General Information of the Drug (ID: M6ADRUG0090)
Name
Osimertinib
Synonyms
Osimertinib
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Status Approved [1]
Structure
Formula
C28H33N7O2
InChI
InChI=1S/C28H33N7O2/c1-7-27(36)30-22-16-23(26(37-6)17-25(22)34(4)15-14-33(2)3)32-28-29-13-12-21(31-28)20-18-35(5)24-11-9-8-10-19(20)24/h7-13,16-18H,1,14-15H2,2-6H3,(H,30,36)(H,29,31,32)
InChIKey
DUYJMQONPNNFPI-UHFFFAOYSA-N
PubChem CID
71496458
TTD Drug ID
D0O8GK
DrugBank ID
DB09330
Full List of m6A Targets Related to This Drug
microRNA let-7b (MIRLET7B)
In total 1 item(s) under this target gene
Experiment 1 Reporting the m6A-centered Drug Response by This Target Gene [2]
Response Summary The participation of Metformin decreased the bindings of DNMT3a/b to the METTL3 promoter with the help of the readers of NKAP and HNRNPA2B1.the mediation of m6A formation on pri-Let-7b processing increased the mature microRNA let-7b (MIRLET7B), whose key role is to suppress the Notch signaling and to re-captivate the Osimertinib treatment.The findings open up future drug development, targeting this pathway for lung cancer patients.
Responsed Disease Lung cancer ICD-11: 2C25
Target Regulator Methyltransferase-like 3 (METTL3) WRITER
Pathway Response Notch signaling pathway hsa04330
In-vitro Model NCI-H1975 Lung adenocarcinoma Homo sapiens CVCL_1511
HCC827 Lung adenocarcinoma Homo sapiens CVCL_2063
H1975OR (Osimertinib resistant H1975 cells)
HCC827OR (Osimertinib resistant HCC827 cells)
Full List of Crosstalk(s) between m6A Modification and Epigenetic Regulation Related to This Drug
In total 33 item(s) under this drug
Crosstalk ID: M6ACROT02064
m6A Regulator Methyltransferase-like 3 (METTL3)
m6A Target microRNA let-7b (MIRLET7B)
Epigenetic Regulator Cysteine methyltransferase DNMT3A (DNMT3A)
Regulated Target Methyltransferase-like protein 3 (METTL3)
Crosstalk relationship DNA modification → m6A
Disease Lung cancer
Crosstalk ID: M6ACROT02065
m6A Regulator NF-kappa-B-activating protein (NKAP)
m6A Target microRNA let-7b (MIRLET7B)
Epigenetic Regulator Cysteine methyltransferase DNMT3A (DNMT3A)
Regulated Target Methyltransferase-like protein 3 (METTL3)
Crosstalk relationship DNA modification → m6A
Disease Lung cancer
Crosstalk ID: M6ACROT02066
m6A Regulator Heterogeneous nuclear ribonucleoproteins A2/B1 (HNRNPA2B1)
m6A Target microRNA let-7b (MIRLET7B)
Epigenetic Regulator Cysteine methyltransferase DNMT3A (DNMT3A)
Regulated Target Methyltransferase-like protein 3 (METTL3)
Crosstalk relationship DNA modification → m6A
Disease Lung cancer
Crosstalk ID: M6ACROT02067
m6A Regulator Methyltransferase-like 3 (METTL3)
m6A Target microRNA let-7b (MIRLET7B)
Epigenetic Regulator DNA (cytosine-5)-methyltransferase 3B (DNMT3B)
Regulated Target Methyltransferase-like protein 3 (METTL3)
Crosstalk relationship DNA modification → m6A
Disease Lung cancer
Crosstalk ID: M6ACROT02068
m6A Regulator NF-kappa-B-activating protein (NKAP)
m6A Target microRNA let-7b (MIRLET7B)
Epigenetic Regulator DNA (cytosine-5)-methyltransferase 3B (DNMT3B)
Regulated Target Methyltransferase-like protein 3 (METTL3)
Crosstalk relationship DNA modification → m6A
Disease Lung cancer
Crosstalk ID: M6ACROT02069
m6A Regulator Heterogeneous nuclear ribonucleoproteins A2/B1 (HNRNPA2B1)
m6A Target microRNA let-7b (MIRLET7B)
Epigenetic Regulator DNA (cytosine-5)-methyltransferase 3B (DNMT3B)
Regulated Target Methyltransferase-like protein 3 (METTL3)
Crosstalk relationship DNA modification → m6A
Disease Lung cancer
Crosstalk ID: M6ACROT02167
m6A Regulator Methyltransferase-like 3 (METTL3)
m6A Target PI3-kinase subunit alpha (PI3k/PIK3CA)
Epigenetic Regulator Cysteine methyltransferase DNMT3A (DNMT3A)
Regulated Target Methyltransferase-like protein 3 (METTL3)
Crosstalk relationship DNA modification → m6A
Disease Lung cancer
Crosstalk ID: M6ACROT02168
m6A Regulator Methyltransferase-like 3 (METTL3)
m6A Target hsa-miR-143-3p
Epigenetic Regulator Cysteine methyltransferase DNMT3A (DNMT3A)
Regulated Target Methyltransferase-like protein 3 (METTL3)
Crosstalk relationship DNA modification → m6A
Disease Lung cancer
Crosstalk ID: M6ACROT02169
m6A Regulator Methyltransferase-like 3 (METTL3)
m6A Target Transcription factor JunB (JUNB)
Epigenetic Regulator Cysteine methyltransferase DNMT3A (DNMT3A)
Regulated Target Methyltransferase-like protein 3 (METTL3)
Crosstalk relationship DNA modification → m6A
Disease Lung cancer
Crosstalk ID: M6ACROT02171
m6A Regulator Methyltransferase-like 3 (METTL3)
m6A Target Histone-lysine N-methyltransferase EZH2 (EZH2)
Epigenetic Regulator Cysteine methyltransferase DNMT3A (DNMT3A)
Regulated Target Methyltransferase-like protein 3 (METTL3)
Crosstalk relationship DNA modification → m6A
Disease Lung cancer
Crosstalk ID: M6ACROT02172
m6A Regulator Methyltransferase-like 3 (METTL3)
m6A Target Hepatocyte growth factor receptor (c-Met/MET)
Epigenetic Regulator Cysteine methyltransferase DNMT3A (DNMT3A)
Regulated Target Methyltransferase-like protein 3 (METTL3)
Crosstalk relationship DNA modification → m6A
Disease Lung cancer
Crosstalk ID: M6ACROT02173
m6A Regulator Methyltransferase-like 3 (METTL3)
m6A Target Zinc finger and BTB domain-containing protein 4 (ZBTB4)
Epigenetic Regulator Cysteine methyltransferase DNMT3A (DNMT3A)
Regulated Target Methyltransferase-like protein 3 (METTL3)
Crosstalk relationship DNA modification → m6A
Disease Lung cancer
Crosstalk ID: M6ACROT02174
m6A Regulator Methyltransferase-like 3 (METTL3)
m6A Target Mutated in multiple advanced cancers 1 (PTEN)
Epigenetic Regulator Cysteine methyltransferase DNMT3A (DNMT3A)
Regulated Target Methyltransferase-like protein 3 (METTL3)
Crosstalk relationship DNA modification → m6A
Disease Lung cancer
Crosstalk ID: M6ACROT02175
m6A Regulator Methyltransferase-like 3 (METTL3)
m6A Target PI3-kinase subunit alpha (PI3k/PIK3CA)
Epigenetic Regulator Cysteine methyltransferase DNMT3A (DNMT3A)
Regulated Target Methyltransferase-like protein 3 (METTL3)
Crosstalk relationship DNA modification → m6A
Disease Lung cancer
Crosstalk ID: M6ACROT02176
m6A Regulator Methyltransferase-like 3 (METTL3)
m6A Target RAC-alpha serine/threonine-protein kinase (AKT1)
Epigenetic Regulator Cysteine methyltransferase DNMT3A (DNMT3A)
Regulated Target Methyltransferase-like protein 3 (METTL3)
Crosstalk relationship DNA modification → m6A
Disease Lung cancer
Crosstalk ID: M6ACROT02177
m6A Regulator Methyltransferase-like 3 (METTL3)
m6A Target Serine/threonine-protein kinase mTOR (MTOR)
Epigenetic Regulator Cysteine methyltransferase DNMT3A (DNMT3A)
Regulated Target Methyltransferase-like protein 3 (METTL3)
Crosstalk relationship DNA modification → m6A
Disease Lung cancer
Crosstalk ID: M6ACROT02178
m6A Regulator Methyltransferase-like 3 (METTL3)
m6A Target SVIL antisense RNA 1 (SVIL-AS1)
Epigenetic Regulator Cysteine methyltransferase DNMT3A (DNMT3A)
Regulated Target Methyltransferase-like protein 3 (METTL3)
Crosstalk relationship DNA modification → m6A
Disease Lung cancer
Crosstalk ID: M6ACROT02179
m6A Regulator Methyltransferase-like 3 (METTL3)
m6A Target SH3 domain-binding protein 5 (SH3BP5)
Epigenetic Regulator Cysteine methyltransferase DNMT3A (DNMT3A)
Regulated Target Methyltransferase-like protein 3 (METTL3)
Crosstalk relationship DNA modification → m6A
Disease Lung cancer
Crosstalk ID: M6ACROT02180
m6A Regulator Methyltransferase-like 3 (METTL3)
m6A Target PI3-kinase subunit alpha (PI3k/PIK3CA)
Epigenetic Regulator DNA (cytosine-5)-methyltransferase 3B (DNMT3B)
Regulated Target Methyltransferase-like protein 3 (METTL3)
Crosstalk relationship DNA modification → m6A
Disease Lung cancer
Crosstalk ID: M6ACROT02181
m6A Regulator Methyltransferase-like 3 (METTL3)
m6A Target hsa-miR-143-3p
Epigenetic Regulator DNA (cytosine-5)-methyltransferase 3B (DNMT3B)
Regulated Target Methyltransferase-like protein 3 (METTL3)
Crosstalk relationship DNA modification → m6A
Disease Lung cancer
Crosstalk ID: M6ACROT02182
m6A Regulator Methyltransferase-like 3 (METTL3)
m6A Target Transcription factor JunB (JUNB)
Epigenetic Regulator DNA (cytosine-5)-methyltransferase 3B (DNMT3B)
Regulated Target Methyltransferase-like protein 3 (METTL3)
Crosstalk relationship DNA modification → m6A
Disease Lung cancer
Crosstalk ID: M6ACROT02184
m6A Regulator Methyltransferase-like 3 (METTL3)
m6A Target Histone-lysine N-methyltransferase EZH2 (EZH2)
Epigenetic Regulator DNA (cytosine-5)-methyltransferase 3B (DNMT3B)
Regulated Target Methyltransferase-like protein 3 (METTL3)
Crosstalk relationship DNA modification → m6A
Disease Lung cancer
Crosstalk ID: M6ACROT02185
m6A Regulator Methyltransferase-like 3 (METTL3)
m6A Target Hepatocyte growth factor receptor (c-Met/MET)
Epigenetic Regulator DNA (cytosine-5)-methyltransferase 3B (DNMT3B)
Regulated Target Methyltransferase-like protein 3 (METTL3)
Crosstalk relationship DNA modification → m6A
Disease Lung cancer
Crosstalk ID: M6ACROT02186
m6A Regulator Methyltransferase-like 3 (METTL3)
m6A Target Zinc finger and BTB domain-containing protein 4 (ZBTB4)
Epigenetic Regulator DNA (cytosine-5)-methyltransferase 3B (DNMT3B)
Regulated Target Methyltransferase-like protein 3 (METTL3)
Crosstalk relationship DNA modification → m6A
Disease Lung cancer
Crosstalk ID: M6ACROT02187
m6A Regulator Methyltransferase-like 3 (METTL3)
m6A Target Mutated in multiple advanced cancers 1 (PTEN)
Epigenetic Regulator DNA (cytosine-5)-methyltransferase 3B (DNMT3B)
Regulated Target Methyltransferase-like protein 3 (METTL3)
Crosstalk relationship DNA modification → m6A
Disease Lung cancer
Crosstalk ID: M6ACROT02188
m6A Regulator Methyltransferase-like 3 (METTL3)
m6A Target PI3-kinase subunit alpha (PI3k/PIK3CA)
Epigenetic Regulator DNA (cytosine-5)-methyltransferase 3B (DNMT3B)
Regulated Target Methyltransferase-like protein 3 (METTL3)
Crosstalk relationship DNA modification → m6A
Disease Lung cancer
Crosstalk ID: M6ACROT02189
m6A Regulator Methyltransferase-like 3 (METTL3)
m6A Target RAC-alpha serine/threonine-protein kinase (AKT1)
Epigenetic Regulator DNA (cytosine-5)-methyltransferase 3B (DNMT3B)
Regulated Target Methyltransferase-like protein 3 (METTL3)
Crosstalk relationship DNA modification → m6A
Disease Lung cancer
Crosstalk ID: M6ACROT02190
m6A Regulator Methyltransferase-like 3 (METTL3)
m6A Target Serine/threonine-protein kinase mTOR (MTOR)
Epigenetic Regulator DNA (cytosine-5)-methyltransferase 3B (DNMT3B)
Regulated Target Methyltransferase-like protein 3 (METTL3)
Crosstalk relationship DNA modification → m6A
Disease Lung cancer
Crosstalk ID: M6ACROT02191
m6A Regulator Methyltransferase-like 3 (METTL3)
m6A Target SVIL antisense RNA 1 (SVIL-AS1)
Epigenetic Regulator DNA (cytosine-5)-methyltransferase 3B (DNMT3B)
Regulated Target Methyltransferase-like protein 3 (METTL3)
Crosstalk relationship DNA modification → m6A
Disease Lung cancer
Crosstalk ID: M6ACROT02192
m6A Regulator Methyltransferase-like 3 (METTL3)
m6A Target SH3 domain-binding protein 5 (SH3BP5)
Epigenetic Regulator DNA (cytosine-5)-methyltransferase 3B (DNMT3B)
Regulated Target Methyltransferase-like protein 3 (METTL3)
Crosstalk relationship DNA modification → m6A
Disease Lung cancer
Crosstalk ID: M6ACROT03380
m6A Regulator Methyltransferase-like 3 (METTL3)
m6A Target microRNA let-7b (MIRLET7B)
Regulated Target Histone H3 lysine 27 acetylation (H3K27ac)
Crosstalk relationship Histone modification → m6A
Disease Lung cancer
Crosstalk ID: M6ACROT03393
m6A Regulator Methyltransferase-like 3 (METTL3)
m6A Target microRNA let-7b (MIRLET7B)
Regulated Target Histone H3 lysine 4 monomethylation (H3K4me1)
Crosstalk relationship Histone modification → m6A
Disease Lung cancer
Crosstalk ID: M6ACROT05549
m6A Regulator Methyltransferase-like 3 (METTL3)
m6A Target microRNA let-7b (MIRLET7B)
Epigenetic Regulator MicroRNA let-7b (MIRLET7B)
Crosstalk relationship m6A → ncRNA
Disease Lung cancer
References
Ref 1 mRNA circularization by METTL3-eIF3h enhances translation and promotes oncogenesis. Nature. 2018 Sep;561(7724):556-560. doi: 10.1038/s41586-018-0538-8. Epub 2018 Sep 19.
Ref 2 Stimulation of Let-7 Maturation by Metformin Improved the Response to Tyrosine Kinase Inhibitor Therapy in an m6A Dependent Manner. Front Oncol. 2022 Jan 6;11:731561. doi: 10.3389/fonc.2021.731561. eCollection 2021.