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  1. General Info
  2. Effects Info
  3. Reference
Molecular Details
01. General Information
Name Broad substrate specificity ATP-binding cassette transporter ABCG2
UniProt ID ABCG2_HUMAN
Gene Name ABCG2
Gene ID 9429
Synonyms
ABCG2, ABC15, ABCP, BCRP, BCRP1, BMDP, CD338, CDw338, CDw388, EST157481, GOUT1, MRX, MXR, MXR-1, MXR1, UAQTL1
Sequence
MSSSNVEVFIPVSQGNTNGFPATASNDLKAFTEGAVLSFHNICYRVKLKSGFLPCRKPVE
KEILSNINGIMKPGLNAILGPTGGGKSSLLDVLAARKDPSGLSGDVLINGAPRPANFKCN
SGYVVQDDVVMGTLTVRENLQFSAALRLATTMTNHEKNERINRVIQELGLDKVADSKVGT
QFIRGVSGGERKRTSIGMELITDPSILFLDEPTTGLDSSTANAVLLLLKRMSKQGRTIIF
SIHQPRYSIFKLFDSLTLLASGRLMFHGPAQEALGYFESAGYHCEAYNNPADFFLDIING
DSTAVALNREEDFKATEIIEPSKQDKPLIEKLAEIYVNSSFYKETKAELHQLSGGEKKKK
ITVFKEISYTTSFCHQLRWVSKRSFKNLLGNPQASIAQIIVTVVLGLVIGAIYFGLKNDS
TGIQNRAGVLFFLTTNQCFSSVSAVELFVVEKKLFIHEYISGYYRVSSYFLGKLLSDLLP
MRMLPSIIFTCIVYFMLGLKPKADAFFVMMFTLMMVAYSASSMALAIAAGQSVVSVATLL
MTICFVFMMIFSGLLVNLTTIASWLSWLQYFSIPRYGFTALQHNEFLGQNFCPGLNATGN
NPCNYATCTGEEYLVKQGIDLSPWGLWKNHVALACMIVIFLTIAYLKLLFLKKYS
Pathway Map MAP LINK
T.C. Number 3.A.1.204.2
KEGG ID hsa9429
TTD ID T56556
Pfam PF00005; PF01061; PF02463; PF03193; PF13304; PF13476; PF13555; PF19055
02. Combinatorial Therapeutic Effect(s)
Synergistic Effect
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Decreasing Drug Toxicity
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Combination Pair ID: 429
Pair Name Carvacrol, Sorafenib
Phytochemical Name Carvacrol
Anticancer drug Name Sorafenib
Disease Info [ICD-11: 2C12] Hepatocellular carcinoma Investigative
Regulate Info Down-regulation Broad substrate specificity ATP-binding cassette transporter ABCG2 Expression
Result CARV/Sora is a promising combination for tumor suppression and overcoming Sora resistance and cardiotoxicity in HCC by modulating TRPM7. To our best knowledge, this study represents the first study to investigate the efficiency of CARV/ Sora on the HCC rat model. Moreover, no previous studies have reported the effect of inhibiting TRPM7 on HCC.
Combination Pair ID: 385
Pair Name Curcumin, Quinacrine
Phytochemical Name Curcumin
Anticancer drug Name Quinacrine
Disease Info [ICD-11: 2C60] Breast cancer Investigative
Regulate Info Down-regulation Broad substrate specificity ATP-binding cassette transporter ABCG2 Expression
Result Quinacrine and Curcumin in combination decreased the breast cancer angiogenesis by modulating ABCG2 via VEGF A
Combination Pair ID: 200
Pair Name Tanshinone IIA, Doxorubicin
Phytochemical Name Tanshinone IIA
Anticancer drug Name Doxorubicin
Disease Info [ICD-11: 2C60] Breast cancer Investigative
Regulate Info Down-regulation Broad substrate specificity ATP-binding cassette transporter ABCG2 Expression
Result Tan IIA could be used as a novel agent combined with Dox in breast cancer therapy.
Enhancing Drug Efficacy
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Combination Pair ID: 1
Pair Name Camptothecin, Sorafenib
Phytochemical Camptothecin
Drug Sorafenib
Disease Info [ICD-11: 2C12] Hepatocellular carcinoma Investigative
Regulate Info Down-regulation Broad substrate specificity ATP-binding cassette transporter ABCG2 Expression
Result The synergetic combination significantly increases lipid peroxidation and iron concentration, decreases TAC, GPX4 and GR activity, and reduces the expression of both Nrf2 and SLC7A11. The downregulation of Nrf2 expression has a vital role in the reduction of resistance mediators to sorafenib against HCC cells like (p62, MT1G, and ABCG2) and improves the cellular uptake of sorafenib. The current study provided evidence that Nrf2 inhibition by CPT improves sorafenib's sensitivity and reduces sorafenib's resistance via the augmentation of sorafenib's ferroptosis action.
Combination Pair ID: 224
Pair Name Curcumol, Cisplatin
Phytochemical Curcumol
Drug Cisplatin
Disease Info [ICD-11: 2B51] Osteosarcoma Investigative
Regulate Info Down-regulation Broad substrate specificity ATP-binding cassette transporter ABCG2 Expression
Result These findings suggest that curcumol inhibits the polarization of M2-like macrophages and could be a promising combination strategy to synergize with CDDP in the osteosarcoma.
Combination Pair ID: 647
Pair Name Daidzein, Topotecan
Phytochemical Daidzein
Drug Topotecan
Disease Info [ICD-11: 2C60] Breast cancer Investigative
Regulate Info Down-regulation Broad substrate specificity ATP-binding cassette transporter ABCG2 Expression
Result Daidzein enhances the anticancer effect of topotecan and reverses BCRP-mediated drug resistance in breast cancer.
Combination Pair ID: 561
Pair Name Fucoxanthin, Doxorubicin
Phytochemical Fucoxanthin
Drug Doxorubicin
Disease Info [ICD-11: 2C12] Hepatocellular carcinoma Investigative
Regulate Info Down-regulation Broad substrate specificity ATP-binding cassette transporter ABCG2 Expression
Result The carotenoid fucoxanthin can sensitize multidrug resistant cancer cells to doxorubicin via induction of apoptosis, inhibition of multidrug resistance proteins and metabolic enzymes
Combination Pair ID: 747
Pair Name Thymoquinone, Imatinib
Phytochemical Thymoquinone
Drug Imatinib
Disease Info [ICD-11: 2B90] Colon cancer Investigative
Regulate Info Down-regulation Broad substrate specificity ATP-binding cassette transporter ABCG2 Expression
Result TQ potentiates IM efficacy on HCT116 cells via uptake/efflux genes modulation
Combination Pair ID: 680
Pair Name Ursolic acid, Cisplatin
Phytochemical Ursolic acid
Drug Cisplatin
Disease Info [ICD-11: 2C73] Ovarian cancer Investigative
Regulate Info Down-regulation Broad substrate specificity ATP-binding cassette transporter ABCG2 Expression
Result UA inhibits the proliferation and reversal of drug resistance in ovarian CSCs by suppressing the expression of downregulation of HIF-1α and ABCG2.
Reversing Drug Resistance
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Combination Pair ID: 159
Pair Name Celastrol, Cisplatin
Phytochemical Celastrol
Drug Cisplatin
Disease Info [ICD-11: 2B72] Gastric cancer Investigative
Regulate Info Down-regulation Broad substrate specificity ATP-binding cassette transporter ABCG2 Expression
Result Celastrol can inhibit the proliferation of the SGC7901/DDP cells, induce their apoptosis, and reduce the expression of drug resistance genes, probably by inhibiting the expression of the proteins related to the mTOR signaling pathway
Combination Pair ID: 985
Pair Name Fisetin, Paclitaxel
Phytochemical Fisetin
Drug Paclitaxel
Disease Info [ICD-11: 2C73] Ovarian cancer Investigative
Regulate Info Down-regulation Broad substrate specificity ATP-binding cassette transporter ABCG2 Expression
Result Our study shows that PTX-FA and Fis-FA PBM NPs directly target platinum-resistant OvCa cells, induce cytotoxic/apoptotic effects, and reverse multi-drug resistance (MDR). These findings allow us to create new clinical applications using PTX-FA and Fis-FA combination nanoparticles to treat drug-resistant cancers.
Combination Pair ID: 1028
Pair Name Saikosaponin D, Gefitinib
Phytochemical Saikosaponin D
Drug Gefitinib
Disease Info [ICD-11: 2C12] Hepatocellular carcinoma Investigative
Regulate Info Down-regulation Broad substrate specificity ATP-binding cassette transporter ABCG2 Expression
Result Saikosaponin D enhances the antitumor effect of gemcitabine by controlling glucose metabolism and drug efflux by inhibiting the ADRB2 signaling. Therefore, the combination of saikosaponin D and gemcitabine may be a potential therapeutic strategy for the treatment of iCCA.
03. Reference
No. Title Href
1 Carvacrol enhances anti-tumor activity and mitigates cardiotoxicity of sorafenib in thioacetamide-induced hepatocellular carcinoma model through inhibiting TRPM7. Life Sci. 2023 Jul 1;324:121735. doi: 10.1016/j.lfs.2023.121735. Click
2 Quinacrine and Curcumin in combination decreased the breast cancer angiogenesis by modulating ABCG2 via VEGF A. J Cell Commun Signal. 2023 Sep;17(3):609-626. doi: 10.1007/s12079-022-00692-0. Click
3 Combination of tanshinone IIA and doxorubicin possesses synergism and attenuation effects on doxorubicin in the treatment of breast cancer. Phytother Res. 2019 Jun;33(6):1658-1669. doi: 10.1002/ptr.6353. Click
4 Camptothecin Sensitizes Hepatocellular Carcinoma Cells to Sorafenib- Induced Ferroptosis Via Suppression of Nrf2. Inflammation. 2023 Aug;46(4):1493-1511. doi: 10.1007/s10753-023-01823-4. Click
5 Curcumol Synergizes with Cisplatin in Osteosarcoma by Inhibiting M2-like Polarization of Tumor-Associated Macrophages. Molecules. 2022 Jul 6;27(14):4345. doi: 10.3390/molecules27144345. Click
6 Functional daidzein enhances the anticancer effect of topotecan and reverses BCRP-mediated drug resistance in breast cancer. Pharmacol Res. 2019 Sep;147:104387. doi: 10.1016/j.phrs.2019.104387. Click
7 The carotenoid fucoxanthin can sensitize multidrug resistant cancer cells to doxorubicin via induction of apoptosis, inhibition of multidrug resistance proteins and metabolic enzymes. Phytomedicine. 2020 Oct;77:153280. doi: 10.1016/j.phymed.2020.153280. Click
8 Thymoquinone chemosensitizes human colorectal cancer cells to imatinib via uptake/efflux genes modulation. Clin Exp Pharmacol Physiol. 2021 Jun;48(6):911-920. doi: 10.1111/1440-1681.13476. Click
9 Ursolic acid inhibits proliferation and reverses drug resistance of ovarian cancer stem cells by downregulating ABCG2 through suppressing the expression of hypoxia-inducible factor-1α in vitro. Oncol Rep. 2016 Jul;36(1):428-40. doi: 10.3892/or.2016.4813. Click
10 Celastrol Inhibits the Proliferation and Decreases Drug Resistance of Cisplatin- Resistant Gastric Cancer SGC7901/DDP Cells. Anticancer Agents Med Chem. 2022;22(2):270-279. doi: 10.2174/1871520621666210528144006. Click
11 The effect of paclitaxel- and fisetin-loaded PBM nanoparticles on apoptosis and reversal of drug resistance gene ABCG2 in ovarian cancer. J Ovarian Res. 2023 Nov 21;16(1):220. doi: 10.1186/s13048-023-01308-w. Click
12 Saikosaponin D reverses epinephrine- and norepinephrine-induced gemcitabine resistance in intrahepatic cholangiocarcinoma by downregulating ADRB2/glycolysis signaling. Acta Biochim Biophys Sin (Shanghai). 2023 Jul 25;55(9):1404-1414. doi: 10.3724/abbs.2023040. Click
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