Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UNIPROT:P20020 (adenosine triphosphatase)
 3,299 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Twenty-two C-3 branched cardenolides were investigated as inhibitors of beef-brain and dog-heart (Na+ + k+) activated adenosine triphosphatase. The synthetic compounds had lower inhibitory strength than digitoxigenin, and there was no indication of an improved safety index. Structure--activity relationships show that increased steric shielding of the 3-OH group results in reduced inhibition.
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PMID:Inhibition of beef-brain and dog-heart (Na+ + k+) activated adenosine triphosphatase by carbon-3 branched cardenolides. 21 61

Nitrated gitoxins (4) and bufotoxin homologues with various lengths of alkyl chain at C-3 of the steroid nucleus (10) were prepared from gitoxin (1). The pharmacological activities of the resulting compounds (4 and 10) were evaluated by measurement of inhibitory effect on NA+, K(+)-adenosine triphosphatase (ATPase) prepared from dog kidney, positive inotropic effect (PIE) on isolated guinea-pig papillary muscle preparations, and the effect on smooth muscle using the mesenteric artery from spontaneously hypertensive rats. Most of the compounds showed a smaller contractile effect on the arterial muscle. Among these compounds, gitoxin 3"-nitrate (4g) exhibited the most desirable biological activities, such as PIE comparable to that of 1, 1.25 times wider concentration-dependent range than 1, and lack of contractile activity on vascular muscle.
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PMID:Studies on cardiac ingredients of plants. XIII: Chemical modification of gitoxin to cardiotonic compounds without vascular effect. 914 99