer cells |
Anwar et al. (2020) |
17 |
Glycogen Synthase kinase 3β |
Alzheimer’s disease |
135 |
Inhibition of GSK-3 β enzyme involved in several human diseases |
Paudel et al. (2018) |