Taming Amphotericin B.
Publication
, Journal Article
Janout, V; Schell, WA; Thévenin, D; Yu, Y; Perfect, JR; Regen, SL
Published in: Bioconjug Chem
October 21, 2015
A strategy is introduced for enhancing the cellular selectivity of Amphotericin B (AmB) and other classes of membrane-disrupting agents. This strategy involves attaching the agent to a molecular umbrella to minimize the disruptive power of aggregated forms. Based on this approach, AmB has been coupled to a molecular umbrella derived from one spermidine and two cholic acid molecules and found to have antifungal activities approaching that of the native drug. However, in sharp contrast to AmB, the hemolytic activity and the cytotoxcity of this conjugate toward HEK293 T cells have been dramatically reduced.
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Published In
Bioconjug Chem
DOI
EISSN
1520-4812
Publication Date
October 21, 2015
Volume
26
Issue
10
Start / End Page
2021 / 2024
Location
United States
Related Subject Headings
- Structure-Activity Relationship
- Spermidine
- Organic Chemistry
- Humans
- Hemolytic Agents
- HEK293 Cells
- Erythrocytes
- Drug Evaluation, Preclinical
- Cholic Acid
- Antifungal Agents
Citation
APA
Chicago
ICMJE
MLA
NLM
Janout, V., Schell, W. A., Thévenin, D., Yu, Y., Perfect, J. R., & Regen, S. L. (2015). Taming Amphotericin B. Bioconjug Chem, 26(10), 2021–2024. https://doi.org/10.1021/acs.bioconjchem.5b00463
Janout, Vaclav, Wiley A. Schell, Damien Thévenin, Yuming Yu, John R. Perfect, and Steven L. Regen. “Taming Amphotericin B.” Bioconjug Chem 26, no. 10 (October 21, 2015): 2021–24. https://doi.org/10.1021/acs.bioconjchem.5b00463.
Janout V, Schell WA, Thévenin D, Yu Y, Perfect JR, Regen SL. Taming Amphotericin B. Bioconjug Chem. 2015 Oct 21;26(10):2021–4.
Janout, Vaclav, et al. “Taming Amphotericin B.” Bioconjug Chem, vol. 26, no. 10, Oct. 2015, pp. 2021–24. Pubmed, doi:10.1021/acs.bioconjchem.5b00463.
Janout V, Schell WA, Thévenin D, Yu Y, Perfect JR, Regen SL. Taming Amphotericin B. Bioconjug Chem. 2015 Oct 21;26(10):2021–2024.
Published In
Bioconjug Chem
DOI
EISSN
1520-4812
Publication Date
October 21, 2015
Volume
26
Issue
10
Start / End Page
2021 / 2024
Location
United States
Related Subject Headings
- Structure-Activity Relationship
- Spermidine
- Organic Chemistry
- Humans
- Hemolytic Agents
- HEK293 Cells
- Erythrocytes
- Drug Evaluation, Preclinical
- Cholic Acid
- Antifungal Agents