ORCID ID
Bioorganic and Medicinal Chemistry Letters
Document Type
Article
Publication Date
2017
Publication Title
Bioorganic & Medicinal Chemistry Letters
Abstract
Histone deacetylase (HDAC) inhibitors modulate various cellular functions including proliferation, differentiation, and apoptosis. Vorinostat (SuberAniloHydroxamic Acid, SAHA) is the first HDAC inhibitor approved by FDA for cancer treatment. However, SAHA distributes in cancer tissue and normal tissue in similar levels. It will be ideal to selectively deliver SAHA into cancer cells. Rapidly growing cancer cells have a great need of cholesterol. Low-density lipoprotein (LDL) is the major cholesterol carrier in plasma and its uptake is mediated by LDL-receptor (LDL-R), a glycoprotein overexpressed on the surface of cancer cells. Herein, we designed and synthesized a SAHA cholesterol conjugate, and further formed the conjugate containing particles with LDL as the carrier. The diameters of the particles were determined. The inhibitory activity of the particles carrying the conjugate was determined with cancer cell proliferation assay, and the hydrolysis of the conjugate by the enzymes in cancer cells was confirmed with LC–MS/MS.
Recommended Citation
Idippily, Nethrie D.; Gan, Chunfang; Orefice, Paul; Peterson, Jane; and Su, Bin Ph.D., "Synthesis of Vorinostat and Cholesterol Conjugate to Enhance the Cancer Cell Uptake Selectivity" (2017). Chemistry Faculty Publications. 528.
https://engagedscholarship.csuohio.edu/scichem_facpub/528
Creative Commons License
This work is licensed under a Creative Commons Attribution-NonCommercial-No Derivative Works 4.0 International License.
DOI
10.1016/j.bmcl.2017.01.025
Version
Postprint
Publisher's Statement
Link to publisher version: http://dx.doi.org/10.1016/j.bmcl.2017.01.025
Volume
27
Comments
This work was supported by Center for Gene Regulation in Health and Disease (GRHD) of Cleveland State University and Ohio Department of Development (ODOD) and Cleveland State University summer undergraduate research program.