Ethylmethylglyoxal bis(guanylhydrazone) (EMGBG) sulfate, an analog of the well-known antileukemic drug methylglyoxal bis(guanylhydrazone), was synthesized. It was shown to be an extremely powerful competitive inhibitor of eukaryotic S-adenosyimethionine decarboxylase, with an apparent Ki value 12 nᴍ. Thus, it appears to be the most powerful known i...
The cytocidal action of Naja naja kaouthia venom on rabbit red blood cells and S-180 tumor cells treated with local anesthetics (tetracaine, lidocaine and procaine) were studied. The S-180 cells were more sensitive to the venom than the red blood cells which required albumin for efficient hemolysis in the 10 minute assay. All three local anesthetic...
abstractThe effects of somatostatin (SS-14 and/or SS-28) and of the three octapeptide SS-analogs that are available for clinical use (octreotide, BIM-23014 and RC-160) on hormone release by primary cultures of 15 clinically nonfunctioning pituitary adenomas (NFA), 7 prolactinomas, and 2 insulinomas were investigated. In the pituitary adenoma cultur...
abstractTibolone, a synthetic steroid acting in a tissue-specific manner and used in hormone replacement therapy, is converted into three active metabolites: a Delta(4) isomer (exerting progestogenic and androgenic effects) and two hydroxy metabolites, 3 alpha-hydroxytibolone (3 alpha-OH-tibolone) and 3beta-OH-tibolone (exerting estrogenic effects)...
abstractStem cell factor (SCF) has an important role in the proliferation, differentiation, survival, and migration of hematopoietic cells. SCF exerts its effects by binding to cKit, a receptor with intrinsic tyrosine kinase activity. Activation of phosphatidylinositol 3'-kinase (PI3-K) by cKit was previously shown to contribute to many SCF-induced...
