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. 2022 Apr 7;45(4):205–228. doi: 10.1007/s12272-022-01378-2

Table 1.

Enzyme Inhibition Constant Data of RA from Binding DB

S. No Target Disease IC50 (nM) Assay description Reference
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)