Abstract 1227: Identification of the molecular target of azithromycin as an autophagy inhibitor and its potential application in cancer therapeutics

UHRF1 is a master regulator of epigenome as it coordinates DNA methylation and histone modifications. Compelling evidence suggests a strong link between UHRF1 overexpression and tumorigenesis, substantiating its ability to act as a potential biomarker for cancer diagnosis and prognosis. UHRF1 also mediates repair of damaged DNA that makes cancer cells resistant toward cytocidal drugs. Hence, understanding the molecular mechanism of UHRF1 regulation would help in developing cancer therapeutics. Natural compounds have shown applicability to downregulate UHRF1 leading to growth arrest and apoptosis in cancer cells.

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Sonochemically prepared BSA microspheres containing Gemcitabine, and their potential application in renal cancer therapeutics

Acta Biomaterialia ◽

10.1016/j.actbio.2009.05.003 ◽

2009 ◽

Vol 5 (8) ◽

pp. 3031-3037 ◽

Cited By ~ 29

Author(s):

Olga Grinberg ◽

Aharon Gedanken ◽

Chitta Ranjan Patra ◽

Sujata Patra ◽

Priyabrata Mukherjee ◽

...

Keyword(s):

Renal Cancer ◽

Potential Application ◽

Cancer Therapeutics

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Peptide-functionalized gold nanoparticles: versatile biomaterials for diagnostic and therapeutic applications

Biomaterials Science ◽

10.1039/c7bm00006e ◽

2017 ◽

Vol 5 (5) ◽

pp. 872-886 ◽

Cited By ~ 72

Author(s):

Jingyi Zong ◽

Steven L. Cobb ◽

Neil R. Cameron

Keyword(s):

Drug Delivery ◽

Gold Nanoparticles ◽

Targeted Drug Delivery ◽

Potential Application ◽

Cancer Therapeutics ◽

Therapeutic Applications ◽

Functionalized Gold Nanoparticles ◽

Anti Cancer ◽

Targeted Drug ◽

Oligonucleotide Delivery

This review provides an overview of the current methods used for preparing peptide-functionalized GNPs, and discusses the key properties of this class of biomaterial. In particular, their potential application in areas of sensing, targeted drug delivery, anti-cancer therapeutics and oligonucleotide delivery are discussed.

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miR-149 as a Potential Molecular Target for Cancer

Current Medicinal Chemistry ◽

10.2174/0929867324666170718102738 ◽

2018 ◽

Vol 25 (9) ◽

pp. 1046-1054 ◽

Cited By ~ 8

Author(s):

Suet H. Ow ◽

Pei J. Chua ◽

Boon H. Bay

Keyword(s):

Cancer Progression ◽

Cancer Therapeutics ◽

Molecular Target ◽

Circular Rnas ◽

Extensive Literature ◽

Cancer Type ◽

Efficient Delivery ◽

Pubmed Database ◽

Anti Cancer ◽

Cancer Spread

Background: MicroRNAs (miRNAs) are frequently dysregulated in cancers and serve as attractive targets for prognostication and therapeutic applications. Besides cancer, the biological functions of miR-149 have been studied in various diseases. This review aims to summarize the reports available in the literature, regarding miR-149 as a molecular target for cancer therapeutics. Methods: An extensive literature search was conducted using the Pubmed database to sieve out articles related to the roles of miR-149 in carcinogenesis and cancer progression, and potential miRNA-based therapies. A total of 89 publications were selected for inclusion in this review. Results: Depending on the cancer type, miR-149 can behave either as a tumor suppressor or as an ‘onco-miR' that promotes tumorigenesis and cancer spread, suggesting that this miRNA has diverse functions. Potential miRNA-based therapies include the use of miRNA mimics, miRNA inhibitors, demethylating agents and circular RNAs. Conclusion: Although targeting miRNA is an attractive anti-cancer strategy, not all cancers can be treated by the same miRNA-based strategy. A comprehensive understanding of miRNA regulatory mechanism is also necessary to improve the design of miRNA-based therapeutics and there is a need for safe and efficient delivery methods when using this approach for anti-cancer treatment.

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Discovery and mechanistic characterization of a novel AhR receptor ligand that induces apoptosis in cancer cells

10.21203/rs.3.rs-131951/v1 ◽

2020 ◽

Author(s):

Edmond O'Donnell ◽

Hyo Sang Jang ◽

Daniel Liefwalker ◽

Nancy Kerkvliet ◽

Siva Kumar Kolluri

Keyword(s):

Cancer Cells ◽

Cancer Cell ◽

Fas Ligand ◽

Cancer Therapeutics ◽

Molecular Target ◽

Therapeutic Interventions ◽

Dependent Manner ◽

New Class ◽

Anti Cancer

Abstract Background: The aryl hydrocarbon receptor (AhR) is a ligand-activated transcription factor and a member of the bHLH/PAS (basic Helix-Loop-Helix/Per-Arnt-Sim) family of proteins. The AhR was cloned and characterized for its role in mediating the toxicity of dioxins. Subsequent research has identified AhR’s role in the suppression of cancer cell growth. We hypothesized that that the AhR is a molecular target for therapeutic interventions, and that activation of the AhR by select AhR modulators in cancer cells could have anti-cancer properties including cell death. This study describes the discovery and characterization of a new class of anti-cancer agents targeting the AhR.Methods: We employed two independent small molecule screening approaches to identify novel modulators of the AhR with unique anti-cancer properties. We established the AhR selective effects of a highly selective modulator in cancer cells with or without the AhR expression and identified the mechanism of action of this anti-cancer compound.Results: We report the identification of CGS-15943, uniquely selective AhR modulator, that activates AhR signaling and induces apoptosis in an AhR-dependent manner in liver and breast cancer cell models. Investigation of the downstream signaling pathway of this newly identified modulator revealed novel upregulation of Fas-ligand, which is required for AhR-mediated apoptosis.Conclusions: We identified CGS-15943 as a novel AhR-selective modulator with anti-cancer properties using two parallel and distinct screening strategies. This compound induced AhR-dependent apoptosis in multiple mouse and human liver cancer cells. Our results provide a basis for the development of a new class of anti-cancer therapeutics targeting an underappreciated molecular target, the AhR.

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