Drug name: Topotecan + Vismodegib


Related CSCTT Targets

ABCG2 [ref.1]Q9UNQ0

Topotecan

Cas.no PubChem ID
123948-87-8 60700
Known Target
DNA topoisomerase 1P11387
DNA topoisomerase I, mitochondrialQ969P6
DNA
Structure
...
Introduction
Topotecan, a semi-synthetic derivative of camptothecin (a plant alkaloid obtained from the Camptotheca acuminata tree), is an anti-tumor drug with topoisomerase I-inhibitory activity similar to irinotecan. DNA topoisomerases are enzymes in the cell nucleus that regulate DNA topology (3-dimensional conformation) and facilitate nuclear processes such as DNA replication, recombination, and repair. During these processes, DNA topoisomerase I creates reversible single-stranded breaks in double-stranded DNA, allowing intact single DNA strands to pass through the break and relieve the topologic constraints inherent in supercoiled DNA.

Vismodegib

Cas.no PubChem ID
879085-55-9 24776445
Known Target
Smoothened homologQ99835
Structure
...
Introduction
Vismodegib (trade name Erivedge) is a drug for the treatment of basal-cell carcinoma (BCC). It acts as a cyclopamine-competitive antagonist of the smoothened receptor (SMO) which is part of the hedgehog signaling pathway. SMO inhibition causes the transcription factors GLI1 and GLI2 to remain inactive, which prevents the expression of tumor mediating genes within the hedgehog pathway. This pathway is pathogenetically relevant in more than 90% of basal-cell carcinomas.

Reference

  • [1] Hedgehog pathway inhibitor HhAntag691 is a potent inhibitor of ABCG2/BCRP and ABCB1/Pgp. Zhang, Y., et al. (2009).Neoplasia.11(1):96-101.
    19107236. [ 19107236 ]

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