m6A-centered Drug Response Information
General Information of the Drug (ID: M6ADRUG0097)
| Name |
Olaparib
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| Synonyms |
Olaparib; 763113-22-0; AZD2281; Lynparza; KU-0059436; AZD 2281; AZD-2281; 1-(Cyclopropylcarbonyl)-4-[5-[(3,4-dihydro-4-oxo-1-phthalazinyl)methyl]-2-fluorobenzoyl]piperazine; 4-(3-(4-(Cyclopropanecarbonyl)piperazine-1-carbonyl)-4-fluorobenzyl)phthalazin-1(2H)-one; Olaparib (AZD2281, Ku-0059436); UNII-WOH1JD9AR8; KU-59436; Olaparib (AZD-2281); 4-[[3-[4-(Cyclopropanecarbonyl)piperazine-1-carbonyl]-4-fluorophenyl]methyl]-2H-phthalazin-1-one; MFCD13185161; WOH1JD9AR8; C24H23FN4O3; CHEBI:83766; AZ2281; 4-(3-{[4-(Cyclopropylcarbonyl)piperazin-1-Yl]carbonyl}-4-Fluorobenzyl)phthalazin-1(2h)-One; 4-[3-(4-Cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one; NSC-747856; KU59436; 4-[(3-{[4-(Cyclopropylcarbonyl)piperazin-1-yl]carbonyl}-4-fluorophenyl)methyl]phthalazin-1(2H)-one; OLAPARIB cpd; Olaparib (AZD2281; Ku-0059436); Olaparib [USAN:INN]; Olaparib (AZD2281); Acylpiperazine analogue, 47; Olaparibum; AZD221; 4-[3-[4-(Cyclopropanecarbonyl)piperazine-1-carbonyl]-4-fluorobenzyl]phthalazin-1(2H)-one; Olaparib- Bio-X; Lynparza (TN); 09L; 4-((3-{(4-(cyclopropylcarbonyl)piperazin-1-yl)carbonyl}-4-fluorophenyl)methyl)phthalazin-1(2H)-one; 937799-91-2; KU 59436; KU0059436; Olaparib - AZD2281; AZD-2281 (Olaparib); Olaparib (JAN/USAN/INN); MLS006010185; SCHEMBL426568; CHEMBL521686; GTPL7519; BDBM27566; AOB1085; DTXSID60917988; EX-A002; BCPP000360; HMS3295I09; HMS3426C03; HMS3654G13; HMS3746K07; HMS3870H03; AMY10295; BCP01872; 763113-22-0, Lynparza,; NSC747856; NSC753686; s1060; ZINC40430143; AKOS005145764; AC-7939; AZ-2281; BCP9000363; CCG-264799; CS-0075; DB09074; EX-7210; KEYLYNK-010 COMPONENT OLAPARIB; NSC 747856; NSC-753686; QC-2660; SB14617; SS-4573; AZD2281,Olaparib, KU-0059436; NCGC00238451-01; NCGC00238451-02; NCGC00238451-08; NCGC00238451-09; NCGC00238451-11; 4-[(3-{[4-Cyclopropylcarbonyl)piperazin-4-yl]carbonyl}-4-fluorophenyl)methyl]phtalazin-1(2H)-one; BO164169; HY-10162; Olaparib (AZD2281, KU0059436); SMR004701291; SY040527; OLAPARIB COMPONENT OF KEYLYNK-010; Olaparib(AZD2281,KuDOSKU-0059436); A9666; BB 0260909; FT-0651458; KU 0059436; SW218142-2; EC-000.2324; D09730; J-503540; Q7083106; BRD-K02113016-001-08-9; BRD-K02113016-001-09-7; AZD 2281; ; ; KU 0059436; ; ; KU 59436; 1-(cyclopropylcarbonyl)-4-[5-[(3,4-dihydro-4-oxo-1-phthalazine; 4-(3-(1-(cyclopropanecarbonyl)piperazine-4-carbonyl)-4-fluorobenzyl)phthalazin-1(2H)-one; (2H)-Phthalazinone, 4-((3-((4-(cyclopropylcarbonyl)-1-piperazinyl)carbonyl)-4-fluorophenyl)methyl)-; [4-(Cyclopropanecarbonyl)piperazin-1-yl]{2-fluoro-5-[(4-hydroxyphthalazin-1-yl)methyl]phenyl}methanone; 1021843-02-6; 4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbonyl]-4-fluorophenyl}methyl)-1,2-dihydrophthalazin-1-one
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| Status | Approved | [1] | |||
| Structure |
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| Formula |
C24H23FN4O3
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| InChI |
InChI=1S/C24H23FN4O3/c25-20-8-5-15(14-21-17-3-1-2-4-18(17)22(30)27-26-21)13-19(20)24(32)29-11-9-28(10-12-29)23(31)16-6-7-16/h1-5,8,13,16H,6-7,9-12,14H2,(H,27,30)
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| InChIKey |
FDLYAMZZIXQODN-UHFFFAOYSA-N
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Full List of m6A Targets Related to This Drug
Transcription factor E2F8 (E2F8)
| In total 2 item(s) under this target gene | ||||
| Experiment 1 Reporting the m6A-centered Drug Response by This Target Gene | [2] | |||
| Response Summary | In breast cancer, accordingly YTHDF1 knockdown sensitizes breast cancer cells to Adriamycin and Cisplatin as well as Olaparib, a PARP inhibitor. Transcription factor E2F8 (E2F8) is a target molecule by YTHDF1 which modulates E2F8 mRNA stability and DNA damage repair in a METTL14-dependent manner. | |||
| Responsed Disease | Breast cancer | ICD-11: 2C60 | ||
| Target Regulator | YTH domain-containing family protein 1 (YTHDF1) | READER | ||
| Target Regulation | Up regulation | |||
| Pathway Response | Nucleotide excision repair | hsa03420 | ||
| Cell Process | RNA stability | |||
| In-vitro Model | MDA-MB-231 | Breast adenocarcinoma | Homo sapiens | CVCL_0062 |
| MCF-7 | Invasive breast carcinoma | Homo sapiens | CVCL_0031 | |
| Hs 578T | Invasive breast carcinoma | Homo sapiens | CVCL_0332 | |
| In-vivo Model | 1×106 MDA-MB-231 cells were resuspended in 100 uL PBS with 50% Matrigel (Corning Costar, USA), and injected into the mammary fat pad of the mice. | |||
| Experiment 2 Reporting the m6A-centered Drug Response by This Target Gene | [2] | |||
| Response Summary | In breast cancer, accordingly YTHDF1 knockdown sensitizes breast cancer cells to Adriamycin and Cisplatin as well as Olaparib, a PARP inhibitor. Transcription factor E2F8 (E2F8) is a target molecule by YTHDF1 which modulates E2F8 mRNA stability and DNA damage repair in a METTL14-dependent manner. | |||
| Responsed Disease | Breast cancer | ICD-11: 2C60 | ||
| Target Regulator | Methyltransferase-like 14 (METTL14) | WRITER | ||
| Target Regulation | Up regulation | |||
| Pathway Response | Nucleotide excision repair | hsa03420 | ||
| Cell Process | RNA stability | |||
| In-vitro Model | MDA-MB-231 | Breast adenocarcinoma | Homo sapiens | CVCL_0062 |
| MCF-7 | Invasive breast carcinoma | Homo sapiens | CVCL_0031 | |
| Hs 578T | Invasive breast carcinoma | Homo sapiens | CVCL_0332 | |
| In-vivo Model | 1×106 MDA-MB-231 cells were resuspended in 100 uL PBS with 50% Matrigel (Corning Costar, USA), and injected into the mammary fat pad of the mice. | |||
Full List of Crosstalk(s) between m6A Modification and Epigenetic Regulation Related to This Drug
| In total 4 item(s) under this drug | ||
| Crosstalk ID: M6ACROT02214 | ||
| m6A Regulator | Methyltransferase-like 14 (METTL14) | |
| m6A Target | Transcription factor E2F8 (E2F8) | |
| Epigenetic Regulator | DNA (cytosine-5)-methyltransferase 3B (DNMT3B) | |
| Regulated Target | Methyltransferase-like protein 14 (METTL14) | |
| Crosstalk relationship | DNA modification → m6A | |
| Disease | Breast cancer | |
| Crosstalk ID: M6ACROT02238 | ||
| m6A Regulator | Methyltransferase-like 14 (METTL14) | |
| m6A Target | Transcription factor E2F8 (E2F8) | |
| Epigenetic Regulator | Cysteine methyltransferase DNMT3A (DNMT3A) | |
| Regulated Target | Methyltransferase-like protein 14 (METTL14) | |
| Crosstalk relationship | DNA modification → m6A | |
| Disease | Breast cancer | |
| Crosstalk ID: M6ACROT02262 | ||
| m6A Regulator | Methyltransferase-like 14 (METTL14) | |
| m6A Target | Transcription factor E2F8 (E2F8) | |
| Epigenetic Regulator | DNA (cytosine-5)-methyltransferase 1 (DNMT1) | |
| Regulated Target | Methyltransferase-like protein 14 (METTL14) | |
| Crosstalk relationship | DNA modification → m6A | |
| Disease | Breast cancer | |
| Crosstalk ID: M6ACROT05147 | ||
| m6A Regulator | Heterogeneous nuclear ribonucleoproteins A2/B1 (HNRNPA2B1) | |
| m6A Target | Cysteine protease ATG4B (ATG4B) | |
| Epigenetic Regulator | Prostate cancer associated transcript 6 (PCAT6) | |
| Regulated Target | Heterogeneous nuclear ribonucleoprotein A2/B1 (HNRNPA2B1) | |
| Crosstalk relationship | ncRNA → m6A | |
| Disease | Breast cancer | |
References