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Drug-Target Interaction

Drug

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PubChem ID:479503
Structure:
Synonyms:
1,4-Naphthalenedione,
1,4-Naphthalenedione, 5,8-dihydroxy-2-[(1R)-1-hydroxy-4-methyl-3-pentenyl]-
5,8-Dihydroxy-2-((R)-1-hydroxy-4-methyl-pent-3-enyl)-[1,4]naphthoquinone
5,8-dihydroxy-2-[(1r)-1-hydroxy-4-methylpent-3-en-1-yl]-1,4-naphthoquinone
517-89-5
AC-11205
AC1LA0SH
AC1Q6B9B
AIDS-094462
AIDS094462
Ambap5024
AR-1G6415
BSPBio_001270
C17412
CHEBI:105268
CHEMBL9470
HMS1792P11
HMS1990P11
HMS2089L09
Isoarnebin 4
NCGC00163489-01
NCGC00163489-02
NSC252844
SBB066976
Shikonin
Tokyo Violet
ZINC02015152

Target

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Uniprot ID:CASP3_MOUSE
Synonyms:
Apopain
CASP-3
Caspase-3
CPP-32
Cysteine protease CPP32
LICE
SCA-1
SREBP cleavage activity 1
Yama protein
EC-Numbers:3.4.22.56
Organism:Mouse
Mus musculus
PDB IDs:-

Binding Affinities:

Ki: Kd:Ic 50:Ec50/Ic50:
----

References:

15224412
Shikonin regulates HeLa cell death via caspase-3 activation and blockage of DNA synthesis.. Zhen Wu; Li-Jun Wu; Lin-Hao Li; Shin-Ichi Tashiro; Satoshi Onodera; Takashi Ikejima (2004) Journal of Asian natural products research display abstract
Shikonin, isolated from the plant Lithospermum erythrorhizon Sieb. ET Zucc, inhibited tumor cell growth and induced cell death in various tumor cells, with 50% growth inhibition of human cervical cancer cells, HeLa, at 18.9 +/- 1.1 mumol L-1. Treated with 40 mumol L-1 shikonin, HeLa cells underwent marked apoptotic morphological changes such as a round shape, membrane blebbing and apoptotic bodies derived from the fragmented nuclei. Another hallmark of apoptosis, DNA fragmentation, was observed by gel electrophoresis. Shikonin (10 mumol L-1) significantly blocked the transition from G1 to S phase in the HeLa cell cycle. Pan-caspase inhibitor (Z-VAD-FMK), caspase-3 inhibitor (Z-DEVD-FMK) or caspase-8 inhibitor (Z-IETD-FMK) effectively inhibited shikonin-induced cell death, while caspase-1 inhibitor (Ac-YVAD-CMK) and caspase-9 inhibitor (Z-LEHD-FMK) failed to affect cell death. Caspase-3 activity significantly increased within 12 h after shikonin treatment. Reduced expression of inhibitor of caspase-activated deoxyribonuclease (ICAD) after exposure to shikonin for 12 h suggests the resultant activation of caspase-activated deoxyribonuclease (CAD), leading to apoptosis.