Theophylline, also known as 1,3-dimethylxanthine, is a phosphodiesterase inhibiting drug used in therapy for respiratory diseases such as chronic obstructive pulmonary disease (COPD) and asthma under a variety of brand names. As a member of the xanthine family, it bears structural and pharmacological similarity to theobromine and caffeine, and is readily found in nature, being present in tea (Camellia sinensis) and cocoa (Theobroma cacao). A small amount of theophylline is one of the products of caffeine metabolic processing in the liver. Theophylline was first extracted from tea leaves and chemically identified around 1888 by the German biologist Albrecht Kossel. Seven years later, a chemical synthesis starting with 1,3-dimethyluric acid was described by Emil Fischer and Lorenz Ach. Like other methylated xanthine derivatives, theophylline is both a competitive nonselective phosphodiesterase inhibitor, which raises intracellular cAMP, activates PKA, inhibits TNF-alpha and inhibits leukotriene synthesis, and reduces inflammation and innate immunity. It is also a nonselective adenosine receptor antagonist, antagonizing A1, A2, and A3 receptors almost equally, which explains many of its cardiac effects. Here you can see a theophyline molecule in complex with an specific RNA aptamer, as determined by X-ray crystallography (PDB code: 8D28)
#molecularart ... #immolecular ... #theophyline ... #aptamer ... #complex ... #xray
Structure rendered with @proteinimaging and depicted with @corelphotopaint
#molecularart ... #immolecular ... #theophyline ... #aptamer ... #complex ... #xray
Structure rendered with @proteinimaging and depicted with @corelphotopaint
