Inhibitory activities

The present study was aimed at the determination of microscopic characteristics and chemical compositions as well as evaluating the antioxidant and acetylcholinesterase inhibitory activities of A. vietnamica.

8p viharuno 03-01-2025 2 2   Download

Pancreatic lipase is one of the safest targets of anti-obesity drugs. To date, orlistat is the only pancreatic lipase inhibitor approved for the long-term treatment of obesity. Therefore, there is an elevated need to find new drugs for this disease.

6p viharuno 03-01-2025 2 2   Download

FtsZ is conserved in almost all bacteria and is an essential protein for bacterial cell division. The cell division is prevented by the inhibitors against FtsZ’s functions. Thus, FtsZ is known as an attractive, and underexploited novel antibacterial target protein. The aim of this research is searching for new antibacterial agents from 72 plants collected in Central Vietnam.

6p viuchiha 03-01-2025 3 2   Download

Hippeastrum reticulatum (L.Hér.) Herb is a species of the Hippeastrum Herb. genus. Screening studies have shown that this species has the ability to inhibit the enzyme acetylcholinesterase. So far, research on this species is still very limited.

5p viuchiha 03-01-2025 5 2   Download

The current study first describes the chemical composition of the leaf essential oil of Cinnamomum subpenninervium Kosterm. ex H.H. Pham collected from Nghe An province, Central Vietnam.

7p vibenya 31-12-2024 2 2   Download

Study on main chemical constituents of two Gymnema species including Gymnema sylvestre and Gymnema latifolium growing in Vietnam and evaluate the inhibitory effect of α-glucosidase and α-amylase enzymes of isolated compounds.

27p closefriend09 16-11-2021 19 4   Download

The objectives of the thesis: Study on chemical constituents of three Trichosanthes species (T. baviensis, T. anguina, and T. kirilowii) grown in Vietnam; evaluation of cytotoxic and tyrosinase enzyme inhibitory activities of isolated compounds from the above mentioned Trichosanthes species.

14p capheviahe26 25-01-2021 20 3   Download

Detection and screening of genes related to biosynthesis of substances with protease inhibitory activity from microorganisms associated with sponge collected from the Mien trung sea of Vietnam by metagenomics method. Then, selective gene, expression of in vitro and determination of activity of the expressed protein.

27p capheviahe26 25-01-2021 19 4   Download

Study on chemical constituents of two Knema species including Knema pachycarpa and Knema saxatilis growing in Vietnam; evaluate cytotoxic and cetylcholinesterase enzyme inhibitory activitiesof isolates to find out bioactive compounds.

25p capheviahe26 25-01-2021 19 4   Download

The objectives of the thesis: Molecular docking studies on acetylcholinesterase were performed to predict the chalcone structure has good in silico AChE acetylcholinesterase inhibitory activity. The potential chalcone compounds were synthesized and studied for their in vitro and in vivo AChE inhibitory activities

25p xacxuoc4321 09-07-2019 43 7   Download

The K103N substitution is a frequently observed HIV-1 RT mutation in patients who do not respond to combinationtherapy. The drugs Efavirenz, MSC194 and PNU142721 belong to the recent generation of NNRTIs characterized by an improved resistance profile to the most common single point mutations within HIV-1 RT, including the K103N mutation. In the present study we present structural observations from Efavirenz in complex with wild-type protein and the K103N mutant and PNU142721 and MSC194 in complex with the K103N mutant.

8p system191 01-06-2013 42 4   Download

Department of Physiology, University of Basel, Switzerland; 2Department of Biophysical Chemistry, Biocenter, University of Basel, Switzerland; 3Xerion Pharmaceuticals, Martinsried, Germany; 4Department of Medicine, Section Pathophysiology, Johannes Gutenberg University of Mainz, Germany; 5Department of Biochemistry, Christian Albrechts University of Kiel, Germany Ciliary neurotrophic factor (CNTF) displays neurotrophic activities on motor neurons and neural cell populations both in vivo and in vitro. ...

9p system191 01-06-2013 41 4   Download

The naturally synchronous plasmodia of myxomycetes synthesize poly(b-L-malic acid), which carries out cell-specific functions. In Physarum polycephalum, poly(b-L-malate) [the salt form of poly(b-L-malic acid)] is highly concentrated in the nuclei, repressing DNA synthetic activity of DNA polymerases by the formation of reversible complexes. To test whether this inhibitory activity is cell-cycle-dependent, purified DNA polymerase a of P.

6p research12 01-06-2013 62 3   Download

Cyclin-dependent kinase-5 (Cdk5) is a serine/threonine kinase activated by its neuron-specific activator, p35, or its truncated form, p25. It has been proposed that the deregu-lation of Cdk5 activity by association with p25 in human brain tissue disrupts the neuronal cytoskeleton and may be involved in neurodegenerative diseases such as Alzheimer’s disease.

8p research12 23-04-2013 33 2   Download

The heterodimeric cytokine composed of the soluble ciliary neurotrophic factor receptor (sCNTFR) and the IL-6 family member cardiotrophin-like cytokine (CLC) was recently identi®ed as a new ligand for gp130±leukemia inhibitory factor receptor (LIFR) complex [Plun-Favreau, H., Elson, G., Chabbert, M., Froger, J., deLapeyriere, O., Lelievre, E., Guillet, C., Hermann, J., Gauchat, J. F., Gascan, H. & Chevalier, S. (2001)EMBO J.20, 1692± 1703]. This heterodimer shows overlapping biological properties with LIF....

10p research12 23-04-2013 30 2   Download

RNA aptamers with anity for the Ras-binding domain (RBD) of Raf-1 were isolated from a degenerate pool by in vitroselection.These aptamers eciently inhibited theRas interaction with the Raf-1 RBD, and also inhibited Ras-induced Raf-1 activation in a cell-free system. The RNA aptamer with the most potent inhibitory e€ect speci®cally inhibited the RasáRaf-1 interaction and had no anity for the RBD of the RGL protein, a homolog of the Ral GDP dissociation stimulator.

8p research12 23-04-2013 40 3   Download

Peptides corresponding to the N-terminus of skeletal myosin light chain 1 (rsMLC1 1–37) and the short loop of human cardiacb-myosin (hcM398–414) have been shown to interact with skeletal F-actin by NMR and fluorescence measurements. Skeletal tropomyosin strengthens the binding of the myosin peptides to actin but does not interact with the peptides. The binding of peptides cor-responding to the inhibitory region of cardiac troponin I (e.g. hcTnI128–153) to F-actin to form a 1 : 1 molar complex is also strengthened in the presence of tropomyo-sin. ...

13p tumor12 22-04-2013 38 2   Download

HIV-1 protease is an important target for treatment of AIDS, and efficient drugs have been developed. However, the resistance and negative side effects of the current drugs has necessitated the development of new compounds with different binding patterns. In this study, nine C-terminally duplicated HIV-1 protease inhibitors were cocrystallised with the enzyme, the crystal structures analysed at 1.8–2.3 A˚ resolution, and the inhibitory activity of the compounds characterized inorder toevaluate the effects of the individual modifications. ...

13p fptmusic 16-04-2013 44 3   Download

Much of the basic biochemistry of antiplasmin was described more than 20 years ago and yet it remains an enigmatic member of the serine protease inhibitor (serpin) family. It possesses all of the characteristics of other inhibitory serpins but in addition it has unique N- and C-terminal exten-sions which significantly modify its activities. The N-terminus serves as a substrate for Factor XIIIa leading to crosslinking and incorporation of antiplasmin into a clot as it is formed.

6p fptmusic 12-04-2013 29 2   Download

The mechanism of inhibition of yeast F0F1-ATPase by its naturally occurring protein inhibitor (IF1) was investi-gated in submitochondrial particles by studying the IF1-mediatedATPase inhibition in the presence andabsence of a protonmotive force. In the presence of protonmotive force, IF1 added during net NTP hydrolysis almost completely inhibitedNTPase activity. At moderate IF1 concentration, subsequent uncoupler addition unexpect-edly caused a burst of NTP hydrolysis.

8p dell39 03-04-2013 49 5   Download