Analogue biological activities

The objective of the thesis is to build the synthesis process of Analogs of Bengamide A and E, conduct the biological activity of the synthesized Analogs. To find out more about the details of the content, please consult the thesis summary.

27p xacxuoc4321 11-07-2019 31 3   Download

The spermine analogue N1,N11-diethylnorspermine (DENSPM) efficiently depletes the cellular pools of putrescine, spermidine and spermine by down-regulating the activity of the polyamine biosynthetic enzymes and up-regulating the activity of the catabolic enzyme spermidine/ spermine N1-acetyltransferase (SSAT). In the breast cancer cell line L56Br-C1, treatment with 10 lM DENSPM induced SSAT activity 60 and 240-fold at 24 and 48 h after seeding, respectively, which resulted in polyamine depletion. ...

7p research12 01-06-2013 55 5   Download

Insulin-like growth factor (IGF) binding to the type 1 IGF receptor (IGF1R) elicits mitogenic e€ects, promotion of di€erentiation and protection from apoptosis. This study has systematically measured IGF1R binding anities of IGF-I, IGF-II and 14 IGF analogues to a recombinant high-anity form of the IGF1R using BIAcore technology. The analogues assessed could be divided into two groups: (a) those designed to investigate binding of IGF-binding protein, which exhibited IGF1R-binding anities similar to those of IGF-I or IGF-II;...

8p research12 01-06-2013 42 4   Download

Calcitonin (Ct) is a 32-residue peptide hormone that is mainly known for its hypocalcemic effect and the inhibition of bone resorption. Our previous studies have led to potent, side-chain lactam-bridged human Ct (hCt) analogues [Kapurniotu, A. Kayed, R., Taylor, J.W. & Voelter W. (1999) Eur. J. Biochem.265, 606±618; Kapurniotu, A. & Taylor, J.W. (1995)J. Med. Chem.38, 836±847]. We have hypothesized that a possibly type Ibturn/bsheet confor-mation in the region 17±21 may play an important role in hCt bioactivity. ...

12p research12 01-06-2013 47 5   Download

Different pathways of bilayer disruption by the structurally related antimicrobial peptides cecropin B, B1 and B3, revealed by surface plasma resonance analysis of immobi-lized liposomes, differential scanning calorimetryof peptide– large unilamellar vesicle interactions, and light microscopic analysis of peptide-treated giant unilamellar vesicles, have been identified inthis study.

10p tumor12 20-04-2013 40 3   Download

Transketolase from baker’s yeast is a thiamin diphosphate-dependent enzyme in sugar metabolism that reconstitutes with various analogues of the coenzyme. The methylated analogues (4¢-methylamino-thiamin diphos-phate and N1¢-methylated thiamin diphosphate) of the native cofactor were used to investigate the function of the aminopyrimidine moiety of the coen-zyme in transketolase catalysis.

17p awards 06-04-2013 39 4   Download

Adenosine 5¢-polyphosphates have been identified in vitro, as products of certain enzymatic reactions, andin vivo. Although the biological role of these compounds is not known, there exist highly specific hydrolases that degrade nucleoside 5¢-polyphosphates into the corresponding nucleoside 5¢-triphos-phates.

10p dell39 27-03-2013 45 3   Download

trans-[PtCl2NH3(4-Hydroxymethylpyridine)] (trans-PtHMP) is an analogue of clinically ineffective transplatin, which is cytotoxic in the human leuke-mia cancer cell line. As DNA is a major pharmacological target of anti-tumor platinum compounds, modifications of DNA by trans-PtHMP and recognition of these modifications by active tumor suppressor protein p53 were studied in cell-free media using the methods of molecular biology and biophysics.

14p dell39 27-03-2013 50 4   Download

Crystal structures of recombinantLactococcus lactis6-phosphogluconate dehydrogenase (LlPDH) in complex with substrate, cofactor, product and inhibitors have been determined. LlPDH shares significant sequence iden-tity with the enzymes from sheep liver and the protozoan parasite Trypano-soma bruceifor which structures have been reported.

12p inspiron33 23-03-2013 33 4   Download

The 3D structure of a complex formed by the acidic fibroblast growth fac-tor (FGF-1) and a specifically designed synthetic heparin hexasaccharide has been determined by NMR spectroscopy. This hexasaccharide can sub-stitute natural heparins in FGF-1 mitogenesis assays, in spite of not indu-cing any apparent dimerization of the growth factor.

12p inspiron33 23-03-2013 39 4   Download

Host-derived anti-infective proteins represent an important source of sequences for designing antimicrobial peptides (AMPs). However such sequences are often long and comprise diverse amino acids with uncertain contribution to biological effects. Previously, we identified a simple highly cationic peptide derivative of human apolipoprotein E (apoEdp) that inhib-ited a range of microorganisms.

15p media19 04-03-2013 31 3   Download

The role of thiamin diphosphate (ThDP) as a cofactor for enzymes has been known for many decades. This minireview covers the progress made in understanding the catalytic mechanism of ThDP-dependent enzymes through the use of ThDP analogues. Many such analogues have been syn-thesized and have provided information on the functional groups necessary for the binding and catalytic activity of the cofactor.

12p viettel02 22-02-2013 39 3   Download

Four 28-amino acid peptides were synthesized whose sequences comprised two molecules of trypsin inhibitor sunflower trypsin inhibitor 1 (SFTI-1) bound through a peptide bond. The peptides in their reactive positions (5 and 19 of the peptide chain) contain two Lys ([KK]BiSFTI-1) and two Phe ([FF]BiSFTI-1) residues, along with a combination of the amino acid residues named thereafter [KF]BiSFTI-1 and [FK]BiSFTI-1.

9p mobifone23 21-01-2013 45 4   Download

The natural antimicrobial cationic peptide protegrin-1 displays a broad spectrum of antimicrobial activity and rapidly kills pathogens by interacting with their cell membrane. We investigated the structure–activity relation-ships of three protegrin-1 analogues: IB-367 (RGGLCYCRGRFCVCVGR-NH2), BM-1 (RGLCYCRGRFCVCVG-NH2) and BM-2 (RGLCYRPRFV CVG-NH2). Our antimicrobial and antifungal activity studies of these peptides showed that BM-1 was much more active than IB-367 against Gram-positive bacteria and fungi, whereas BM-2 was inactive. ...

13p mobifone23 18-01-2013 55 4   Download