Sustained compensatory p38 MAPK signaling following treatment with MAPK inhibitors induces the immunosuppressive protein CD73 in cancer: combined targeting could improve outcomes.
Sign Up to like & getrecommendations! Published in 2021 at "Molecular oncology"
DOI: 10.1002/1878-0261.13046
Abstract: RAS-MAPK signaling promotes immune evasion and cancer cell survival, and MAPK inhibitors (MAPKi) are frequently used as cancer therapies. Despite progress elucidating the direct effects of MAPKi on immune cells, their indirect effect on the… read more here.
Keywords: treatment; mapki; cd73; mapk signaling ... See more keywords
Specific blockade CD73 alters the 'exhausted' phenotype of T cells in head and neck squamous cell carcinoma.
Sign Up to like & getrecommendations! Published in 2018 at "International journal of cancer"
DOI: 10.1002/ijc.31426
Abstract: The adenosine-induced immunosuppression hampers the immune response toward tumor cells and facilitates the tumor cells to evade immunosurveillance. CD73, an ecto-5-nucleotidase, is the ectoenzyme dephosphorylating extracellular AMP to adenosine. Here, using immunocompetent transgenic head and… read more here.
Keywords: neck squamous; cell carcinoma; squamous cell; exhausted phenotype ... See more keywords
Specific blockade CD73 alters the “exhausted” phenotype of T cells in head and neck squamous cell carcinoma
Sign Up to like & getrecommendations! Published in 2018 at "International Journal of Cancer"
DOI: 10.1002/ijc.31534
Abstract: The adenosine‐induced immunosuppression hampers the immune response toward tumor cells and facilitates the tumor cells to evade immunosurveillance. CD73, an ecto‐5‐nucleotidase, is the ectoenzyme dephosphorylating extracellular AMP to adenosine. Here, using immunocompetent transgenic head and… read more here.
Keywords: neck squamous; cell carcinoma; squamous cell; exhausted phenotype ... See more keywords
CD73 Downregulation Decreases In Vitro and In Vivo Glioblastoma Growth
Sign Up to like & getrecommendations! Published in 2018 at "Molecular Neurobiology"
DOI: 10.1007/s12035-018-1240-4
Abstract: AbstractGlioblastoma is the worst and most common primary brain tumor. Here, we demonstrated the role of CD73, an enzyme responsible for adenosine (ADO) production, in glioblastoma progression. ADO increased glioma cell viability via A1 receptor… read more here.
Keywords: ado; glioma; glioblastoma; cd73 downregulation ... See more keywords
The therapeutic potential of targeting CD73 and CD73-derived adenosine in melanoma.
Sign Up to like & getrecommendations! Published in 2020 at "Biochimie"
DOI: 10.1016/j.biochi.2020.06.001
Abstract: The 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… read more here.
Keywords: melanoma; cd73 derived; cd73; derived adenosine ... See more keywords
Orally Bioavailable Small Molecule CD73 Inhibitor (OP-5244) Reverses Immunosuppression Through Blockade of Adenosine Production.
Sign Up to like & getrecommendations! Published in 2020 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.0c01086
Abstract: The adenosinergic pathway represents an attractive new therapeutic approach in cancer immunotherapy. In this pathway, ecto-5-nucleotidase CD73 has the unique function of regulating production of immunosuppressive adenosine (ADO) through the hydrolysis of AMP. CD73 is… read more here.
Keywords: orally bioavailable; production; cd73 inhibitor; small molecule ... See more keywords
Discovery of Small and Bifunctional Molecules Targeting PD-L1/CD73 for Cancer Dual Immunotherapy.
Sign Up to like & getrecommendations! Published in 2024 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.4c00553
Abstract: In this work, a series of bifunctional PD-L1/CD73 (cluster of differentiation 73) small-molecule inhibitors were designed and synthesized. Among them, CC-5 showed the strongest PD-L1 inhibitory effects with an IC50 of 6 nM and potent… read more here.
Keywords: cd73; discovery small; small bifunctional; bifunctional molecules ... See more keywords
Discovery of ORIC-533, an Orally Bioavailable CD73 Inhibitor That Maintains Activity in High AMP Environments to Reverse Tumor Immunosuppression.
Sign Up to like & getrecommendations! Published in 2025 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.5c02153
Abstract: Immunosuppressive adenosine (ADO) is catabolized from adenosine monophosphate (AMP) by CD73 in the tumor microenvironment and corresponds to poor patient prognosis in many cancers. Reducing levels of ADO via inhibition of CD73 may reverse this… read more here.
Keywords: cd73; amp; tumor; inhibitor ... See more keywords
Increased Synaptic ATP Release and CD73-Mediated Formation of Extracellular Adenosine in the Control of Behavioral and Electrophysiological Modifications Caused by Chronic Stress
Sign Up to like & getrecommendations! Published in 2023 at "ACS Chemical Neuroscience"
DOI: 10.1021/acschemneuro.2c00810
Abstract: Increased ATP release and its extracellular catabolism through CD73 (ecto-5′-nucleotidase) lead to the overactivation of adenosine A2A receptors (A2AR), which occurs in different brain disorders. A2AR blockade blunts mood and memory dysfunction caused by repeated… read more here.
Keywords: cd73 mediated; cd73; stress; release ... See more keywords
A novel small molecule inhibitor of CD73 triggers immune-mediated multiple myeloma cell death
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DOI: 10.1038/s41408-024-01019-5
Abstract: CD73 is the key ectoenzyme involved in the generation of AMP-derived adenosine, which contributes to immunosuppression in the MM BM milieu. Blocking CD73 activity with a potent, selective, orally bioavailable CD73 inhibitor ORIC-533 decreases adenosine… read more here.
Keywords: cd73; generation; novel small; cell ... See more keywords
CD73 facilitates EMT progression and promotes lung metastases in triple-negative breast cancer
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DOI: 10.1038/s41598-021-85379-z
Abstract: CD73 is a cell surface ecto-5′-nucleotidase, which converts extracellular adenosine monophosphate to adenosine. High tumor CD73 expression is associated with poor outcome among triple-negative breast cancer (TNBC) patients. Here we investigated the mechanisms by which… read more here.
Keywords: negative breast; breast cancer; cd73; cancer ... See more keywords