The DOI matches its Crossref record; 21 of the 21 references it cites were found in a registry or an index.
NPI-2358 is a tubulin-depolymerizing agent: in-vitro evidence for activity as a tumor vascular-disrupting agent
Abstract
The diketopiperazine NPI-2358 is a synthetic analog of NPI-2350, a natural product isolated from Aspergillus sp., which depolymerizes microtubules in A549 human lung carcinoma cells. Although structurally different from the colchicine-binding site agents reported to date, NPI-2358 binds to the colchicine-binding site of tubulin. NPI-2358 has potent in-vitro anti-tumor activity against various human tumor cell lines and maintains activity against tumor cell lines with various multidrug-resistant (MDR) profiles. In addition, when evaluated in proliferating human umbilical vein endothelial cells (HUVECs), concentrations as low as 10 nmol/l NPI-2358 induced tubulin depolymerization within 30 min. Furthermore, NPI-2358 dose dependently increases HUVEC monolayer permeability--an in-vitro model of tumor vascular collapse. NPI-2358 was compared with three tubulin-depolymerizing agents with vascular-disrupting activity: colchicine, vincristine and combretastatin A-4 (CA4). Results showed that the activity of NPI-2358 in HUVECs was more potent than either colchicine or vincristine; the profile of CA4 approached that of NPI-2358. Altogether, our data show that NPI-2358 is a potent anti-tumor agent which is active in MDR tumor cell lines, and is able to rapidly induce tubulin depolymerization and monolayer permeability in HUVECs. These data warrant further evaluation of NPI-2358 as a vascular-disrupting agent in vivo. Currently, NPI-2358 is in preclinical development for the treatment of cancer.
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Cites
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Cited by
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Metadata
- Authors
- Nicholson, B., Lloyd, G. K., Miller, B. R., Palladino, M. A., Kiso, Y., Hayashi, Y., & Neuteboom, S. T. C.
- Venue
- Anti-Cancer Drugs
- Published
- 2006-01
- Volume
- 17
- Issue
- 1
- Pages
- 25-31
- ISSN
- 0959-4973 (ISSN-L)
- OpenAlex
- W2034483653
- Cited by
- 260
- References
- 21
- FWCI
- 2.60
- Type
- journal article
- Language
- en
- Open access
- closed
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- CoChat. (2026). Citation check: NPI-2358 is a tubulin-depolymerizing agent: in-vitro evidence for activity as a tumor vascular-disrupting agent. https://app.cochat.ai/papers/10.1097/01.cad.0000182745.01612.8a
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- Nicholson, B., Lloyd, G. K., Miller, B. R., Palladino, M. A., Kiso, Y., Hayashi, Y., & Neuteboom, S. T. C. (2006). NPI-2358 is a tubulin-depolymerizing agent: in-vitro evidence for activity as a tumor vascular-disrupting agent. Anti-Cancer Drugs. https://doi.org/10.1097/01.cad.0000182745.01612.8a
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