Báo cáo khoa học: Structure–activity relation for synthetic phenoxazone drugs Evidence for a direct correlation between DNA binding and pro-apoptotic activity pdf

... Structure activity relation for synthetic phenoxazone drugs Evidence for a direct correlation between DNA binding and pro-apoptotic activity Alexei N. Veselkov1, Vladimir Ya. Maleev2, ... width at half height) of the heat absorptioncurve. All values of thermodynamic parameters werecalculated for 1 mol base pairs, taking an average molecularmass of a DNA base pair as 660 Da.ResultsDose-dependent ... struc-ture activity relation. Keywords: apoptotic activity; differential scanning calori-metry (DSC); drug DNA binding; phenoxazone drugs; structure activity relationship.Many anti-tumour drugs are...

... of an arginine residue atposition 12 (Table 1) appears to contribute to a4 b2anda7subtype activity but not a3 b2 activity. A decrease in a4 b2 and a7 subtype activity but not a3 b2 activity was ... Mutational analyses havealso been valuable in elucidating factors important for activity. Table 2 lists the most informative mutations thathave been made in a range of a- conotoxins. In addition,an ... Queensland, Brisbane, QLD, Australia a- Conotoxins that target the neuronal nicotinic acetylcho-line receptor have a range of potential therapeutic applica-tions and are valuable probes for examining...

... that retainsthe antibacterial potency but which has substantiallyreduced cytotoxicity. Such a peptide analog may rep-resent an excellent candidate as a novel antimicrobialagent against bacteria ... fowlicidin-1 and its analogsTwo representative Gram-negative bacteria (Escher-ichia coli ATCC 25922 and Salmonella enterica serovarTyphimurium ATCC 14028) and two Gram-positivebacteria (Listeria monocytogenes ... 94,672–682.9 Nagaoka I, Hirota S, Yomogida S, Ohwada A & HirataM (2000) Synergistic actions of antibacterial neutrophildefensins and cathelicidins. Inflamm Res 49, 73–79.10 Tossi A, Sandri L &...

... described here and is present in theS. agalactiae PPase, kinase and adenylosuccinate syn-thase, but not in S. agalactiae CovR ⁄ CsrR. The motifis located at the surface of the SaPPase (Rantanen,unpublished), ... mechanisms inStreptococcus agalactiae. Mol Microbiol 62, 941–957.23 Rantanen MK, Lehtio¨L, Rajagopal L, Rubens CE &Goldman A (2006) Crystallization and preliminary crys-tallographic analysis ... fused to an EF-hand motif, and human STP(HsSTP), which has an additional 8 kDa a- helicaldomain at the C-terminus [3,4].The sizes of the catalytic domains of both PPP and PPM families are well...

... themutant proteins were as follows (mutated sites are under-lined): D8 8A, 5¢-ACATTTGTCGCCATGGATCC-3¢;D88V, 5¢-GCCGACATTTGTCGTCATGGATCC-3¢;D88N, 5¢-GCCGACATTTGTCAACATGGATCC-3¢; and D39 3A, 5¢-CTGAACCGAGCTGTCGGAAT-3¢.The ... in absorbance (DA) at 413 nm from that at395 nm caused by Cl– binding. Analytical methodsThe Nor activity of P450nor was assayed as reported [4].P450nor (6 nM) was incubated anaerobically ... cluster is important for releasing NAD+, leading to a charge balance in the accesschannel. This charge balance would b e important for both binding to NADH and release of NAD+.It is evident...

... FEBSAsp110Asp185Asp186Trp229Tyr181NNRTIbpETyr188Asp110Asp185Asp186Trp229Cys181NNRTIbpBAsp110Asp185Asp186Trp229Tyr181NNRTIbpTyr188FAsp110Asp185Asp186Trp229Cys181NNRTIbpCAsp110Asp185Asp186Trp229Tyr181Tyr188NNRTIbpGTyr188Tyr181Trp229Asn103DAsp110Asp185Asp186Trp229Tyr181Tyr188NNRTIbpHAsp110Asp185Asp186Trp229Cys181NNRTIbp A K126K126IAsp110Asp185Asp186Tyr181Trp229Asn103K126K54K54KNA53KNA53K49K49VAL10 8A VAL10 6A PHE22 7A LEU23 4A TRP22 9A TYR18 8A TYR31 8A LEU10 0A TYR18 1A VAL10 8A TRP22 9A LEU23 4A PHE22 7A PRO23 6A TYR18 8A VAL10 6A LEU23 4A PHE22 7A VAL10 8A TYR18 8A TYR18 3A TRP22 9A LEU10 0A LEU10 0A TYR31 8A TYR18 8A TRP22 9A LEU23 4A ASN10 3A VAL10 6A VAL10 8A TYR18 8A VAL10 8A TYR18 8A MET23 0A LEU23 4A TRP22 9A VAL10 8A LEU22 8A TRP22 9A LEU10 0A TYR18 8A TYR18 8A VAL10 6A VAL10 8A PHE22 7A TYR31 8A LEU23 4A LEU10 0A VAL10 8A PHE22 7A TYR18 8A LEU23 4A LEU10 0A TYR31 8A VAL10 6A OOOOOOOOOOOOBrOOOOOOOOOOOOOOOOOOOOOOOOOOOOOOOOOOOOOOOOOOPrOFig. ... FEBSAsp110Asp185Asp186Trp229Tyr181NNRTIbpETyr188Asp110Asp185Asp186Trp229Cys181NNRTIbpBAsp110Asp185Asp186Trp229Tyr181NNRTIbpTyr188FAsp110Asp185Asp186Trp229Cys181NNRTIbpCAsp110Asp185Asp186Trp229Tyr181Tyr188NNRTIbpGTyr188Tyr181Trp229Asn103DAsp110Asp185Asp186Trp229Tyr181Tyr188NNRTIbpHAsp110Asp185Asp186Trp229Cys181NNRTIbp A K126K126IAsp110Asp185Asp186Tyr181Trp229Asn103K126K54K54KNA53KNA53K49K49VAL10 8A VAL10 6A PHE22 7A LEU23 4A TRP22 9A TYR18 8A TYR31 8A LEU10 0A TYR18 1A VAL10 8A TRP22 9A LEU23 4A PHE22 7A PRO23 6A TYR18 8A VAL10 6A LEU23 4A PHE22 7A VAL10 8A TYR18 8A TYR18 3A TRP22 9A LEU10 0A LEU10 0A TYR31 8A TYR18 8A TRP22 9A LEU23 4A ASN10 3A VAL10 6A VAL10 8A TYR18 8A VAL10 8A TYR18 8A MET23 0A LEU23 4A TRP22 9A VAL10 8A LEU22 8A TRP22 9A LEU10 0A TYR18 8A TYR18 8A VAL10 6A VAL10 8A PHE22 7A TYR31 8A LEU23 4A LEU10 0A VAL10 8A PHE22 7A TYR18 8A LEU23 4A LEU10 0A TYR31 8A VAL10 6A OOOOOOOOOOOOBrOOOOOOOOOOOOOOOOOOOOOOOOOOOOOOOOOOOOOOOOOOPrOFig. ... transcriptase (RT) has two associated activities, DNA poly-merase and RNase H, both essential for viral replication and validated drugtargets. Although all RT inhibitors approved for therapy...

... bacterial and mammalian templates.P. falciparum Glu295 aligns with an Asp in mam-mals (human arginase II: Asp223; rat arginase I:Asp204), fungi and bacteria (B. caldovelox arginase:Asp199). ... indicated that P. falciparum arginase has a strong depen-dency between trimer formation, enzyme activity and metal co-ordination.Mutations that abolished Mn2+ binding also caused dissociation ... mutations that abolished trimer formation resultedin inactive monomers. By contrast, the monomers of mammalian (and therefore host) arginase are also active. P. falciparum arginase thus appearsto...

... re-activation ratewas observed in all cases. Relative re-activation rates and maximum recoveries were as follows: 1.1 and 82% for yeastmutarotase, 3.2 and 88% for epimerase, and 6.8 and 91% for capsicum ... optima of mutarotase from both kidney cortex and capsicum are broad, with maxima at % 7.4, and activity atpH 4.0 and 8.0 was 70–72%. For yeast mutarotase, the pHoptimum was 7.5, with 60–70% of activity ... from bacteria tomammals, its quaternary structure, size and NAD require-ment vary. The bacterial and yeast enzymes are homo-dimers with bound NAD, whereas, mammalian enzymesare monomeric and...

... CGACACGTAGTTCGCCACCGTCTTTTCfdxA-C8G f TGACGAATAAGGCGTTTGGTCCTTTCCfdxA-C8G r GGAAAGGACCAAACGCCTTATTCGTCAfdxA -A9 T f TGACGAATAAGGCCATTGGTCCTTTCCfdxA -A9 T r GGAAAGGACCAATGGCCTTATTCGTCAfdxA-C8G -A9 T f TGACGAATAAGGCGATTGGTCCTTTCCfdxA-C8G -A9 T ... TGACGGGCTATCGTAAGTTTATGfdxA r CACGCACTCACTACCGATCACAK182G f GAAAAGACGGTGGGGAACTACGTGTCGK182G r CGACACGTAGTTCCCCACCGTCTTTTCK18 2A f GAAAAGACGGTGGCGAACTACGTGTCGK18 2A r CGACACGTAGTTCGCCACCGTCTTTTCfdxA-C8G ... mutation inthe Dev box impairs protein DNA interaction and abrogates DevR-mediated gene induction inMycobacterium tuberculosisRajesh Kumar Gupta, Santosh Chauhan* and Jaya Sivaswami TyagiDepartment...

... times.Analytical HPAECThe deacylated LPS was analysed by analytical high-performance anion exchange chromatography (HPAEC)on a column of CarboPak PA1 (4 mm · 250 mm, Dionex)using the eluents (A) ... metallicsample holder, dried in a stream of air and analyzedimmediately after evaporation. The spectra are the sum of atleast 50 single laser shot experiments. External mass scalecalibration ... [8]. Analytical data haveshown that the fatty acids in LPS of Chlamydiae have acylchains with up to 22 carbon atoms and also that 3-hydroxyfatty acids occur only with amide-linkage [9,10]....