Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0027960 (mole)
 21,279 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Out of a series of fourteen 1,2,4-triazolo(4,3-b)-, and 1,2,3,4-tetrazolo-(1,5-b)pyridazine derivatives, 4 compounds have been found to reveal high cytostatic activity in KB and HeLa human cancer cell lines in vitro with ED50 activity values ranging from 0.25 to 3.0 micrograms/cm3 (0.009-0.158 x 10(-4) mole/l), and according to DR and D, NCI, NIH Bethesda criterion were qualified for further in vivo screening investigation. 6-Chloro-8-(N,N-dimethylaminosulfonylmethyl)-1,2,3,4-tetrazolo+ ++-(1,5-b)- pyridazine exhibited the strongest in vitro cytostatic activity (ED50 = 0.009 x 10(-4) mole/l), comparable with the best standards, and higher in comparison with a standard cytosine arabinoside (ED50 = 0.03-0.04 x 10(-4) mole/l). The presence of chlorine atom at C-6 position in the pyridazine ring determines the cytotoxic activity of tetrazolopyridazines as the primary factor and C-8 substituents, which influence their better solubility seems to be a secondary one, as confirmed by the results of the structure-activity and solubility-activity relationship analysis. However, for the exhibition of the triazolopyridazine activities the presence of two chlorine atoms at C-6 and C-3 position was essential.
Pol J Pharmacol
PMID:In vitro cytostatic activity of 1,2,4-triazolo- and 1,2,3,4-tetrazolo pyridazines. 956 51

The title compounds have been synthesized in good yields by the interaction of 2,3,4-pentanetrione-3-oxime with ethanedithioamide in 1:1, 1:2, and 2:2 mole proportions. The structures of these compounds have been elucidated from its physico-chemical and spectral data and by correlation with well-known products. Preliminary screening of these compounds for biological activity against several microorganisms has indicated that they are selective growth inhibitors of Mycobacterium tuberculosis in particular.
Acta Pol Pharm
PMID:Synthesis, structural characterization and antimicrobial studies of 2,4-pentanedione derivatives. Part I. 967 54

Congenital and acquired nevi are common cutaneous malformation occurring in childhood. 315 children were cured in 1990-1995. 62% of nevi did not show any abnormalities of growth pattern and typical appearance. In 119 nevi there were danger signals present, that suggested unusual activity or possible malignant transformation. Changes of pigmentation were present in 36%, enlargement and abnormal texture in 21%, satellite nevi in 11%. Histologically, they were dermal in 28% and epidermodermal in 24%. Only in 3 children melanoma malignum was found, in 2 melanoma juvenile, in 4 dysplastic nevi. All of the children were operated. The very good final result was obtained in 289 children (92%).
Pol Merkur Lekarski 1998 Aug
PMID:[Pigmented nevus in children as a diagnostic and treatment problem]. 1010 59

In 28 Spitz nevi DNA content was determined by video-imaging cytometry. The nevi were selected for this study because of difficulties in differentiation from melanoma and heterogeneity of this type of nevus. Morphological features of Spitz nevi and differences helpful for differentiation between Spitz nevi and malignant melanoma were identified. DNA ploidy was measured in paraffin embedded and fresh tissue material from each patient and the results were comparable. The sample preparation process and video-imaging method are presented in this study. Twenty two (78.6%) lesions contained diploid cell populations, 5 (17.9%) aneuploid and 1 (3.6%) tetraploid cell population. A significant correlation was observed between DNA ploidy measured in fresh tissue and retrospective material. The results indicate the presence of abnormal DNA content in some of the lesions. This observation does not indicate that DNA ploidy cytometry is useful for the differentiation of Spitz nevi from malignant melanoma.
Pol J Pathol 2000
PMID:Significance of DNA ploidy measurements in Spitz nevi. 1083 3

Annexin VI (AnxVI) of molecular mass 68-70 kDa belongs to a multigenic family of ubiquitous Ca2+- and phospholipid-binding proteins. In this report, we describe the GTP-binding properties of porcine liver AnxVI, determined with a fluorescent GTP analogue, 2'-(or 3')-O-(2,4,6-trinitrophenyl)guanosine 5'-triphosphate (TNP-GTP). The optimal binding of TNP-GTP to AnxVI was observed in the presence of Ca2+ and asolectin liposomes, as evidenced by a 5.5-fold increase of TNP-GTP fluorescence and a concomitant blue shift (by 17 nm) of its maximal emission wavelength. Titration of AnxVI with TNP-GTP resulted in the determination of the dissociation constant (Kd) and binding stoichiometry that amounted to 1.3 microM and 1:1 TNP-GTP/AnxVI, mole/mole, respectively. In addition, the intrinsic fluorescence of the membrane-bound form of AnxVI was quenched by TNP-GTP and this was accompanied by fluorescence resonance energy transfer (FRET) from AnxVI Trp residues to TNP-GTP. This indicates that the GTP-binding site within the AnxVI molecule is probably located in the vicinity of a Trp-containing domain of the protein. By controlled proteolysis of human recombinant AnxVI, followed by purification of the proteolytic fragments by affinity chromatography on GTP-agarose, we isolated a 35 kDa fragment corresponding to the N-terminal half of AnxVI containing Trp192. On the basis of these results, we suggest that AnxVI is a GTP-binding protein and the binding of the nucleotide may have a regulatory impact on the interaction of annexin with membranes, e.g. formation of ion channels by the protein.
Acta Biochim Pol 2001
PMID:GTP-binding properties of the membrane-bound form of porcine liver annexin VI. 1199 96

Enterobacter cloacae NAD(P)H:nitroreductase catalyzes the reduction of a series of nitroaromatic compounds with steady-state bimolecular rate constants (kcat/Km) ranging from 10(4) M(-1) s(-1) to 10(7) M(-1) s(-1), and oxidizing 2 moles NADH per mole mononitrocompound. Oxidation of excess NADH by polynitrobenzenes including explosives 2,4,6-trinitrotoluene (TNT) and 2,4,6-trinitrophenyl-N-methylnitramine (tetryl), has been observed as a slower secondary process, accompanied by O2 consumption. This type of 'redox cycling' was not related to reactions of nitroaromatic anion-radicals, but was caused by the autoxidation of relatively stable reaction products. The logs kcat/Km of all the compounds examined exhibited parabolic dependence on their enthalpies of single-electron- or two-electron (hydride) reduction, obtained by quantum mechanical calculations. This type of quantitative structure-activity relationships shows that the reactivity of nitroaromatics towards E. cloacae nitroreductase depends mainly on their hydride accepting properties, but not on their particular structure, and does not exclude the possibility of multistep hydride transfer.
Acta Biochim Pol 2000
PMID:Two-electron reduction of nitroaromatic compounds by Enterobacter cloacae NAD(P)H nitroreductase: description of quantitative structure-activity relationships. 1199 17

Out of a series of twenty 8-substituted or/and 1,N-2-bridged (tricyclic) derivatives of acyclovir (a selective antiherpetic drug), known to be nontoxic to normal cells, seven compounds were found to exhibit moderate cytostatic activity in KB human tumor tissue culture system with ED50 activity values ranging from 0.052-0.094 x 10(-3) mole/l. The structure-activity relationship analysis indicated that the primary factors determining their cytotoxicity were: 1) bromine atom at the C-8 position of the bicyclic derivatives and 2) unsubstituted appended ring in the tricyclic derivatives. Combination of two structural elements carrying the cytotoxicity gave diverse effects, enhancement or decrease in activity depending on particular cases. Two compounds (of four selected), 8-bromoacyclovir and 1,N-2-etheno-acyclovir, having unsubstituted 9-[(2-hydroxyethoxy)methyl] chain, showed approximately 2-fold increase in their cytotoxicity against HeLa tumor cells in the presence of the induced microsomal generating system suggesting that their cytotoxicity depends on the drug metabolic transformation into their active metabolites (intermediates) via MFO-system, and that structural unit of this chain is essential for abovementioned activation. Presently found remarkable cytotoxic selectivity of acyclovir analogues against KB and HeLa tumor cells together with previously reported in the literature specific cytotoxic activity of acyclovir against murine leukemia L 1210 cells seem to be encouraging for further investigation of this class of compounds in other tumor systems.
Pol J Pharmacol
PMID:In vitro cytostatic activity of 8-substituted and tricyclic analogues of acyclovir. 1202 43

Linearly polarized light that illuminates skin is backscattered by superficial layers and rapidly depolarized by birefringent collagen fibers. It is possible to distinguish such superficially backscattered light from the total diffusely reflected light that is dominated by light penetrating deeply into the dermis. The method involves acquisition of two images through an analyzing linear polarizer in front of the camera, one image (I(par)) acquired with the analyzer oriented parallel to the polarization of illumination and one image (I(per)) acquired with the analyzer oriented perpendicular to the illumination. An image based on the polarization ratio, Pol=(I(par)-I(per))/(I(par)+I(per)), is created. This paper compares normal light images, represented by I(per), and Pol images of various skin pathologies in a pilot clinical study using incoherent visible-spectrum light. Images include pigmented skin sites (freckle, tattoo, pigmented nevi) and unpigmented skin sites [nonpigmented intradermal nevus, neurofibroma, actinic keratosis, malignant basal cell carcinoma, squamous cell carcinoma, vascular abnormality (venous lake), burn scar]. Images of a shadow cast from a razor blade onto a forearm skin site illustrate the behavior of Pol values near the shadow edge. Near the shadow edge, Pol approximately doubles in value because no I(per) photons are superficially scattered into the shadow-edge pixels by the shadow region while I(par) photons are directly backscattered from the superficial layer of these pixels. This result suggests that the point spread function in skin for cross-talk between Pol pixels has a half-width-half-max of about 390 microm.
 ...
PMID:Imaging skin pathology with polarized light. 1217 82

Phosphorylated fructose-1,6-bisphosphatase (FBPase) was isolated from rabbit muscle in an SDS/PAGE homogeneous form. Its dephosphorylation with alkaline phosphatase revealed 2.8 moles of inorganic phosphate per mole of FBPase. The phosphorylated FBPase (P-FBPase) differs from the dephosphorylated enzyme in terms of its kinetic properties like K(m) and k(cat), which are two times higher for the phosphorylated FBPase, and in the affinity for aldolase, which is three times lower for the dephosphorylated enzyme. Dephosphorylated FBPase can be a substrate for protein kinase A and the amount of phosphate incorporated per FBPase monomer can reach 2-3 molecules. Since interaction of muscle aldolase with muscle FBPase results in desensitisation of the latter toward AMP inhibition (Rakus & Dzugaj, 2000, Biochem. Biophys. Res. Commun. 275, 611-616), phosphorylation may be considered as a way of muscle FBPase activity regulation.
Acta Biochim Pol 2003
PMID:Rabbit muscle fructose-1,6-bisphosphatase is phosphorylatedin vivo. 1267 51

A chlorocoulometric method for determination of sulfadimethoxine and sulfafurazole in pharmaceutical preparation is proposed. The electrogeneration of chloride is carried out in the supporting electrolyte consisting of 0.5 mole x dm(-3) sulphuric acid and 0.2 mole x dm(-3) sodium chloride. The results obtained show that the method is accurate and reproducible and can be applied for determination of small quantities of sulfafurazole and sulfadimethoxine.
Acta Pol Pharm 1990
PMID:Coulometric determination of sulfadimethoxine and sulfafurazole. 1295 51


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