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1.
Silvia Pastorekova Daniela Vullo Angela Casini Andrea Scozzafava Jaromir Pastorek Isao Nishimori 《Journal of enzyme inhibition and medicinal chemistry》2013,28(3):211-217
The tumor-associated transmembrane carbonic anhydrase (CA, EC 4.2.1.1) isozymes IX (CA IX) and XII (CA XII) are involved in acidification of hypoxic tumors, a process correlated with poor prognosis and clinical outcome of patients harboring such tumors. This process may be reversed by inhibiting these enzymes with potent sulfonamide/sulfamate inhibitors. A series of such aromatic/heterocyclic sulfonamides incorporating 2,3,5,6-tetrafluorobenzoyl-, 2,3,5,6-tetrafluoro- phenylsulfonyl- and pentafluorophenylureido moieties has been investigated for its interaction with the catalytic domain of the human isozymes hCA IX and hCA XII. Some of these compounds showed excellent inhibitory properties against both isozymes IX and XII, with several subnanomolar inhibitors detected for the first time. These sulfonamides may constitute valuable candidates for the development of novel antitumor therapies based on the inhibition of such tumor-associated CA isozymes. 相似文献
2.
Jaromir Konecny Michael Eckert Michael Schöniger G. Ludwig Hofacker 《Journal of molecular evolution》1993,36(5):407-416
Summary We lay new foundations to the hypothesis that the genetic code is adapted to evolutionary retention of information in the
antisense strands of natural DNA/RNA sequences. In particular, we show that the genetic code exhibits, beyond the neutral
replacement patterns of amino acid substitutions, optimal properties by favoring simultaneous evolution of proteins encoded
in DNA/RNA sense-antisense strands. This is borne out in the sense-antisense transformations of the codons of every amino
acid which target amino acids physicochemically similar to each other. Moreover, silent mutations in the sense strand generate
conservative ones in its antisense counterpart and vice versa. Coevolution of proteins coded by complementary strands is shown
to be a definite possibility, a result which does not depend on any physical interaction between the coevolving proteins.
Likewise, the degree to which the present genetic code is dedicated to evolutionary sense-antisense tolerance is demonstrated
by comparison with many randomized codes. Double-strand coding is quantified from an information-theoretical point of view. 相似文献
3.
Jan Benes Hana Tomankova Martina Novakova Zdeněk Rohan Richard Kvetnansky Jaromir Myslivecek 《Cellular and molecular neurobiology》2013,33(4):503-511
Glucocorticoids act via glucocorticoid receptors (GR), typically localized in the cytosol (cGR). Rapid action is probably mediated via membrane receptors (mGR). In corticotropin-releasing hormone knockouts (CRH-KO), basal plasma glucocorticoid levels do differ from wild type levels (WT), but are approximately ten times lower during exposure to immobilization stress (IMMO) in comparison to WT. We tested the following hypotheses: (1) the mice lung tissue GR basal numbers would not be changed in CRH-KO (because of similar glucocorticoid levels), (2) the number of GR would be changed in WT but not in KO during short (30, 90, and 120 min) IMMO (because of higher increase of glucocorticoid levels in WT). The basal levels of cGR were not changed in CRH-KO (compared to WT), while mGR were significantly lower (62 %) in CRH-KO. In WT, there was the only decrease (to 32 %) in cGR after 120 min when we also found an increase in mGR in WT (to 201 %). In CRH-KO, IMMO caused gradual decrease in cGR (to 52 % after 30 min, to 46 % after 90 min, and to 32 % after 120 min). In CRH-KO, the only increase in mGR appeared already at 30 min of IMMO. These data suggest, on the contrary to our hypotheses, that CRH-KO are more susceptible to GR changes in early phases of stress. 相似文献
4.
Jiří Macháček Ivana Vaníčková Jaromir Seda Mathilde Cordellier Klaus Schwenk 《Hydrobiologia》2013,715(1):113-123
Long-term persistence of a Daphnia population is allowed by the production of dormant stages, produced mostly through sexual reproduction. We investigated the spatio-temporal dynamics of male production in a spring population of Daphnia galeata in the reservoir, and compared the genetic structure of three groups within this population: male-, female-producing females, and adult males. With a fine resolution sampling design and the use of highly variable microsatellite markers we revealed that: (1) the spring period of male offspring production was delimited in time with minimum interannual variation to about 3 weeks, and in space to the upper 5-m water layer; (2) there were no remarkable changes in the clonal composition of male-producing females within the period of male production; (3) overall certain clones exhibited a higher tendency to produce male offspring and therefore the clonal structure of male-producing lineages was significantly different from that of female-producing lineages; and (4) the clonal structure of male-producing females was not significantly different from that of adult males occurring later in the reservoir. This suggests that males were not subjected to any significant selective forces till maturity and the male-producing females confer a long-term fitness advantage over female-producing females. 相似文献
5.
Satoshi Fujita Jaromir Pytela Takashi Hotta Takehide Kato Takahiro Hamada Rie Akamatsu Yasumasa Ishida Natsumaro Kutsuna Seiichiro Hasezawa Yuko Nomura Hirofumi Nakagami Takashi Hashimoto 《Current biology : CB》2013,23(20):1969-1978
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6.
Franchi M Vullo D Gallori E Pastorek J Russo A Scozzafava A Pastorekova S Supuran CT 《Journal of enzyme inhibition and medicinal chemistry》2003,18(4):333-338
A series of new compounds was obtained by reaction of aromatic/heterocyclic sulfonamides incorporating amino groups with N,N-diphenylcarbamoyl chloride and diphenylacetyl chloride. These sulfonamides were assayed for the inhibition of three carbonic anhydrase (CA, EC 4.2.1.1) isozymes: the cytosolic CA I and CA II, and the transmembrane, cancer-associated isozyme CA IX. Good inhibitors against all these isoforms were detected, and the inhibition profile of the newly investigated isozyme IX was observed to be different from that of the cytosolic isozymes, I and II. This may lead to the development of novel anticancer therapies based on the selective inhibition of CA IX. 相似文献
7.
Expression of transmembrane carbonic anhydrase isoenzymes IX and XII in normal human pancreas and pancreatic tumours 总被引:1,自引:1,他引:0
Kivelä AJ Parkkila S Saarnio J Karttunen TJ Kivelä J Parkkila AK Pastoreková S Pastorek J Waheed A Sly WS Rajaniemi H 《Histochemistry and cell biology》2000,114(3):197-204
Carbonic anhydrase (CA) IX and XII are transmembrane isoenzymes which are expressed in several epithelia and overexpressed in some carcinomas. They have recently been linked to von Hippel-Lindau gene-mediated carcinogenesis in that both isoenzymes are downregulated by the product of the wild-type von Hippel-Lindau tumour suppressor gene. This paper describes the localisation of CA IX and XII in the normal human pancreas and pancreatic tumours. Both isoenzymes showed positive reaction in the basolateral plasma membrane of the normal acinar and ductal epithelia. The hyperplastic ductal epithelium in tumour specimens generally showed an increased staining for CA IX. Of 29 malignant tumours of exocrine pancreas, 10 showed moderate or strong immunoreaction for CA IX. The signal for CA XII remained weak in most malignant lesions. The present results show that both CA IX and XII are unevenly expressed in the ductal and acinar compartments of the human pancreas. The expression of these isoenzymes in a relatively low number of malignant tumour specimens suggests that they have a limited value in diagnostic evaluation of pancreatic carcinoma. However, the increased expression of CA IX in hyperplastic ductal epithelium may contribute to the pancreatic tumourigenesis. 相似文献
8.
Seda Jaromir; Petrusek Adam; Machacek Jiri; Smilauer Petr 《Journal of plankton research》2007,29(7):619-628
Canyon-shaped reservoirs are often characterised by longitudinalgradients of environmental factors (including trophic level,phytoplankton and zooplankton biomass and abundance of planktivorousfish) affecting the taxonomic composition of the pelagic community.We tested the hypothesis that the spatial distribution of differentspecies and interspecific hybrids of the Daphnia longispinaspecies complex is non-random under such conditions. Duringthe summer stratification, we sampled crustacean zooplanktonfrom 11 reservoirs, covering both longitudinal (upstream, middle,dam) and vertical (epi-, meta- and hypolimnion) environmentalgradients. Allozyme electrophoresis was used to discriminateamong different Daphnia taxa. All three frequently hybridizingEuropean species of the complex (galeata, cucullata, longispina= hyalina) and hybrids with Daphnia galeata were commonly recorded.Smaller-bodied Daphnia cucullata and its hybrids, when present,preferred mostly the nutrient- and food-rich upstream regions;D. longispina and its hybrids were more commonly found in thedownstream part, and often dominated in the meta- or hypolimnion.Redundancy analyses confirmed significant differences in theDaphnia taxon composition, as well as in spatial distributionof other crustacean species, along both gradients. For the firsttime, we demonstrate regular patterns in the horizontal distributionof Daphnia species and hybrids within a water body, thus acceptingour hypothesis. Such spatial distributional patterns may stronglyimpact local hybridization processes. 相似文献
9.
<Emphasis Type="Italic">Daphnia galeata</Emphasis> in the deep hypolimnion: spatial differentiation of a “typical epilimnetic” species 总被引:2,自引:1,他引:1
One of the most serious threats to tropical mangrove ecosystems caused by shrimp farming activities is the poor management
of pond waste materials. We hypothesise that mangroves can tolerate chemical residues discharged from shrimp farms and can
be used as biofilters, but the capability of mangroves to cope with solid sediments dredged from shrimp ponds is limited.
Our study in Pak Phanang, Thailand, confirmed that the excess sediments discharged from nearby shrimp ponds reduced mangrove
growth rates and increased mortality rates. A series of transformed multi-temporal satellite images was used in combination
with the field data to support this claim. In addition, a comparison between four dominant mangrove species revealed that
Avicennia marina could tolerate sedimentation rates of >6 cm year−1, while Bruguiera cylindrica tolerated sedimentation rates of 5 cm year−1 (total sediment depth = 25 cm) before dying, while Excoecaria agallocha and Lumnitzera racemosa performed intermediate. This outcome implied that in our situation A. marina and to lesser extent E. agallocha and L. racemosa could be more effective as biofilters than B. cylindrica, as they may survive the sedimentation longer in the disposal areas. Further studies on the impact of sedimentation and chemical
pollution of shrimp farm wastes on mangrove mortality and growth are required. 相似文献
10.