There are considerable interests in the development of novel small-molecule CD73 inhibitors for the treatment of cancers, autoimmune diseases, precancerous syndromes, and other diseases associated with CD73 activity. Areas covered: The application claims novel substituted benzothiadiazine derivatives as CD73 inhibitors for the treatment of cancer, precancerous syndromes, AIDS, autoimmune diseases, infections, atherosclerosis, and ischemia-reperfusion injury. Many of the exemplified compounds have pIC50 values between 5 to 8.4 against CD73. Expert Opinion: These benzothiadiazine derivatives provide good leads for the discovery of potent CD73 inhibitors for the treatment of cancer and other diseases mediated by adenosine and its action on adenosine receptors.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1080/13543776.2018.1407756 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Ultraviolet (UV)-induced DNA mutations produce genetic drivers of cutaneous melanoma initiation and numerous neoantigens that can trigger anti-tumor immune responses in the host. Consequently, melanoma cells must rapidly evolve to evade immune detection by simultaneously modulating cell-autonomous epigenetic mechanisms and tumor-microenvironment interactions. Angiogenesis has been implicated in this process; although an increase of vasculature initiates the immune response in normal tissue, solid tumors manage to somehow enhance blood flow while preventing immune cell infiltration.
View Article and Find Full Text PDFSimultaneous blockade of the CD73/EGFR axis inhibits tumor growth.
IUBMB Life
January 2025
Immunology Research Center, Tabriz University of Medical Sciences, Tabriz, Iran.
Targeting the influencing factors in tumor growth and expansion in the tumor microenvironment is one of the key approaches to cancer immunotherapy. Various factors in the tumor microenvironment can in cooperation stimulate tumor growth, suppress anti-tumor immune responses, promote drug resistance, and ultimately enhance tumor recurrence. Therefore, due to the dependence and close cooperation of these axes, their combined targeting can have a greater effect compared to their individual targeting.
View Article and Find Full Text PDFAn antibody cocktail targeting two different CD73 epitopes enhances enzyme inhibition and tumor control.
Nat Commun
December 2024
Key Laboratory of Immune Response and Immunotherapy, Guangzhou Institutes of Biomedicine and Health (GIBH), Chinese Academy of Scienes, Guangzhou, China.
CD73, an ectoenzyme responsible for adenosine production, is often elevated in immuno-suppressive tumor environments. Inhibition of CD73 activity holds great promise as a therapeutic strategy for CD73-expressing cancers. In this study, we have developed a therapeutic anti-human CD73 antibody cocktail, HB0045.
View Article and Find Full Text PDFCD73: agent development potential and its application in diabetes and atherosclerosis.
Front Immunol
December 2024
The Affiliated Hospital of Qingdao University, Qingdao University, Qingdao Cancer Institute, Qingdao, Shandong, China.
CD73, an important metabolic and immune escape-promoting gene, catalyzes the hydrolysis of adenosine monophosphate (AMP) to adenosine (ADO). AMP has anti-inflammatory and vascular relaxant properties, while ADO has a strong immunosuppressive effect, suggesting that CD73 has pro-inflammatory and immune escape effects. However, CD73 also decreased proinflammatory reaction, suggesting that CD73 has a positive side to the body.
View Article and Find Full Text PDFCo-Delivery of aPD-L1 and CD73 Inhibitor Using Calcium Phosphate Nanoparticles for Enhanced Melanoma Immunotherapy with Reduced Toxicity.
Adv Sci (Weinh)
December 2024
Xiangya School of Pharmaceutical Sciences, Central South University, Changsha, Hunan, 410013, China.
Melanoma, a malignant skin tumor, presents significant treatment challenges, particularly in unresectable and metastatic cases. While immune checkpoint inhibitors (ICIs) targeting PD-1/PD-L1 have brought new hope, their efficacy is limited by low response rates and significant immune-mediated adverse events (irAEs). Through multi-omics data analysis, it is discovered that the spatial co-localization of CD73 and PD-L1 in melanoma correlates with improved progression-free survival (PFS), suggesting a synergistic potential of their inhibitors.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!