Soluble cyanobacterial granule polypeptide (CGP), especially that isolated from recombinant Escherichia coli strains, consists of aspartic acid, arginine, and a greater amount of lysine than that in insoluble CGP isolated from cyanobacteria or various other recombinant bacteria. In vitro guanidination of lysine side chains of soluble CGP with o-methylisourea (OMIU) yielded the nonproteinogenic ...

Mitochondrial calcium (Ca(2+)) dyshomeostasis constitutes a critical step in the metabolic crossroads leading to cell death. Therefore, we have studied here whether 7-chloro-5-(2-chlorophenyl)-1,5-dihydro-4,1-benzothiazepin-2(3H)-one (CGP37157; CGP), a blocker of the mitochondrial Na(+)/Ca(2+)-exchanger (mNCX), protects against veratridine-elicited chromaffin cell death, a model suitable to stu...

The pharmacological profile of the gamma-aminobutyric acid (GABA)(B) receptor regulating cholinergic twitch contraction in the guinea pig ileum myenteric plexus-longitudinal muscle preparation was investigated. GABA and (-)-baclofen inhibited the contraction, exhibiting quite close potencies (pD(2) for GABA = 5.70; pD(2) for (-)-baclofen = 5.33). The compound CGP 47656 also reduced the choliner...

The antitumor efficacy and the hormonal effects of the thiazolidine-dione derivative (sodium methyl((-3-methyl-2- ([5-methyl-3-(2-methylallyl)-4-oxo-2 thiazolidinyliden]hydrazono)-4-oxo-5-thiazolidinyl)) phosphate, CGP 19984, have been studied in in vivo rat prostatic and mammary cancer models. CGP 19984 significantly inhibited growth of the androgen-dependent Dunning R3327 rat prostate adenoca...

Embedded Cartesian Genetic Programming (ECGP) is an extension of Cartesian Genetic Programming (CGP) capable of acquiring, evolving and re-using partial solutions. In this paper, we apply for the first time CGP and ECGP to the ones-max and order-3 deceptive problems, which are normally associated with Genetic Algorithms. Our approach uses CGP and ECGP to evolve a sequence of commands for a tape...

The rate of insulin secretion from isolated rat islets of Langerhans was affected by a number of dihydropyridine derivatives known to interact with voltage-sensitive Ca2+ channels in excitable cells. The channel antagonists nifedipine and nitrendipine were potent inhibitors of glucose-induced insulin secretion in response to both 8 mM- and 20 mM-glucose, although they did not lower the basal se...

We examined the effects of SEA0400 and CGP-37157 on the plasmalemmal Na(+)-Ca(2+) exchanger (NCX) and mitochondrial NCX using H9c2 cardiomyocytes loaded with Ca(2+)-sensitive fluorescent probes. The plasmalemmal NCX activity, which was measured as the increase in cytoplasmic Ca(2+) concentration after application of low Na(+) extracellular solution, was inhibited by SEA0400 but not by CGP-37157...

OBJECTIVE The effects of the beta-3-receptor agonist CGP-12177 on thyroxine (T4) deiodination in sympathectomized (SX) interscapular brown adipose tissue (BAT) were assessed in 300 g body weight (BW) Wistar rats. DESIGN Seven days after SX, groups of rats were implanted s.c. with pellets containing 5mg CGP-12177 or 5mg norepinephrine (NE) and were immediately placed at 4 degrees C for 24h. Ot...

Blackshaw, L. Ashley, Esther Staunton, Anders Lehmann, and John Dent. Inhibition of transient LES relaxations and reflux in ferrets by GABA receptor agonists. Am. J. Physiol. 277 (Gastrointest. Liver Physiol. 40): G867– G874, 1999.—Transient lower esophageal sphincter (LES) relaxation is the major mechanism of gastroesophageal reflux. This study uses an established ferret model to evaluate GABA...

Transient lower esophageal sphincter (LES) relaxation is the major mechanism of gastroesophageal reflux. This study uses an established ferret model to evaluate GABAB receptor agonists' ability to reduce triggering of transient LES relaxations. One hundred sixty manometric/pH studies were performed on 18 conscious ferrets. In untreated animals, intragastric infusion of 25 ml glucose (pH 3.5) le...