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  1. General Info
  2. Effects Info
  3. Reference
Molecular Details
01. General Information
Name Methylated-DNA--protein-cysteine methyltransferase
UniProt ID MGMT_HUMAN
Gene Name MGMT
Gene ID 4255
Synonyms
MGMT
Sequence
MDKDCEMKRTTLDSPLGKLELSGCEQGLHEIKLLGKGTSAADAVEVPAPAAVLGGPEPLM
QCTAWLNAYFHQPEAIEEFPVPALHHPVFQQESFTRQVLWKLLKVVKFGEVISYQQLAAL
AGNPKAARAVGGAMRGNPVPILIPCHRVVCSSGAVGNYSGGLAVKEWLLAHEGHRLGKPG
LGGSSGLAGAWLKGAGATSGSPPAGRN
Pathway Map MAP LINK
KEGG ID hsa4255
TTD ID T24587
Pfam PF01035; PF02870
02. Combinatorial Therapeutic Effect(s)
Synergistic Effect
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Enhancing Drug Efficacy
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Combination Pair ID: 1038
Pair Name Cryptotanshinone, Temozolomide
Phytochemical Cryptotanshinone
Drug Temozolomide
Disease Info [ICD-11: 2A00] Glioblastoma multiforme Investigative
Regulate Info Down-regulation Methylated-DNA--protein-cysteine methyltransferase Expression
Result Combined treatment with CTS and TMZ might be an effective option to overcome the chemoresistance of GBM cells in a long-term treatment strategy.
Combination Pair ID: 475
Pair Name Protocatechualdehyde, Dacarbazine
Phytochemical Protocatechualdehyde
Drug Dacarbazine
Disease Info [ICD-11: 2C30] Melanoma Investigative
Regulate Info Down-regulation Methylated-DNA--protein-cysteine methyltransferase Expression
Result Our study demonstrates that the bioactive compound, Protocatechuic aldehyde, synergistically promotes the cytotoxicity of DTIC to melanoma cells through destabilization of MGMT protein. It could be a potential candidate for melanoma chemotherapy.
Combination Pair ID: 376
Pair Name Resveratrol, Temozolomide
Phytochemical Resveratrol
Drug Temozolomide
Disease Info [ICD-11: 2A00] Glioblastoma multiforme Investigative
Regulate Info Down-regulation Methylated-DNA--protein-cysteine methyltransferase Activity
Result Our results demonstrated synergistic effects of Res/TMZ on RG-2 cells and their bilaterally sensitizing effects to LN-18 and LN-428 cells. Frequent upregulation of MGMT and activation of STAT3 are the unfavorable factors for the treatment of GBMs and they may be the potential targets of Res/TMZ therapy.
Combination Pair ID: 382
Pair Name Resveratrol, Temozolomide
Phytochemical Resveratrol
Drug Temozolomide
Disease Info [ICD-11: 2A00] Glioblastoma multiforme Investigative
Regulate Info Down-regulation Methylated-DNA--protein-cysteine methyltransferase Expression
Result Res inhibited STAT3 signaling through modulation of PIAS3, SHP1, SHP2, and SOCS3, thereby attenuating tumor growth and increasing sensitivity to TMZ. Therefore, Res is an ideal candidate to be used in TMZ combined chemotherapy for GBM.
Combination Pair ID: 758
Pair Name Thymoquinone, Temozolomide
Phytochemical Thymoquinone
Drug Temozolomide
Disease Info [ICD-11: 2A00] Glioblastoma multiforme Investigative
Regulate Info Up-regulation Methylated-DNA--protein-cysteine methyltransferase Expression
Result Our findings demonstrate that TQ can effectively cross the BBB and function alone or in combination with TMZ to treat glioblastoma.
Combination Pair ID: 249
Pair Name Tubeimoside I, Temozolomide
Phytochemical Tubeimoside I
Drug Temozolomide
Disease Info [ICD-11: 2A00] Glioblastoma multiforme Investigative
Regulate Info Down-regulation Methylated-DNA--protein-cysteine methyltransferase Expression
Result We first demonstrated that synergistic effects of TBMS1 and TMZ induced apoptosis in GBM cells through reducing MGMT expression and inhibiting the EGFR induced PI3K/Akt/mTOR/NF-κB signaling pathway. This study provides a rationale for combined application of TMZ and TBMS1 as a potential chemotherapeutic treatment for MGMT+ GBM patients.
Reversing Drug Resistance
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Combination Pair ID: 742
Pair Name Aloe emodin, Temozolomide
Phytochemical Aloe emodin
Drug Temozolomide
Disease Info [ICD-11: 2A00] Glioblastoma multiforme Investigative
Regulate Info Down-regulation Methylated-DNA--protein-cysteine methyltransferase Expression
Result These convincing results suggest that AE could be a natural adjuvant agent to potentiate the effects of traditional drugs (TMZ) and overcome drug resistance in glioblastoma cells.
Combination Pair ID: 176
Pair Name Parthenolide, Temozolomide
Phytochemical Parthenolide
Drug Temozolomide
Disease Info [ICD-11: 2F7Z] Glioma Investigative
Regulate Info Down-regulation Methylated-DNA--protein-cysteine methyltransferase Expression
Result These findings suggest that NF-κB is a potential target for inducing cell death in gliomas. A targeted combination strategy in which the response to TMZ is synergistically enhanced by the addition of parthenolide which may be useful, especially in chemoresistant gliomas with high MGMT expression.
Combination Pair ID: 552
Pair Name Sulforaphane, Temozolomide
Phytochemical Sulforaphane
Drug Temozolomide
Disease Info [ICD-11: 2A00] Glioblastoma multiforme Investigative
Regulate Info Down-regulation Methylated-DNA--protein-cysteine methyltransferase Expression
Result The present study suggests that the clinical efficacy of TMZ-based chemotherapy in TMZ-resistant GBM may be improved by combination with SFN.
03. Reference
No. Title Href
1 Synergistic effect of cryptotanshinone and temozolomide treatment against human glioblastoma cells. Sci Rep. 2023 Dec 9;13(1):21835. doi: 10.1038/s41598-023-48777-z. Click
2 Protocatechuic aldehyde acts synergistically with dacarbazine to augment DNA double-strand breaks and promote apoptosis in cutaneous melanoma cells. BMC Complement Med Ther. 2023 Apr 27;23(1):133. doi: 10.1186/s12906-023-03965-2. Click
3 Synergistic Effects of Resveratrol and Temozolomide Against Glioblastoma Cells: Underlying Mechanism and Therapeutic Implications. Cancer Manag Res. 2020 Sep 11;12:8341-8354. doi: 10.2147/CMAR.S258584. Click
4 Resveratrol Enhances Temozolomide Efficacy in Glioblastoma Cells through Downregulated MGMT and Negative Regulators-Related STAT3 Inactivation. Int J Mol Sci. 2023 May 29;24(11):9453. doi: 10.3390/ijms24119453. Click
5 Thymoquinone induces apoptosis in temozolomide-resistant glioblastoma cells via the p38 mitogen-activated protein kinase signaling pathway. Environ Toxicol. 2023 Jan;38(1):90-100. doi: 10.1002/tox.23664. Click
6 Tubeimoside-I sensitizes temozolomide-resistant glioblastoma cells to chemotherapy by reducing MGMT expression and suppressing EGFR induced PI3K/Akt/mTOR/NF-κB-mediated signaling pathway. Phytomedicine. 2022 May;99:154016. doi: 10.1016/j.phymed.2022.154016. Click
7 Aloe-Emodin Overcomes Anti-Cancer Drug Resistance to Temozolomide and Prevents Colony Formation and Migration in Primary Human Glioblastoma Cell Lines NULU and ZAR. Molecules. 2023 Aug 11;28(16):6024. doi: 10.3390/molecules28166024 Click
8 Inhibition of NF-κB results in anti-glioma activity and reduces temozolomide-induced chemoresistance by down-regulating MGMT gene expression. Cancer Lett. 2018 Aug 1;428:77-89. doi: 10.1016/j.canlet.2018.04.033. Click
9 Sulforaphane reverses chemo-resistance to temozolomide in glioblastoma cells by NF-κB-dependent pathway downregulating MGMT expression. Int J Oncol. 2016 Feb;48(2):559-68. doi: 10.3892/ijo.2015.3271. Click
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