The DOI matches its Crossref record; 107 of the 107 references it cites were found in a registry or an index.
Colchicine-Binding Site Inhibitors from Chemistry to Clinic: A Review
Open accessAbstract
It is over 50 years since the discovery of microtubules, and they have become one of the most important drug targets for anti-cancer therapies. Microtubules are predominantly composed of the protein tubulin, which contains a number of different binding sites for small-molecule drugs. There is continued interest in drug development for compounds targeting the colchicine-binding site of tubulin, termed colchicine-binding site inhibitors (CBSIs). This review highlights CBSIs discovered through diverse sources: from natural compounds, rational design, serendipitously and via high-throughput screening. We provide an update on CBSIs reported in the past three years and discuss the clinical status of CBSIs. It is likely that efforts will continue to develop CBSIs for a diverse set of cancers, and this review provides a timely update on recent developments.
Overview
The claims and statistics of this paper haven’t been checked yet.
Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.
Integrity signals
Registry
Cites
Statistics
Verification
Claims the paper makes
The claims and statistics of this paper haven’t been checked yet.
Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.
Self-check
Percentages, sums and reported differences re-computed from the paper’s own numbers.
The self-check needs the paper’s full text.
Citations
Cites
El-Khoueiry, A. B., Sangro, B., Yau, T., Crocenzi, T. S., Kudo, M., Hsu, C., Kim, T.-Y., Choo, S.-P., Trojan, J., Welling, T. H., et al. (2017) · The Lancet · doi:10.1016/s0140-6736(17)31046-2 · Cited by 4,280
Structure of the αβ tubulin dimer by electron crystallography
Nogales, E., Wolf, S. G., & Downing, K. H. (1998) · Nature · doi:10.1038/34465 · Cited by 2,076
A Comprehensive Survey of Ras Mutations in Cancer
Prior, I. A., Lewis, P. D., & Mattos, C. (2012) · Cancer Research · doi:10.1158/0008-5472.can-11-2612 · Cited by 2,063 · cited 1×
“The effectiveness of chemotherapy is limited in KRAS-driven cancers and is often associated with toxicity [169].”
BackgroundInsight into tubulin regulation from a complex with colchicine and a stathmin-like domain
Ravelli, R. B. G., Gigant, B., Curmi, P. A., Jourdain, I., Lachkar, S., Sobel, A., & Knossow, M. (2004) · Nature · doi:10.1038/nature02393 · Cited by 1,630
Photopharmacology: Beyond Proof of Principle
Velema, W. A., Szymanski, W., & Feringa, B. L. (2014) · Journal of the American Chemical Society · doi:10.1021/ja413063e · Cited by 1,178
Etoposide: four decades of development of a topoisomerase II inhibitor
Hande, K. R. (1998) · European Journal of Cancer · doi:10.1016/s0959-8049(98)00228-7 · Cited by 949
Isolation and structure of the strong cell growth and tubulin inhibitor combretastatin A-4
Pettit, G. R., Singh, S. B., Hamel, E., Lin, C. M., Alberts, D. S., & Garcia-Kendal, D. (1989) · Experientia · doi:10.1007/bf01954881 · Cited by 786
A Roadmap to Success in Photopharmacology
Broichhagen, J., Frank, J. A., & Trauner, D. (2015) · Accounts of Chemical Research · doi:10.1021/acs.accounts.5b00129 · Cited by 730
An overview of tubulin inhibitors that interact with the colchicine binding site
Lu, Y., Chen, J., Xiao, M., Li, W., & Miller, D. D. (2012) · Pharmaceutical Research · doi:10.1007/s11095-012-0828-z · Cited by 709
Stuck in Division or Passing through
Rieder, C. L., & Maiato, H. (2004) · Developmental Cell · doi:10.1016/j.devcel.2004.09.002 · Cited by 657
Cited by
Regulation of microtubule dynamics, mechanics and function through the growing tip
Gudimchuk, N. B., & McIntosh, J. R. (2021) · Nature Reviews Molecular Cell Biology · doi:10.1038/s41580-021-00399-x · Cited by 369
Horin, L. J., Sonnett, M., Li, B., & Mitchison, T. J. (2025) · doi:10.1101/2025.01.22.632572 · Cited by 4
Metadata
- Authors
- McLoughlin, E. C., & O’Boyle, N. M.
- Venue
- Pharmaceuticals
- Publisher
- MDPI AG
- Published
- 2020-01-03
- Volume
- 13
- Issue
- 1
- Pages
- 8
- ISSN
- 1424-8247 (ISSN-L)
- OpenAlex
- W2996972660
- Cited by
- 316
- References
- 107
- FWCI
- 19.62
- Type
- journal article
- Language
- en
- Open access
- gold
About these checks
Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
Statistics and arithmetic are recomputed, not judged.
Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.
What counts as a claim ›How we measure confidence ›How we check this ›
Are you an author, or do you see a problem with this page? Request a review
How to cite
Cite CoChat for the checks on this page, and the paper for its own findings.
- This page
- CoChat. (2026). Citation check: Colchicine-Binding Site Inhibitors from Chemistry to Clinic: A Review. https://app.cochat.ai/papers/10.3390/ph13010008
- The paper
- McLoughlin, E. C., & O’Boyle, N. M. (2020). Colchicine-Binding Site Inhibitors from Chemistry to Clinic: A Review. Pharmaceuticals. https://doi.org/10.3390/ph13010008
Data sources
Bibliographic data: Semantic Scholar, OpenAlex, Crossref.
Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
