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Drug-Target Interaction

Drug

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PubChem ID:637511
Structure:
Synonyms:
(2E)-3-phenyl-2-propenal
(2E)-3-phenylacrylaldehyde
(2E)-3-phenylprop-2-enal
(3E)-3-phenylprop-2-enal
(E)-3-Phenyl-2-propenal
(E)-3-phenyl-2-propenal(E)-cinnamaldehyde
(E)-3-phenylprop-2-enal
(E)-3-Phenylpropenal
(E)-Cinnamaldehyde
104-55-2
14371-10-9
2-07-00-00273 (Beilstein Handbook Reference)
2-Propenal, 3-phenyl-
2-propenal, 3-phenyl-, (2E)-
2-Propenal, 3-phenyl-, (E)-
2-Propenal, 3-phenyl-, (E)- (9CI)
2-propenal,3-phenyl-,(E)-
239968_ALDRICH
3-Fenylpropenal
3-Fenylpropenal [Czech]
3-Phenyl-2-propen-1-al
3-Phenyl-2-propenal
3-PHENYL-2-PROPENAL (TRANS)
3-Phenyl-2-propenaldehyde
3-Phenylacrolein
3-Phenylacrylaldehyde
3-phenylprop-2-enal
3-phenylprop-2-enaldehyde
3-Phenylpropenal
4-07-00-00984 (Beilstein Handbook Reference)
AB1002163
Abion CA
AC1LCUDE
AC1Q6BJW
AC1Q6PPL
Acrolein, 3-phenyl-
AG-D-16902
AI3-00473
AI3-33275
AIDS-097032
AIDS097032
AKOS000119171
Aldehyd skoricovy
Aldehyd skoricovy [Czech]
AR-1F5016
B99DD6C7-1C6D-4FE3-A172-54BFDB987683
BB_NC-2240
Benzylideneacetaldehyde
beta-phenylacrolein
beta-Phenylcrolein
bmse010257
BRN 0605737
BRN 1071571
C00903
C012843
C80687_ALDRICH
C9H8O
Cassia aldehyde
Caswell No. 221A
CCRIS 3189
CCRIS 6222
CHEBI:16731
CHEMBL293492
Cinnamal
CINNAMALDEHYDE
CINNAMALDEHYDE (SEE ALSO TRANS-CINNAMALDEHYDE (14371-10-9))
CINNAMALDEHYDE (TRANS)
Cinnamaldehyde (trans), neat
Cinnamaldehyde, (E)-
Cinnamaldehyde, trans-
Cinnamic aldehyde
Cinnamic aldehyde (natural)
cinnamic aldehyde, (E)-isomer
Cinnamyl aldehyde
Cinnamylaldehyde
Cinnemaldehyde
CNMA
EINECS 203-213-9
EPA Pesticide Chemical Code 040506
FEMA No. 2286
FEMA Number 2286
Hefty Dog and Cat Repellent
HMS2268O08
HSDB 209
I14-7336
LS-378
LS-850
MLS002454394
MolPort-000-871-213
NCGC00091512-01
NCGC00091512-02
NCGC00091512-04
NCGC00091512-05
NCGC00091512-06
NCGC00091512-07
nchem.727-comp2a
nchem.801-comp5b
nchembio.146-comp3
NCI-C56111
NSC 16935
NSC16935
NSC40346
Phenylacrolein
SMR000112334
ST5213393
STK397371
supercinnamaldehyde
trans-3-Phenyl-2-propenal
trans-3-phenylprop-2-enaldehyde
trans-Cinnamaldehyde
TRANS-CINNAMALDEHYDE (SEE ALSO CINNAMALDEHYDE (104-55-2))
trans-Cinnamic aldehyde
trans-Cinnamylaldehyde
trans-Phenylacrolein
trans-Phenylacrylaldehyde
UNII-SR60A3XG0F
W228605_ALDRICH
W228613_ALDRICH
WLN: VH1U1R
Zimtaldehyde
ZINC01532777

Target

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Uniprot ID:MK03_HUMAN
Synonyms:
ERK-1
ERT2
Extracellular signal-regulated kinase 1
Insulin-stimulated MAP2 kinase
MAP kinase 1
MAPK 1
Microtubule-associated protein 2 kinase
Mitogen-activated protein kinase 3
p44-ERK1
p44-MAPK
EC-Numbers:2.7.11.24
Organism:Homo sapiens
Human
PDB IDs:2ZOQ
Structure:
2ZOQ

Binding Affinities:

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

References:

15964311
Cinnamaldehyde-induced apoptosis in human PLC/PRF/5 cells through activation of the proapoptotic Bcl-2 family proteins and MAPK pathway.. Shu-Jing Wu; Lean-Teik Ng; Chun-Ching Lin (2005) Life sciences display abstract
Cinnamaldehyde (Cin) has been shown to be effective in inducing apoptotic cell death in a number of human cancer cells. However, the intracellular death signaling mechanisms by which Cin inhibits tumor cell growth are poorly understood. In this study, we investigated the effect of mitogen-activated protein kinases (MAPKs) inhibitors [namely SP600125 (a specific JNK inhibitor), SB203580 (a specific p38 inhibitor) and PD98059 (a specific ERK inhibitor)] on the stress-responsive MAPK pathway induced by Cin in PLC/PRF/5 cells. Trypan blue staining assay indicated that Cin was cytotoxic to PLC/PRF/5 cells. Cin caused cell cycle perturbation (S-phase arrest) and triggered apoptosis as revealed by the externalization of annexin V-targeted phosphatidylserine and accumulation of sub-G1 peak. It down-regulated the Bcl-2 and Mcl-1 expression, and up-regulated Bax protein in a time-response manner. Treatment with 1 microM Cin resulted in an activation of caspase-8 and cleavage of Bid to its truncated form in a time-dependent pattern. JNK, ERK and p38 kinases in cells were activated and phosphorylated after Cin treatment. Pre-incubation with SP600125 and SB203580 markedly suppressed the effect of Cin-induced apoptosis, but not PD98059. Both SP600125 and SB203580 significantly prevented the phosphorylation of JNK and p38 proteins, but not ERK. These results conclude that Cin triggers apoptosis in PLC/PRF/5 cells could be through the activation of pro-apoptotic Bcl-2 family (Bax and Bid) proteins and MAPK signaling pathway.