Báo cáo khoa học: Alternative binding modes of an inhibitor to two different kinases doc

... Alternative binding modes of an inhibitor to two different kinases Erika De Moliner*, Nick R. Brown and Louise N. JohnsonLaboratory of Molecular Biophysics, Department of Biochemistry, ... designed to target one particularkinase with other kinases. It is generally assumed that the mode of binding of an inhibitor to one kinase is likely to be similar to the mode of binding to other kinases. ... involve contacts to the nitrogens of TBB. Theresults indicate that similar binding modes of an inhibitor to different kinases cannot be assumed.Materials and methodsCrystal preparation and data collectionHuman...

Báo cáo khoa học: Alternative binding proteins: Anticalins – harnessing the structural plasticity of the lipocalin ligand pocket to engineer novel binding activities pdf

... recombinant expression. With fourstructurally variable loops, the binding site of lipoca-lins is less complex and easier to manipulate [5] thanthe CDR of antibodies, which is composed of alto-gether ... dubbed‘anticalins’ [7,8].Properties and potential of anticalinsEngineered lipocalins offer several advantages overimmunoglobulins. Their size, of < 20 kDa, is muchsmaller than that of antibodies, ... Freising-Weihenstephan, GermanyLipocalins occur in many organisms, such as verte-brates, insects and plants, and even in bacteria, wheretheir physiological role usually lies in the transport orstorage of...

Tài liệu Báo cáo khoa học: Receptor binding characteristics of the endocrine disruptor bisphenol A for the human nuclear estrogen-related receptor c pptx

... deactivation to theoriginally high basal activation state in a dose-depen-dent manner, and thus acts as an inverse antagonist of ERRc.ERRs are a subfamily of orphan NRs and are clo-sely related to two ... role of Arg316 for the ERRc receptor in ligand binding. Thiskind of structure–activity relationship between NRsand ligands has never been explored, and thus it isvery important to seek an amino ... of BPAhave been reported in vivo for many organ tissues andsystems in mice and rats [6,7]. Because the binding of Keywordsbisphenol A; estrogen-related receptor c;nuclear receptor; receptor...

Báo cáo khoa học: Alternative splicing: role of pseudoexons in human disease and potential therapeutic strategies pot

... 8673–8677.62 Friedman KJ, Kole J, Cohn JA, Knowles MR,Silverman LM & Kole R (1999) Correction of aberrantsplicing of the cystic ﬁbrosis transmembrane conduc-tance regulator (CFTR) gene by antisense ... & Bojar H (2002) Analysis of BRCA1, TP53, and TSG101 germline mutations inGerman breast and ⁄ or ovarian cancer families. CancerGenet Cytogenet 138, 120–127.84 Lee WI, Torgerson TR, Schumacher ... bydisruption of an exon splice enhancer: a novelmechanism causing 3-methylcrotonyl-CoA carboxylasedeﬁciency. J Biol Chem 284, 28953–28957.117 Hilgert N, Topsakal V, van Dinther J, Offeciers E,Van de...

Báo cáo khoa học: Alternative splicing: regulation of HIV-1 multiplication as a target for therapeutic action docx

... 4A)[19,24–26]. Binding of SR proteins downstream of asplice acceptor can increase the efﬁciency of U2AF binding to the PPT, either by displacement of hnRNPA1 protein that blocks access of spliceosomal ... multimeriza-tion of hnRNP A1 towards the A3 3¢ss leads to theocclusion of the PPT and to site A3 inhibition [36].Enzymatic and chemical probing revealed theoccurrence of several SC35 and SRp40 binding ... cofactor of ASF ⁄ SF2 [39].Splicing acceptor sites A4a, A4b and A4cRev mRNAs are spliced at all three of these acceptorsites (Fig. 1). The RNA binding proteins Tat and Revare key regulators...

Báo cáo khoa học: Ion-binding properties of Calnuc, Ca2+ versus Mg2+ – Calnuc adopts additional and unusual Ca2+-binding sites upon interaction with G-protein pdf

... metalion binding. Ca2+and Mg2+ binding lead to an increase in the fluorescence intensity of the trypto-phans in an ion-dependent fashion. Ca2+ binding leads to a two- fold increase in tryptophan ... hand,behave differently, and seem to have specific affinityfor only one of the binding sites. Mg2+ binding reduces the intensities of only the c-band, and doesnot cause any change to the J-band.A ... resonance energy transfer from anytryptophan residue near the EF-hand Ca2+site leads to the lanthanide ion showing fluorescence emission inthe bound state. Calnuc shows binding to terbium,and...

Báo cáo khoa học: Activator-binding domains of the SWI ⁄ SNF chromatin remodeling complex characterized in vitro are required for its recruitment to promoters in vivo pot

... coupled binding and folding mecha-nism is likely to be relevant in vivo. This binding mech-anism is assumed to be generally important fortranscription factor interactions with other proteinsand ... activation by galactose To determine whether the activator -binding domains of the SWI ⁄ SNF complex are important for its recruit-ment to promoters in vivo and to determine whetherthe Swi1 and Snf5 domains ... similarly to its recruitment to GAL1-10 andGAL2.The activator -binding domains of Swi1 and Snf5are required for galactose-induced expression of SWI⁄SNF-dependent genesIt was next necessary to determine...

Báo cáo khoa học: DNA-binding characteristics of the regulator SenR in response to phosphorylation by the sensor histidine autokinase SenS from Streptomyces reticuli doc

... responding to diverse extracellu-lar signals? Analysis of the sensor kinases and responseregulators of Streptomyces coelicolor A3(2). Microbio-logy 150, 2795–2806.10 Brian P, Riggle PJ, Santos RA ... [10,11], and the VanR–VanS systemactivates the expression of vancomycin resistance[12,13]. Phosphate control of the production of actino-rhodin and undecylprodigiosin in S. lividans andS. coelicolor ... (2006) Thevancomycin resistance VanRS two- component signaltransduction system of Streptomyces coelicolor. MolMicrobiol 59, 923–935.14 Sola-Landa A, Moura RS & Martı´n JF (2003) The two- component...

Báo cáo khoa học: Actin-binding domain of mouse plectin Crystal structure and binding to vimentin pot

... subdomain of the first (N-terminal) of fimbrin’s two ABDs [20]. In light of the extensive structuralresemblance of fimbrin and plectin ABDs it was therefore of interest to assess IF -binding activity of ... binding domain of plectin suggests alternative mechanisms for binding to F-actin and integrin beta 4. Structure 11, 615–625.25. Hanein, D., Volkmann, N., Goldsmith, S., Michon, A.M., Leh-man,W.,Craig,R.,DeRosier,D.,Almo,S.&Matsudaira,P.(1998) ... structure of two distinctcrystalline forms of one of its ABD versions (pleABD/2a)from mouse, to a resolution of 1.95 and 2.0 A˚. Comparison of pleABD/2a with the ABDs of fimbrin and utrophinrevealed...

Báo cáo khoa học: ATP-binding domain of heat shock protein 70 is essential for its effects on the inhibition of the release of the second mitochondria-derived activator of caspase and apoptosis in C2C12 cells potx

... RG (2005) Antiapoptotic and anti-inﬂammatorymechanisms of heat-shock protein protection. Ann N YAcad Sci 1053, 74–83.34 Liang P, Jiang B, Yang X, Xiao X, Huang X, Long J,Zhang P, Zhang M, Xiao ... inhibition of the release of thesecond mitochondria-derived activator of caspase andapoptosis in C2C12 cellsBimei Jiang1, Kangkai Wang1, Pengfei Liang2, Weimin Xiao1, Haiyun Wang1and Xianzhong ... activationby eliminating inhibition of caspases by inhibitor of apoptosis protein (IAP) and is known to be a new andimportant regulator of apoptosis in a variety of cancercells. The evidence obtained...

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