The Anti-Cancer Effect of A3 Adenosine Receptor Agonists : A Novel, Targeted Therapy

The A3 adenosine receptor (A3AR) is highly expressed in various human solid tumor cells whereas low expression is found in the adjacent normal tissues. Activation of the A3AR with synthetic highly selective agonists, such as IB-MECA, Cl-IB-MECA or LJ529, induces tumor growth inhibition of melanoma, lymphoma, breast, hepatoma, prostate and colon carcinoma cells both in vitro and in vivo. Two molecular events take place upon receptor activation and include: a. receptor internalization and subsequent degradation, followed by decreased receptor mRNA and protein expression level. b. modulation of down-stream signal transduction pathways, including those related to Wnt and NF-κB. Subsequently, the levels of cyclin D1 and c-Myc are decreased leading to tumor growth inhibition. IB-MECA synergizes with chemotherapeutic agents to yield an additive anti-tumor effect and protects against myelotoxicity induced by chemotherapy. Taken together, A3AR agonists may be suggested as a new family of orally bioavailable compounds to be developed as potent inhibitors of malignant diseases.

Media Type:

Electronic Article

Year of Publication:

2007

Publication:

2007

Contained In:

To Main Record - volume:7

Contained In:

Immunology, endocrine & metabolic agents in medicinal chemistry - 7(2007) vom: 20. Aug., Seite 298-303

Language:

English

Contributors:

Fishman, P [Author]
Jacobson, K A [Author]
Ochaion, A [Author]
Cohen, S [Author]
Bar-Yehuda, S [Author]

Links:

Volltext

Keywords:

A3 Adenosine receptor
Anti-cancer effect
Journal Article
NF-κB.
PKB/Akt
Synthetic agonists
Wnt

Notes:

Date Revised 08.11.2023

published: Print

Citation Status PubMed-not-MEDLINE

doi:

10.2174/187152207781369878

Clinical Trials/ Publications:


Study related publications :

funding:

Supporting institution / Project title:

PPN (Catalogue-ID):

NLM333617711