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The therapeutic potential of targeting CD73 and CD73-derived adenosine in melanoma
Biochimie, 2020The hypoxic environment of melanoma results in CD73 upregulation on the surface of various tumor microenvironment (TME) cells including tumor cells, stromal cells and infiltrated immune cells. Consequently, CD73 through both enzymatic and none enzymatic functions affect melanoma progression.
Anvar Soleimani +8 more
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CD73 as a potential opportunity for cancer immunotherapy
Expert Opinion on Therapeutic Targets, 2018Cancer cells apply various mechanisms to induce and enhance immune escape. The complex network of immune-response modulating factors in the tumor microenvironment is a reason for the difficulties encountered when attempting to treat many cancers. Adenosine is a potent immune-modulating factor that can be generated through the degradation of ATP by ...
Ghasem Ghalamfarsa +7 more
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CD73 Inhibitors as Antitumor Agents
20235′-Ectonucleotidase (e5NT), a metalloenzyme incorporating two zinc ions in its structure, also known as CD73, hydrolyzes AMP to phosphate and adenosine. It is involved in several physiological and pathological processes, among which immune homeostasis, inflammation, tumor progression. The last decade saw the development of small molecule and monoclonal
Capasso, Clemente +2 more
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T Cell Signalling Through CD73
Cellular Signalling, 1997CD73 (ecto-5'-nucleotidase), a glycosyl phosphatidylinositol (GPI) anchored purine salvage enzyme expressed on the surface of human T and B lymphocytes, catalyzes the conversion of purine and pyrimidine ribo- and deoxyribonucleoside monophosphates to the corresponding nucleosides.
R, Resta, L F, Thompson
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Discovery of AB680: A Potent and Selective Inhibitor of CD73
Journal of Medicinal Chemistry, 2020Extracellular adenosine (ADO), present in high concentrations in the tumor microenvironment (TME), suppresses immune function via inhibition of T cell and NK cell activation. Intratumoral generation of ADO depends on the sequential catabolism of ATP by two ecto-nucleotidases, CD39 (ATP → AMP) and CD73 (AMP → ADO).
Kenneth V. Lawson +25 more
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5′-Ectonucleotidase (e5NT), a metalloenzyme also known as CD73, hydrolyzes AMP to phosphate and adenosine. In mammalians, CD73 is involved in several physiological and pathological processes, among which immune homeostasis, inflammation, and tumor progression.
Supuran C. T., Capasso C.
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Supuran C. T., Capasso C.
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Evaluation of CD73 in lung cancer.
Journal of Clinical Oncology, 2017e14525 Background: Immunotherapy has shown promising results in multiple forms of cancer including lung cancer patients. Treatment targeting alternative immune checkpoints may demonstrate value for specific cancers or in combination therapy with other immunotherapies or chemotherapeutic agents.
Hui Yu +7 more
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Novel CD73 Inhibitors for Treating Cancer
ACS Medicinal Chemistry LettersProvided herein are novel CD73 inhibitors, pharmaceutical compositions, use of such compounds in treating cancer, and processes for preparing such compounds.
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Opportunities and Challenges for anti-CD73 Cancer Therapy
Immunotherapy, 2012Biotherapy Center of the First Affiliated Hospital, Zhengzhou University, Zhengzhou 450052, China and Department of Medicine, Cancer Therapy & Research Center, University of Texas Health Science Center, San Antonio, TX 78229, USA and Robert H Lurie Comprehensive Cancer Center, Department of Medicine – Division of Hematology/Oncology, Northwestern ...
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