---
OA_type: free access
_id: '865'
abstract:
- lang: eng
  text: Research on existing drugs often discovers novel mechanisms of their action
    and leads to the expansion of their therapeutic scope and subsequent remarketing.
    The Wnt signaling pathway is of the immediate therapeutic relevance, as it plays
    critical roles in cancer development and progression. However, drugs which disrupt
    this pathway are unavailable despite the high demand. Here we report an attempt
    to identify antagonists of the Wnt-FZD interaction among the library of the FDA-approved
    drugs. We performed an in silico screening which brought up several potential
    antagonists of the ligand-receptor interaction. 14 of these substances were tested
    using the TopFlash luciferase reporter assay and four of them identified as active
    and specific inhibitors of the Wnt3a-induced signaling. However, further analysis
    through GTP-binding and β-catenin stabilization assays showed that the compounds
    do not target the Wnt-FZD pair, but inhibit the signaling at downstream levels.
    We further describe the previously unknown inhibitory activity of an anti-leprosy
    drug clofazimine in the Wnt pathway and provide data demonstrating its efficiency
    in suppressing growth of Wnt-dependent triple-negative breast cancer cells. These
    data provide a basis for further investigations of the efficiency of clofazimine
    in treatment of Wnt-dependent cancers.
article_processing_charge: No
article_type: original
author:
- first_name: Alexey
  full_name: Koval, Alexey
  last_name: Koval
- first_name: Peter
  full_name: Vlasov, Peter
  last_name: Vlasov
- first_name: Polina
  full_name: Shichkova, Polina
  last_name: Shichkova
- first_name: S
  full_name: Khunderyakova, S
  last_name: Khunderyakova
- first_name: Yury
  full_name: Markov, Yury
  last_name: Markov
- first_name: J
  full_name: Panchenko, J
  last_name: Panchenko
- first_name: A
  full_name: Volodina, A
  last_name: Volodina
- first_name: Fyodor
  full_name: Kondrashov, Fyodor
  id: 44FDEF62-F248-11E8-B48F-1D18A9856A87
  last_name: Kondrashov
  orcid: 0000-0001-8243-4694
- first_name: Vladimir
  full_name: Katanaev, Vladimir
  last_name: Katanaev
citation:
  ama: Koval A, Vlasov P, Shichkova P, et al. Anti leprosy drug clofazimine inhibits
    growth of triple-negative breast cancer cells via inhibition of canonical Wnt
    signaling. <i>Biochemical Pharmacology</i>. 2014;87(4):571-578. doi:<a href="https://doi.org/10.1016/j.bcp.2013.12.007">10.1016/j.bcp.2013.12.007</a>
  apa: Koval, A., Vlasov, P., Shichkova, P., Khunderyakova, S., Markov, Y., Panchenko,
    J., … Katanaev, V. (2014). Anti leprosy drug clofazimine inhibits growth of triple-negative
    breast cancer cells via inhibition of canonical Wnt signaling. <i>Biochemical
    Pharmacology</i>. Elsevier. <a href="https://doi.org/10.1016/j.bcp.2013.12.007">https://doi.org/10.1016/j.bcp.2013.12.007</a>
  chicago: Koval, Alexey, Peter Vlasov, Polina Shichkova, S Khunderyakova, Yury Markov,
    J Panchenko, A Volodina, Fyodor Kondrashov, and Vladimir Katanaev. “Anti Leprosy
    Drug Clofazimine Inhibits Growth of Triple-Negative Breast Cancer Cells via Inhibition
    of Canonical Wnt Signaling.” <i>Biochemical Pharmacology</i>. Elsevier, 2014.
    <a href="https://doi.org/10.1016/j.bcp.2013.12.007">https://doi.org/10.1016/j.bcp.2013.12.007</a>.
  ieee: A. Koval <i>et al.</i>, “Anti leprosy drug clofazimine inhibits growth of
    triple-negative breast cancer cells via inhibition of canonical Wnt signaling,”
    <i>Biochemical Pharmacology</i>, vol. 87, no. 4. Elsevier, pp. 571–578, 2014.
  ista: Koval A, Vlasov P, Shichkova P, Khunderyakova S, Markov Y, Panchenko J, Volodina
    A, Kondrashov F, Katanaev V. 2014. Anti leprosy drug clofazimine inhibits growth
    of triple-negative breast cancer cells via inhibition of canonical Wnt signaling.
    Biochemical Pharmacology. 87(4), 571–578.
  mla: Koval, Alexey, et al. “Anti Leprosy Drug Clofazimine Inhibits Growth of Triple-Negative
    Breast Cancer Cells via Inhibition of Canonical Wnt Signaling.” <i>Biochemical
    Pharmacology</i>, vol. 87, no. 4, Elsevier, 2014, pp. 571–78, doi:<a href="https://doi.org/10.1016/j.bcp.2013.12.007">10.1016/j.bcp.2013.12.007</a>.
  short: A. Koval, P. Vlasov, P. Shichkova, S. Khunderyakova, Y. Markov, J. Panchenko,
    A. Volodina, F. Kondrashov, V. Katanaev, Biochemical Pharmacology 87 (2014) 571–578.
date_created: 2018-12-11T11:48:55Z
date_published: 2014-02-15T00:00:00Z
date_updated: 2026-09-09T11:17:42Z
day: '15'
doi: 10.1016/j.bcp.2013.12.007
extern: '1'
external_id:
  pmid:
  - '24355563'
fulldoi: https://doi.org/10.1016/j.bcp.2013.12.007
intvolume: '        87'
issue: '4'
language:
- iso: eng
month: '02'
oa_version: None
page: 571 - 578
pmid: 1
publication: Biochemical Pharmacology
publication_identifier:
  eissn:
  - 1873-2968
  issn:
  - 0006-2952
publication_status: published
publisher: Elsevier
publist_id: '6782'
status: public
title: Anti leprosy drug clofazimine inhibits growth of triple-negative breast cancer
  cells via inhibition of canonical Wnt signaling
type: journal_article
user_id: 317138e5-6ab7-11ef-aa6d-ffef3953e345
volume: 87
year: '2014'
...