scholarly journals Adenosine Receptor A2a

2020 ◽  
Author(s):  
Keyword(s):  
Adenosine Receptor ◽  
Adenosine Receptor A2a

scholarly journals Conversion of ATP to adenosine by CD39 and CD73 in multiple myeloma can be successfully targeted together with adenosine receptor A2A blockade

2020 ◽  
Vol 8 (1) ◽  
pp. e000610 ◽  
Author(s):  
Rui Yang ◽  
Samah Elsaadi ◽  
Kristine Misund ◽  
Pegah Abdollahi ◽  
Esten Nymoen Vandsemb ◽  
...  
Keyword(s):  
Multiple Myeloma ◽  
T Cell ◽  
Stromal Cells ◽  
Adenosine Receptor ◽  
Immune Checkpoints ◽  
Incurable Cancer ◽  
Myeloma Cells ◽  
Hematological Cancers ◽  
Adenosine Receptor A2a

BackgroundPD1/PDL1-directed therapies have been unsuccessful for multiple myeloma (MM), an incurable cancer of plasma cells in the bone marrow (BM). Therefore, other immune checkpoints such as extracellular adenosine and its immunosuppressive receptor should be considered. CD39 and CD73 convert extracellular ATP to adenosine, which inhibits T-cell effector functions via the adenosine receptor A2A (A2AR). We set out to investigate whether blocking the adenosine pathway could be a therapy for MM.MethodsExpression of CD39 and CD73 on BM cells from patients and T-cell proliferation were determined by flow cytometry and adenosine production by Liquid chromatograpy-mass spectrometry (HPCL/MS). ENTPD1 (CD39) mRNA expression was determined on myeloma cells from patients enrolled in the publicly available CoMMpass study. Transplantable 5T33MM myeloma cells were used to determine the effect of inhibiting CD39, CD73 and A2AR in mice in vivo.ResultsElevated level of adenosine was found in BM plasma of MM patients. Myeloma cells from patients expressed CD39, and high gene expression indicated reduced survival. CD73 was found on leukocytes and stromal cells in the BM. A CD39 inhibitor, POM-1, and an anti-CD73 antibody inhibited adenosine production and reduced T-cell suppression in vitro in coculture of myeloma and stromal cells. Blocking the adenosine pathway in vivo with a combination of Sodium polyoxotungstate (POM-1), anti-CD73, and the A2AR antagonist AZD4635 activated immune cells, increased interferon gamma production, and reduced the tumor load in a murine model of MM.ConclusionsOur data suggest that the adenosine pathway can be successfully targeted in MM and blocking this pathway could be an alternative to PD1/PDL1 inhibition for MM and other hematological cancers. Inhibitors of the adenosine pathway are available. Some are in clinical trials and they could thus reach MM patients fairly rapidly.

The Discovery and Synthesis of Novel Adenosine Receptor (A2A) Antagonists.

ChemInform ◽  
2005 ◽  
Vol 36 (28) ◽  
Author(s):  
Julius J. Matasi ◽  
John P. Caldwell ◽  
Jinsong Hao ◽  
Bernard Neustadt ◽  
Leyla Arik ◽  
...  
Keyword(s):  
Adenosine Receptor ◽  
Adenosine Receptor A2a

IL-1β and TNF-α Regulation of the Adenosine Receptor (A2A) Expression: Differential Requirement for NF-κB Binding to the Proximal Promoter

2006 ◽  
Vol 177 (10) ◽  
pp. 7173-7183 ◽  
Author(s):  
Silvana Morello ◽  
Kazuhiro Ito ◽  
Satoshi Yamamura ◽  
Kang-Yun Lee ◽  
Elen Jazrawi ◽  
...  
Keyword(s):  
Adenosine Receptor ◽  
Proximal Promoter ◽  
Tnf Α ◽  
Adenosine Receptor A2a

scholarly journals Adenosine Receptor A2a is Differentially Expressed in CD4+ T Lymphocytes of Asthmatic and Healthy Individuals

2008 ◽  
Vol 59 (6) ◽  
pp. 622-622
Author(s):  
P. Holopainen ◽  
C. Karagiannidis ◽  
B. Rückert ◽  
G. Hense ◽  
C. Schmidt-Weber ◽  
...  
Keyword(s):  
T Lymphocytes ◽  
Adenosine Receptor ◽  
Differentially Expressed ◽  
Healthy Individuals ◽  
Adenosine Receptor A2a

Adenosine receptor A2A expression is higher in placentas of women with preeclampsia

2008 ◽  
Vol 68 (S 01) ◽  
Author(s):  
FM von Versen-Höynck ◽  
A Rajakumar ◽  
JM Roberts ◽  
C Bartz ◽  
W Rath ◽  
...  
Keyword(s):  
Adenosine Receptor ◽  
Adenosine Receptor A2a

Role of Adenosine Receptor A2A in Traumatic Optic Neuropathies

2013 ◽  
Author(s):  
Gregory I. Liou ◽  
Saif Ahmad ◽  
Ahmed Elsherbini
Keyword(s):  
Adenosine Receptor ◽  
Adenosine Receptor A2a

Comparative molecular field analysis (CoMFA) of a series of selective adenosine receptor A2A antagonists

1999 ◽  
Vol 46 (2) ◽  
pp. 126-133 ◽  
Author(s):  
Pier Giovanni Baraldi ◽  
Pier Andrea Borea ◽  
Manuela Bergonzoni ◽  
Barbara Cacciari ◽  
Ennio Ongini ◽  
...  
Keyword(s):  
Adenosine Receptor ◽  
Field Analysis ◽  
Molecular Field ◽  
Comparative Molecular Field Analysis ◽  
Molecular Field Analysis ◽  
Adenosine Receptor A2a
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