共查询到20条相似文献,搜索用时 31 毫秒
1.
Tomá? Gucky Eva ?ezní?ková Petr D?ubák Marián Hajdúch Vladimír Kry?tof 《Monatshefte für Chemie / Chemical Monthly》2010,55(7):709-714
Abstract
The deregulation of cell cycle components in cancer cells has provided a rationale for the development of small molecule inhibitors of cyclin-dependent kinases as novel anticancer drugs. A series of 1,5-diaryl-3-(3,4,5-trihydroxyphenyl)-1H-pyrazolo[4,3-e][1,2,4]triazines was synthesized and their kinase inhibitory activity and cytotoxicity against several cancer cell lines has been evaluated. Some of the compounds of the series exhibited induction of caspase-dependent cell death and inhibition of cyclin-dependent kinase 2 (CDK2). 相似文献2.
Sadashiva Maralinganadoddi Panchegowda Basappa NanjundaSwamy Shivananju Li Feng Manu Kanjoormana Aryan Sengottuvelan Murugan Prasanna Doddakunche Shivaramu Anilkumar Nirvanappa Chikkagundagal Sethi Gautam Sugahara Kazuyuki Rangappa Kanchugarakoppal Subbegowda 《BMC chemical biology》2012,12(1):1-11
Background
Nef is an HIV-1 accessory protein essential for viral replication and AIDS progression. Nef interacts with a multitude of host cell signaling partners, including members of the Src kinase family. Nef preferentially activates Hck, a Src-family kinase (SFK) strongly expressed in macrophages and other HIV target cells, by binding to its regulatory SH3 domain. Recently, we identified a series of kinase inhibitors that preferentially inhibit Hck in the presence of Nef. These compounds also block Nef-dependent HIV replication, validating the Nef-SFK signaling pathway as an antiretroviral drug target. Our findings also suggested that by binding to the Hck SH3 domain, Nef indirectly affects the conformation of the kinase active site to favor inhibitor association. 相似文献3.
Background
The expression of the drug-metabolizing enzyme cytochrome P450 3A4 (CYP3A4) is regulated by the pregnane × receptor (PXR), which is modulated by numerous signaling pathways, including the cyclin-dependent kinase (Cdk) pathway. Flavonoids, commonly consumed by humans as dietary constituents, have been shown to modulate various signaling pathways (e.g., inhibiting Cdks). Flavonoids have also been shown to induce CYPs expression, but the underlying mechanism of action is unknown. Here, we report the mechanism responsible for flavonoid-mediated PXR activation and CYP expression. 相似文献4.
Katrin de Graaf Hanna Czajkowska Sabine Rottmann Len C Packman Richard Lilischkis Bernhard Lüscher Walter Becker 《BMC biochemistry》2006,7(1):7
Background
The U2 small nuclear ribonucleoprotein particle (snRNP) component SF3b1/SAP155 is the only spliceosomal protein known to be phosphorylated concomitant with splicing catalysis. DYRK1A is a nuclear protein kinase that has been localized to the splicing factor compartment. Here we describe the identification of DYRK1A as a protein kinase that phosphorylates SF3b1in vitro and in cultivated cells. 相似文献5.
Background
We have recently demonstrated that modulation of the gap junction protein, connexin43, can affect the response of osteoblasts to fibroblast growth factor 2 in a protein kinase C-delta-dependent manner. Others have shown that the C-terminal tail of connexin43 serves as a docking platform for signaling complexes. It is unknown whether protein kinase C-delta can physically interact with connexin43. 相似文献6.
Volker Seibert Corinna Prohl Ida Schoultz Edward Rhee Rebecca Lopez Kareem Abderazzaq Chunshui Zhou Dieter A Wolf 《BMC biochemistry》2002,3(1):22-15
Background
SCF ubiquitin ligases share the core subunits cullin 1, SKP1, and HRT1/RBX1/ROC1, which associate with different F-box proteins. F-box proteins bind substrates following their phosphorylation upon stimulation of various signaling pathways. Ubiquitin-mediated destruction of the fission yeast cyclin-dependent kinase inhibitor Rum1p depends on two heterooligomerizing F-box proteins, Pop1p and Pop2p. Both proteins interact with the cullin Pcu1p when overexpressed, but it is unknown whether this reflects their co-assembly into bona fide SCF complexes. 相似文献7.
John E OatisJr Pam Brunsfeld James W Rushing Peter D Moeller Daniel W Bearden Thomas N Gallien George CooperIV 《Chemistry Central journal》2008,2(1):12
Background
The Hedgehog signaling pathway is essential for embryogenesis and for tissue homeostasis in the adult. However, it may induce malignancies in a number of tissues when constitutively activated, and it may also have a role in other forms of normal and maladaptive growth. Cyclopamine, a naturally occurring steroidal alkaloid, specifically inhibits the Hedgehog pathway by binding directly to Smoothened, an important Hedgehog response element. To use cyclopamine as a tool to explore and/or inhibit the Hedgehog pathway in vivo, a substantial quantity is required, and as a practical matter cyclopamine has been effectively unavailable for usage in animals larger than mice. 相似文献8.
Neil G Brown D Nick Morrice Georges Beaud Grahame Hardie David P Leader 《BMC biochemistry》2000,1(1):2-5
Background
Vaccinia virus gene B1R encodes a serine/threonine protein kinase. In vitro this protein kinase phosphorylates ribosomal proteins Sa and S2 and vaccinia virus protein H5R, proteins that become phosphorylated during infection. Nothing is known about the sites phosphorylated on these proteins or the general substrate specificity of the kinase. The work described is the first to address these questions. 相似文献9.
Background
Protein tyrosine kinases are important enzymes for cell signalling and key targets for anticancer drug discovery. The catalytic mechanisms of protein tyrosine kinase-catalysed phosphorylation are not fully understood. Protein tyrosine kinase Csk requires two Mg2+ cations for activity: one (M1) binds to ATP, and the other (M2) acts as an essential activator. 相似文献10.
Mohammed El Amine Dib Nassim Djabou Jean-Marie Desjobert Houcine Allali Boufeldja Tabti Alain Muselli Jean Costa 《Chemistry Central journal》2010,4(1):16
Background
Traditionally, the essential oil of aromatic herbs is obtained using hydrodistillation (HD). Because the emitted volatile fraction plays a fundamental role in a plant's life, various novel techniques have been developed for its extraction from plants. Among these, headspace solid phase microextraction (HS-SPME) can be used to obtain a rapid fingerprint of a plant's headspace. Daucus crinitus Desf. is a wild plant that grows along the west coast of Algeria. Only a single study has dealt with the chemical composition of the aerial part oils of Algerian D. crinitus, in which isochavicol isobutyrate (39.0%), octyl acetate (12.3%), and β-caryophyllene (5.4%) were identified. Using GC-RI and GC-MS analysis, the essential oils and the volatiles extracted from separated organs of D. crinitus Desf. were studied using HS-SPME. 相似文献11.
Background
When eukaryotic cells are deprived of amino acids, uncharged tRNAs accumulate and activate the conserved GCN2 protein kinase. Activated Gcn2p up-regulates the general amino acid control pathway through phosphorylation of the translational initiation factor eIF2. In Saccharomyces cerevisiae, Gcn2p is the only kinase that phosphorylates eIF2 to regulate translation through this mechanism. We addressed changes in yeast growth and tRNA aminoacylation, or charging, during amino acid depletion in the presence and absence of GCN2. tRNA charging was measured using a microarray technique which simultaneously measures all cytosolic tRNAs. A fully prototrophic strain, and its isogenic gcn2Δ counterpart, were used to study depletion for each of the 20 amino acids, with a focus on Trp, Arg, His and Leu, which are metabolically distinct and together provide a good overview on amino acid metabolism. 相似文献12.
Heather B Bradshaw Neta Rimmerman Sherry Shu-Jung Hu Valery M Benton Jordyn M Stuart Kim Masuda Benjamin F Cravatt David K O'Dell J Michael Walker 《BMC biochemistry》2009,10(1):14-11
Background
N-arachidonoyl glycine (NAGly) is an endogenous signaling lipid with a wide variety of biological activity whose biosynthesis is poorly understood. Two primary biosynthetic pathways have been proposed. One suggests that NAGly is formed via an enzymatically regulated conjugation of arachidonic acid (AA) and glycine. The other suggests that NAGly is an oxidative metabolite of the endogenous cannabinoid, anandamide (AEA), through an alcohol dehydrogenase. Here using both in vitro and in vivo assays measuring metabolites with LC/MS/MS we test the hypothesis that both pathways are present in mammalian cells. 相似文献13.
Abstract
Oxovanadium(IV/V) complexes of 2-hydroxyacetophenone-3-hydroxy-2-naphthoylhydrazone (H2L) have been synthesized and characterized. The complexes were characterized by elemental analyses, IR, electronic and EPR spectra. The oxovanadium(V) complex [VOL(OCH3)] is crystallized in two polymorphic forms, denoted by 1a and 1b, with space groups Pn21a and P[`1] P_{{\bar{1}}} , respectively. Both have distorted square pyramidal structures. 相似文献14.
Background
M.tb icd-1 and M.tb icd-2, have been identified in the Mycobacterium tuberculosis genome as probable isocitrate dehydrogenase (ICD) genes. Earlier we demonstrated that the two isoforms can elicit B cell response in TB patients and significantly differentiate TB infected population from healthy, BCG-vaccinated controls. Even though immunoassays suggest that these proteins are closely related in terms of antigenic determinants, we now show that M.tb icd-1 and M.tb icd-2 code for functional energy cycle enzymes and document the differences in their biochemical properties, oligomeric assembly and phylogenetic affiliation. 相似文献15.
Madhukar N. Jachak Sandeep M. Bagul Bhausaheb K. Ghotekar Raghunath B. Toche 《Monatshefte für Chemie / Chemical Monthly》2009,20(5):655-662
Abstract
A series of (2E)-3-(1-chloro-6-methoxy-3,4-dihydronaphthalen-2-yl)-1-(4-aryl)prop-2-en-1-ones (chalcones) have been synthesized by a new synthetic route. The 3-pyridinecarbonitrile derivatives were synthesized by the Michael reaction of malononitrile (in base) and aroylacetonitriles (in acid) with chalcones in one pot. The fluorescent properties and quantum yields of these compounds were studied. 相似文献16.
Qiuhao Qu Hiroki Morizono Dashuang Shi Mendel Tuchman Ljubica Caldovic 《BMC biochemistry》2007,8(1):4
Background
In microorganisms and plants, the first two reactions of arginine biosynthesis are catalyzed by N-acetylglutamate synthase (NAGS) and N-acetylglutamate kinase (NAGK). In mammals, NAGS produces an essential activator of carbamylphosphate synthetase I, the first enzyme of the urea cycle, and no functional NAGK homolog has been found. Unlike the other urea cycle enzymes, whose bacterial counterparts could be readily identified by their sequence conservation with arginine biosynthetic enzymes, mammalian NAGS gene was very divergent, making it the last urea cycle gene to be discovered. Limited sequence similarity between E. coli NAGS and fungal NAGK suggests that bacterial and eukaryotic NAGS, and fungal NAGK arose from the fusion of genes encoding an ancestral NAGK (argB) and an acetyltransferase. However, mammalian NAGS no longer retains any NAGK catalytic activity. 相似文献17.
Abstract
The paths connecting the stationary points of tesseract (four-dimensional hypercube) have been explored. The minimum energy conformations and the different transition states of N,N′-dinaphthyl imidazol-2-ylidenes and imidazolin-2-ylidenes have been calculated. The available experimental results were conveniently reproduced. The dimerization of carbenes to enetetramines has also been calculated. 相似文献18.
Vítor Mendes Ana Maranha Pedro Lamosa Milton S da Costa Nuno Empadinhas 《BMC biochemistry》2010,11(1):21
Background
Maltose-1-phosphate was detected in Mycobacterium bovis BCG extracts in the 1960's but a maltose-1-phosphate synthetase (maltokinase, Mak) was only much later purified from Actinoplanes missouriensis, allowing the identification of the mak gene. Recently, this metabolite was proposed to be the intermediate in a pathway linking trehalose with the synthesis of glycogen in M. smegmatis. Although the M. tuberculosis H37Rv mak gene (Rv0127) was considered essential for growth, no mycobacterial Mak has, to date, been characterized. 相似文献19.
Maria Hägg Olofsson Aleksandra Mandic Havelka Slavica Brnjic Maria C Shoshan Stig Linder 《BMC chemical biology》2008,8(1):2
Background
Intracellular free calcium ([Ca2+]i) is a key element in apoptotic signaling and a number of calcium-dependent apoptosis pathways have been described. We here used a chemical biology strategy to elucidate the relative importance of such different pathways. 相似文献20.
Øystein Stakkestad Anja CV Larsen Anne-Katrine Kvissel Sissel Eikvar Sigurd Ørstavik Bjørn S Skålhegg 《BMC biochemistry》2011,12(1):7