Physiological control of immune response and inflammatory tissue damage by hypoxia-inducible factors and adenosine A2A receptors

MV Sitkovsky, D Lukashev, S Apasov… - Annu. Rev …, 2004 - annualreviews.org
▪ Abstract Immune cell–mediated destruction of pathogens may result in excessive collateral
damage to normal tissues, and the failure to control activated immune cells may cause …

The A3 adenosine receptor: history and perspectives

PA Borea, K Varani, F Vincenzi, PG Baraldi… - Pharmacological …, 2015 - ASPET
By general consensus, the omnipresent purine nucleoside adenosine is considered a major
regulator of local tissue function, especially when energy supply fails to meet cellular energy …

Medicinal chemistry and the molecular operating environment (MOE): application of QSAR and molecular docking to drug discovery

S Vilar, G Cozza, S Moro - Current topics in medicinal chemistry, 2008 - ingentaconnect.com
The search for new compounds with a given biological activity requires enormous effort in
terms of manpower and cost. This effort arises from the large number of compounds that …

A3 Adenosine Receptors as Modulators of Inflammation: From Medicinal Chemistry to Therapy

KA Jacobson, S Merighi, K Varani… - Medicinal research …, 2018 - Wiley Online Library
The A3 adenosine receptor (A3AR) subtype is a novel, promising therapeutic target for
inflammatory diseases, such as rheumatoid arthritis (RA) and psoriasis, as well as liver …

Adenosine receptor antagonists: translating medicinal chemistry and pharmacology into clinical utility

PG Baraldi, MA Tabrizi, S Gessi, PA Borea - Chemical reviews, 2008 - ACS Publications
The purine nucleoside adenosine is consensually identified as a major local regulator of
tissue function especially when energy supply fails to meet cellular energy demand. Due to …

Caffeine inhibits adenosine-induced accumulation of hypoxia-inducible factor-1α, vascular endothelial growth factor, and interleukin-8 expression in hypoxic human …

S Merighi, A Benini, P Mirandola, S Gessi, K Varani… - Molecular …, 2007 - ASPET
Frequent coffee consumption has been associated with a reduced risk of colorectal cancer
in a number of case-control studies. Coffee is a leading source of methylxanthines, such as …

Progress in the pursuit of therapeutic adenosine receptor antagonists

S Moro, ZG Gao, KA Jacobson… - Medicinal research …, 2006 - Wiley Online Library
Ever since the discovery of the hypotensive and bradycardiac effects of adenosine,
adenosine receptors continue to represent promising drug targets. First, this is due to the fact …

Structure–activity relationships of thiazole and thiadiazole derivatives as potent and selective human adenosine A3 receptor antagonists

KY Jung, SK Kim, ZG Gao, AS Gross, N Melman… - Bioorganic & medicinal …, 2004 - Elsevier
4-(4-Methoxyphenyl)-2-aminothiazole and 3-(4-methoxyphenyl)-5-aminothiadiazole
derivatives have been synthesized and evaluated as selective antagonists for human …

Use of the A2A adenosine receptor as a physiological immunosuppressor and to engineer inflammation in vivo

MV Sitkovsky - Biochemical pharmacology, 2003 - Elsevier
Inflammation must be inhibited in order to treat, eg, sepsis or autoimmune diseases or must
be selectively enhanced to improve, for example, immunotherapies of tumors or the …

Synthesis of functionalized tetrasubstituted pyrazolyl heterocycles–a review

S Dadiboyena, A Nefzi - European journal of medicinal chemistry, 2011 - Elsevier
Heterocyclic chemistry constitutes an essential branch of organic chemistry and
heterocycles are widely known to display an array of biological properties. Pyrazoles …