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71.
72.
NÓRA BREZA JÁNOS PATÓ LÁSZLÓ ŐRFI BÁLINT HEGYMEGI-BARAKONYI PÉTER BÁNHEGYI EDIT VÁRKONDI 《Journal of receptor and signal transduction research》2013,33(4):361-373
The development of selective protein kinase inhibitors has become an important area of drug discovery for the treatment of different diseases. We report the synthesis and characterization of a series of novel quinazoline derivatives against three therapeutically important and pharmacologically related kinases: 1) epidermal growth factor receptor (EGFR; wild type and mutant) in the field of cancer, 2) receptor-interacting caspase-like apoptosis-regulatory kinase (RICK) in the field of inflammation, and 3) pUL97 of human cytomegalovirus (HCMV). For reference purpose we have synthesized the four clinically relevant quinazolines, including the lead compounds, which we previously identified for RICK and pUL97. A total of 52 quinazoline derivatives were synthesized and tested on the basis of these leads to specifically target the hydrophobic pocket of the ATP-binding site. Selected compounds were tested on wild-type and mutant forms of EGFR, RICK, and pUL97 kinases; their logP and logS values for assessing suitability as drugs were calculated and hit or lead compounds identified. 相似文献
73.
74.
SEBASTIÁN APESTEGUÍA RAÚL O. GÓMEZ GUILLERMO W. ROUGIER 《Zoological Journal of the Linnean Society》2012,166(2):342-360
Herein we describe a new rhynchocephalian taxon from the Middle Jurassic of Patagonia, Argentina, representing the first Jurassic record of the group in South America. The new taxon, consisting of a complete dentary, is ascribed to Sphenodontia based on the presence of a deep and wide Meckelian groove, long posterior process, well‐developed coronoid process, and acrodont teeth showing dental regionalization including successional, alternate hatchling, and additional series. This allocation is reinforced by a phylogenetic analysis that places the new taxon in a basal position within a clade of sphenodontians that excludes Diphydontosaurus and Planocephalosaurus. Additionally, the new taxon clusters within a Gondwanan clade with the Indian Godavarisaurus from the Jurassic Kota Formation, sharing the presence of recurved and relatively large posterior successional teeth that are ribbed and bear a peculiar anterolingual groove. This sister‐group relationship is intriguing from a palaeobiogeographical viewpoint, as it suggests some degree of endemism during the initial stages of the breakup of Pangaea. We also discuss the ontogenetic stage of the new taxon and provide insights on the evolution of successional dentition in rhynchocephalians. © 2012 The Linnean Society of London, Zoological Journal of the Linnean Society, 2012, 166 , 342–360. 相似文献
75.
76.
Background
Ran GTPase has multiple functions during the cell division cycle, including nucleocytoplasmic transport, mitotic spindle assembly and nuclear envelope formation. The activity of Ran is determined by both its guanine nucleotide-bound state and its subcellular localization. 相似文献77.
Randa A Abusham RA Noor Zaliha Raja Rahman Abu Bakar Salleh Mahiran Basri 《Microbial cell factories》2009,8(1):20-9
Background
Many researchers have reported on the optimization of protease production; nevertheless, only a few have reported on the optimization of the production of organic solvent-tolerant proteases. Ironically, none has reported on thermostable organic solvent-tolerant protease to date. The aim of this study was to isolate the thermostable organic solvent-tolerant protease and identify the culture conditions which support its production. The bacteria of genus Bacillus are active producers of extra-cellular proteases, and the thermostability of enzyme production by Bacillus species has been well-studied by a number of researchers. In the present study, the Bacillus subtilis strain Rand was isolated from the contaminated soil found in Port Dickson, Malaysia. 相似文献78.
The phylogenetic origin of the bifunctional tyrosine-pathway protein in the enteric lineage of bacteria 总被引:5,自引:0,他引:5
Because bifunctional enzymes are distinctive and highly conserved products
of relatively infrequent gene-fusion events, they are particularly useful
markers to identify clusters of organisms at different hierarchical levels
of a phylogenetic tree. Within the subdivision of gram-negative bacteria
known as superfamily B, there are two distinctive types of tyrosine-pathway
dehydrogenases: (1) a broad- specificity dehydrogenase (recently termed
cyclohexadienyl dehydrogenase [CDH]) that can utilize either prephenate or
L-arogenate as alternative substrates and (2) a bifunctional CDH that also
posseses chorismate mutase activity. (T-proteins). The bifunctional
T-protein, thought to be encoded by fused ancestral genes for chorismate
mutase and CDH, was found to be present in enteric bacteria (Escherichia,
Shigella, Salmonella, Citrobacter, Klebsiella, Erwinia, Serratia,
Morganella, Cedecea, Kluyvera, Hafnia, Edwardsiella, Yersinia, and Proteus)
and in Aeromonas and Alteromonas. Outside of the latter "enteric lineage,"
the T-protein is absent in other major superfamily-B genera, such as
Pseudomonas (rRNA homology group I), Xanthomonas, Acinetobacter, and
Oceanospirillum. Hence, the T-protein must have evolved after the
divergence of the enteric and Oceanospirillum lineages.
3-Deoxy-D-arabino-heptulosonate 7-phosphate synthase-phe, an early-pathway
isozyme sensitive to feedback inhibition by L- phenylalanine, has been
found in each member of the enteric lineage examined. The absence of both
the T-protein and DAHP synthase-phe elsewhere in superfamily B indicates
the emergence of these character states at approximately the same
evolutionary time.
相似文献
79.
Molecular phylogenetics of Stenodermatini bat genera: congruence of data from nuclear and mitochondrial DNA 总被引:2,自引:1,他引:1
Van den Bussche RA; Baker RJ; Wichman HA; Hamilton MJ 《Molecular biology and evolution》1993,10(5):944-959
Within the tribe Stenodermatini the systematics of the complex of species
allied with the genus Artibeus has generated several alternative
phylogenetic hypotheses. The most recent treatment recognized four genera
(Artibeus, Dermanura, Enchisthenes, and Koopmania) and suggested that the
most recent common ancestor of these four genera would include the common
ancestor of all other currently recognized Stenodermatini genera except
Sturnira. To test this hypothesis, we examined an EcoRI-defined nuclear
satellite DNA repeat and 402 bp of DNA sequence variation from the
mitochondrial cytochrome b gene. Phylogenetic conclusions based on Southern
blot analyses, in situ hybridization, and mitochondrial DNA sequence data
indicate that Enchisthenes is not closely related to Dermanura, Artibeus,
or Koopmania and that Dermanura, Artibeus, and Koopmania shared a common
ancestor after diverging from the remainder of the Stenodermatini. If our
conclusions are correct, then justification for recognizing Dermanura and
Koopmania as generically distinct from Artibeus must be based on the
magnitude of difference that distinguishes each rather than on the
conclusion that to place them as congeneric with Artibeus creates a
paraphyletic taxon.
相似文献
80.
Biotinyl-oligosaccharides are a relatively new generation of saccharide
probes that enable immobilization of desired oligosaccharides on
streptavidin matrices for studies of carbohydrate-protein interactions.
Here we describe the facile preparation of biotinyl-l-3-(2-naphthyl)-
alanine hydrazide (BNAH) derivatives of oligosaccharides, containing a
strong UV absorbing and fluorescent group, in which the ring of the
reducing-end monosaccharide is nonreduced. We evaluate reactivities of
immobilized BNAH- N -glycans with plant lectins that recognize aspects of
the oligosaccharide core or outer-arms. We make some comparisons with
2-amino-6-amidobiotinyl-pyridine (BAP) derivatives obtained by reductive
amination, and 6-(biotinyl)-aminocaproyl-hydrazide (BACH) derivatives which
have a longer spacer-arm. N -Glycan-BNAH and-BAP derivatives have, overall,
comparable reactivities with lectins which recognize N -glycan outer-arms
or the trimannosyl core, but only BNAH and BACH derivatives are bound by
lectins which recognize the non- reduced core. Moreover, with Pisum sativum
agglutinin (PSA) which additionally requires the fucosyl- N-
glycan-asparaginyl core for high affinity binding, the immobilized BNAH
derivative (which is an alanine hydrazide beta-glycoside) can substitute
for the natural beta- glycosylasparaginyl core, whereas the BACH derivative
(aminocaproyl- hydrazide-beta-glycoside) is less effective. BNAH is a
derivatization reagent of choice, therefore, for solid phase
carbohydrate-binding experiments with immobilized N -glycans.
相似文献