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  1. General Info
  2. Effects Info
  3. Reference
Molecular Details
01. General Information
Name Histone-lysine N-methyltransferase EZH2
UniProt ID EZH2_HUMAN
Gene Name EZH2
Gene ID 2146
Synonyms
EZH2, ENX-1, ENX1, EZH2b, KMT6, KMT6A, WVS, WVS2
Sequence
MGQTGKKSEKGPVCWRKRVKSEYMRLRQLKRFRRADEVKSMFSSNRQKILERTEILNQEW
KQRRIQPVHILTSVSSLRGTRECSVTSDLDFPTQVIPLKTLNAVASVPIMYSWSPLQQNF
MVEDETVLHNIPYMGDEVLDQDGTFIEELIKNYDGKVHGDRECGFINDEIFVELVNALGQ
YNDDDDDDDGDDPEEREEKQKDLEDHRDDKESRPPRKFPSDKIFEAISSMFPDKGTAEEL
KEKYKELTEQQLPGALPPECTPNIDGPNAKSVQREQSLHSFHTLFCRRCFKYDCFLHPFH
ATPNTYKRKNTETALDNKPCGPQCYQHLEGAKEFAAALTAERIKTPPKRPGGRRRGRLPN
NSSRPSTPTINVLESKDTDSDREAGTETGGENNDKEEEEKKDETSSSSEANSRCQTPIKM
KPNIEPPENVEWSGAEASMFRVLIGTYYDNFCAIARLIGTKTCRQVYEFRVKESSIIAPA
PAEDVDTPPRKKKRKHRLWAAHCRKIQLKKDGSSNHVYNYQPCDHPRQPCDSSCPCVIAQ
NFCEKFCQCSSECQNRFPGCRCKAQCNTKQCPCYLAVRECDPDLCLTCGAADHWDSKNVS
CKNCSIQRGSKKHLLLAPSDVAGWGIFIKDPVQKNEFISEYCGEIISQDEADRRGKVYDK
YMCSFLFNLNNDFVVDATRKGNKIRFANHSVNPNCYAKVMMVNGDHRIGIFAKRAIQTGE
ELFFDYRYSQADALKYVGIEREMEIP
Pathway Map MAP LINK
KEGG ID hsa2146
TTD ID T25265
Pfam PF00856; PF11616; PF18118; PF18264; PF21358
02. Combinatorial Therapeutic Effect(s)
Synergistic Effect
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Enhancing Drug Efficacy
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Combination Pair ID: 715
Pair Name Atractylenolide I, Erlotinib
Phytochemical Atractylenolide I
Drug Erlotinib
Disease Info [ICD-11: 2C25] Lung cancer Investigative
Regulate Info Down-regulation Histone-lysine N-methyltransferase EZH2 Expression
Result Targeting the PDK1- and HOTAIR-mediated downstream molecule EZH2 by the combination of ATL-1 and erlotinib potentially facilitates the development of an additional novel strategy to combat lung cancer
Combination Pair ID: 557
Pair Name Lycopene, Enzalutamide
Phytochemical Lycopene
Drug Enzalutamide
Disease Info [ICD-11: 2C82] Prostate cancer Investigative
Regulate Info Down-regulation Histone-lysine N-methyltransferase EZH2 Phosphorylation
Result These results suggest that the enhanced antitumor effects of enzalutamide by lycopene may be related to the reduction of AR protein levels through lycopene-mediated inhibition of AKT/EZH2 pathway, which may provide a new approach to improve the efficacy of enzalutamide in CRPC.
Combination Pair ID: 193
Pair Name Oleanolic Acid, Gemcitabine
Phytochemical Oleanolic Acid
Drug Gemcitabine
Disease Info [ICD-11: 2C10] Pancreatic cancer Investigative
Regulate Info Down-regulation Histone-lysine N-methyltransferase EZH2 Expression
Result We found an interesting finding that the 73-03 in combination with GCB can improve GCB efficacy and decrease PCa resistance, which induced apoptosis and mitochondrial damage through epigenetic inhibition of SPINK1 transcription by miR-421 up-regulation. This was the first study that used OA derivatives on GCB-resistant PCa cells, so this combined strategy warrants further investigation.
03. Reference
No. Title Href
1 Repression of PDK1- and LncRNA HOTAIR-Mediated EZH2 Gene Expression Contributes to the Enhancement of Atractylenolide 1 and Erlotinib in the Inhibition of Human Lung Cancer Cells. Cell Physiol Biochem. 2018;49(4):1615-1632. doi: 10.1159/000493497. Click
2 Lycopene enhances the sensitivity of castration-resistant prostate cancer to enzalutamide through the AKT/EZH2/ androgen receptor signaling pathway. Biochem Biophys Res Commun. 2022 Jul 12;613:53-60. doi: 10.1016/j.bbrc.2022.04.126. Click
3 Enhancement of gemcitabine efficacy by K73-03 via epigenetically regulation of miR-421/SPINK1 in gemcitabine resistant pancreatic cancer cells. Phytomedicine. 2021 Oct;91:153711. doi: 10.1016/j.phymed.2021.153711. Click
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