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Discovery of Survivin Inhibitors Part 1: Screening the Harbor Branch Pure Compound Library

Survivin is a 16.5 KDa protein whose functions include promoting cellular mitosis, angiogenesis, and senescence as well as inhibiting apoptosis. Higher survivin expression is found in cancer tissues than normal tissues, and this expression correlates with disease progression and aggressiveness. Surv...

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Autores principales: Guzmán, Esther A., Pitts, Tara P., Tandberg, Kirstie R., Winder, Priscilla L., Wright, Amy E.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7911841/
https://www.ncbi.nlm.nih.gov/pubmed/33573152
http://dx.doi.org/10.3390/md19020073
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author Guzmán, Esther A.
Pitts, Tara P.
Tandberg, Kirstie R.
Winder, Priscilla L.
Wright, Amy E.
author_facet Guzmán, Esther A.
Pitts, Tara P.
Tandberg, Kirstie R.
Winder, Priscilla L.
Wright, Amy E.
author_sort Guzmán, Esther A.
collection PubMed
description Survivin is a 16.5 KDa protein whose functions include promoting cellular mitosis, angiogenesis, and senescence as well as inhibiting apoptosis. Higher survivin expression is found in cancer tissues than normal tissues, and this expression correlates with disease progression and aggressiveness. Survivin has been validated as a clinical target for cancer. Small molecules are important antagonists of survivin levels in cancer cells. A structurally diverse library of genetically encoded small molecules (natural products) derived from marine plants, invertebrates, and microbes was screened for their ability to reduce expression levels of survivin in the DLD-1 colon adenocarcinoma and the A549 nonsmall cell lung carcinoma cell lines. This led to the identification of this novel activity for the known compounds eryloside E, ilicicolin H, tanzawaic acid A, and p-hydroxyphenopyrrozin. Both eryloside E and ilicicolin H showed the ability to reduce survivin expression in the low micromolar range against both cell lines.
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spelling pubmed-79118412021-02-28 Discovery of Survivin Inhibitors Part 1: Screening the Harbor Branch Pure Compound Library Guzmán, Esther A. Pitts, Tara P. Tandberg, Kirstie R. Winder, Priscilla L. Wright, Amy E. Mar Drugs Article Survivin is a 16.5 KDa protein whose functions include promoting cellular mitosis, angiogenesis, and senescence as well as inhibiting apoptosis. Higher survivin expression is found in cancer tissues than normal tissues, and this expression correlates with disease progression and aggressiveness. Survivin has been validated as a clinical target for cancer. Small molecules are important antagonists of survivin levels in cancer cells. A structurally diverse library of genetically encoded small molecules (natural products) derived from marine plants, invertebrates, and microbes was screened for their ability to reduce expression levels of survivin in the DLD-1 colon adenocarcinoma and the A549 nonsmall cell lung carcinoma cell lines. This led to the identification of this novel activity for the known compounds eryloside E, ilicicolin H, tanzawaic acid A, and p-hydroxyphenopyrrozin. Both eryloside E and ilicicolin H showed the ability to reduce survivin expression in the low micromolar range against both cell lines. MDPI 2021-01-30 /pmc/articles/PMC7911841/ /pubmed/33573152 http://dx.doi.org/10.3390/md19020073 Text en © 2021 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Guzmán, Esther A.
Pitts, Tara P.
Tandberg, Kirstie R.
Winder, Priscilla L.
Wright, Amy E.
Discovery of Survivin Inhibitors Part 1: Screening the Harbor Branch Pure Compound Library
title Discovery of Survivin Inhibitors Part 1: Screening the Harbor Branch Pure Compound Library
title_full Discovery of Survivin Inhibitors Part 1: Screening the Harbor Branch Pure Compound Library
title_fullStr Discovery of Survivin Inhibitors Part 1: Screening the Harbor Branch Pure Compound Library
title_full_unstemmed Discovery of Survivin Inhibitors Part 1: Screening the Harbor Branch Pure Compound Library
title_short Discovery of Survivin Inhibitors Part 1: Screening the Harbor Branch Pure Compound Library
title_sort discovery of survivin inhibitors part 1: screening the harbor branch pure compound library
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7911841/
https://www.ncbi.nlm.nih.gov/pubmed/33573152
http://dx.doi.org/10.3390/md19020073
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