Drug Information

Drug (ID: DG00927) and It's Reported Resistant Information

• Name: Gardiquimod
• Synonyms: Gardiquimod; 1020412-43-4; UNII-Y3W4QVW5BY; Y3W4QVW5BY; 1-[4-amino-2-(ethylaminomethyl)imidazo[4,5-c]quinolin-1-yl]-2-methylpropan-2-ol; CHEMBL1085742; 1-{4-amino-2-[(ethylamino)methyl]-1H-imidazo[4,5-c]quinolin-1-yl}-2-methylpropan-2-ol; 1-(4-amino-2-((ethylamino)methyl)-1H-imidazo[4,5-c]quinolin-1-yl)-2-methylpropan-2-ol; 1-yl]-2-methylpropan-2-ol; SCHEMBL1256396; BCP30187; EX-A5848; VQB41243; BDBM50320067; ZINC40897136; NCGC00387769-01; NCGC00387769-02; NCGC00387769-04; AS-82322; HY-103697; CS-0032943; J3.515.101J; J-000553; 1-[4-Amino-2-(ethylaminomethyl)imidazo[4,5-c]quinolin-; 1-(4-amino-2-ethylaminomethylimidazo[4,5-c]quinolin-1-yl)-2-methylpropan-2-ol; 1-[4-amino-2-(ethylaminomethyl)imidazo[4,5-c]quinolin-1-yl]-2-methyl-propan-2-ol; 1H-Imidazo(4,5-C)quinoline-1-ethanol, 4-amino-2-((ethylamino)methyl)-alpha,alpha-dimethyl-; 4-Amino-2-((ethylamino)methyl)-alpha,alpha-dimethyl-1H-imidazo(4,5-C)quinoline-1-ethanol; 9K3
• Drug Resistance Disease(s):
  Disease(s) with Resistance Information Discovered by Cell Line Test for This Drug (3 diseases)
  Breast cancer [ICD-11: 2C60]; [1]
  Melanoma [ICD-11: 2C30]; [1]
  Prostate cancer [ICD-11: 2C82]; [1]
• Target: .; NOUNIPROTAC; [1]
• Formula: C17H23N5O
• IsoSMILES: CCNCC1=NC2=C(N1CC(C)(C)O)C3=CC=CC=C3N=C2N
• InChI: 1S/C17H23N5O/c1-4-19-9-13-21-14-15(22(13)10-17(2,3)23)11-7-5-6-8-12(11)20-16(14)18/h5-8,19,23H,4,9-10H2,1-3H3,(H2,18,20)
• InChIKey: FHJATBIERQTCTN-UHFFFAOYSA-N
• PubChem CID: 44592366

Type(s) of Resistant Mechanism of This Drug

  IDUE: Irregularity in Drug Uptake and Drug Efflux

Drug Resistance Data Categorized by Their Corresponding Diseases

ICD-02: Benign/in-situ/malignant neoplasm

Melanoma [ICD-11: 2C30]

Drug Resistance Data Categorized by Their Corresponding Mechanisms

Irregularity in Drug Uptake and Drug Efflux (IDUE)

Key Molecule: Multidrug resistance protein 1 (ABCB1) [1]

• Molecule Alteration: Expression; Up-regulation
• Resistant Disease: Melanoma [ICD-11: 2C30.0]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: A549 cells; Lung; Homo sapiens (Human); CVCL_0023
• Experiment for Molecule Alteration: Western blotting analysis
• Experiment for Drug Resistance: Resazurin Cell Viability Assay
• Mechanism Description: Imidazoquinolines IMQ, RSQ, and GDQ are substrates for P-gp and begins to elucidate differences in their trafficking in cancer cells as a consequence of acquired drug resistance. We believe this work that begins to examine imidazoquinoline trafficking will prove useful in the future rational design of immunotherapeutics with enhanced susceptibility to P-gp efflux that enable increased bioavailability, in MDR cancers.

Breast cancer [ICD-11: 2C60]

Drug Resistance Data Categorized by Their Corresponding Mechanisms

Irregularity in Drug Uptake and Drug Efflux (IDUE)

Key Molecule: Multidrug resistance protein 1 (ABCB1) [1]

• Molecule Alteration: Expression; Up-regulation
• Resistant Disease: Breast cancer [ICD-11: 2C60.3]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: COLO205 cells; Colon; Homo sapiens (Human); CVCL_F402
• Experiment for Molecule Alteration: Western blotting analysis
• Experiment for Drug Resistance: Resazurin Cell Viability Assay
• Mechanism Description: Imidazoquinolines IMQ, RSQ, and GDQ are substrates for P-gp and begins to elucidate differences in their trafficking in cancer cells as a consequence of acquired drug resistance. We believe this work that begins to examine imidazoquinoline trafficking will prove useful in the future rational design of immunotherapeutics with enhanced susceptibility to P-gp efflux that enable increased bioavailability, in MDR cancers.

Prostate cancer [ICD-11: 2C82]

Drug Resistance Data Categorized by Their Corresponding Mechanisms

Irregularity in Drug Uptake and Drug Efflux (IDUE)

Key Molecule: Multidrug resistance protein 1 (ABCB1) [1]

• Molecule Alteration: Expression; Up-regulation
• Resistant Disease: Prostate cancer [ICD-11: 2C82.0]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: Hep3B cells; Liver; Homo sapiens (Human); CVCL_0326
• Experiment for Molecule Alteration: Western blotting analysis
• Experiment for Drug Resistance: Resazurin Cell Viability Assay
• Mechanism Description: Imidazoquinolines IMQ, RSQ, and GDQ are substrates for P-gp and begins to elucidate differences in their trafficking in cancer cells as a consequence of acquired drug resistance. We believe this work that begins to examine imidazoquinoline trafficking will prove useful in the future rational design of immunotherapeutics with enhanced susceptibility to P-gp efflux that enable increased bioavailability, in MDR cancers.

References

• Ref 1: Acquired Drug Resistance Enhances Imidazoquinoline Efflux by P-Glycoprotein .Pharmaceuticals (Basel). 2021 Dec 10;14(12):1292. doi: 10.3390/ph14121292. 10.3390/ph14121292