Design and synthesis of adenosine receptor antagonist bioconjugates as anti-tumor immunotherapies

Istradefylline (KW-6002) is one of many xanthines that act as antagonists of the A2A adenosine receptor (A2AR). While this molecule has recently been involved in phase III clinical trials as a target therapeutic for Parkinson's disease, its target pathway also implicated in tumorigenesis. As wa...

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Online Access:http://hdl.handle.net/2047/D20001031
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spelling ndltd-NEU--neu-7762021-05-26T05:10:40ZDesign and synthesis of adenosine receptor antagonist bioconjugates as anti-tumor immunotherapiesIstradefylline (KW-6002) is one of many xanthines that act as antagonists of the A2A adenosine receptor (A2AR). While this molecule has recently been involved in phase III clinical trials as a target therapeutic for Parkinson's disease, its target pathway also implicated in tumorigenesis. As was described by Ohta et al, the oxygen-deprived hypoxic tumor microenvironment fosters increased production of adenosine, which up-regulates formation of cAMP following binding to the A2A receptor. Increased intracellular levels of cAMP are responsible for immunosuppression and misguided protection of cancerous cells. KW-6002 has shown efficacy in rescuing T-cell regulatory function in models of adoptive transfer immunotherapy.http://hdl.handle.net/2047/D20001031
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sources NDLTD
description Istradefylline (KW-6002) is one of many xanthines that act as antagonists of the A2A adenosine receptor (A2AR). While this molecule has recently been involved in phase III clinical trials as a target therapeutic for Parkinson's disease, its target pathway also implicated in tumorigenesis. As was described by Ohta et al, the oxygen-deprived hypoxic tumor microenvironment fosters increased production of adenosine, which up-regulates formation of cAMP following binding to the A2A receptor. Increased intracellular levels of cAMP are responsible for immunosuppression and misguided protection of cancerous cells. KW-6002 has shown efficacy in rescuing T-cell regulatory function in models of adoptive transfer immunotherapy.
title Design and synthesis of adenosine receptor antagonist bioconjugates as anti-tumor immunotherapies
spellingShingle Design and synthesis of adenosine receptor antagonist bioconjugates as anti-tumor immunotherapies
title_short Design and synthesis of adenosine receptor antagonist bioconjugates as anti-tumor immunotherapies
title_full Design and synthesis of adenosine receptor antagonist bioconjugates as anti-tumor immunotherapies
title_fullStr Design and synthesis of adenosine receptor antagonist bioconjugates as anti-tumor immunotherapies
title_full_unstemmed Design and synthesis of adenosine receptor antagonist bioconjugates as anti-tumor immunotherapies
title_sort design and synthesis of adenosine receptor antagonist bioconjugates as anti-tumor immunotherapies
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url http://hdl.handle.net/2047/D20001031
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