Inhibitors

The specific research objectives of this study are: 1. The development of a high throughput method for evaluation of alloys (5xxx Al as model materials in this work) subject to pitting; 2. Understanding the roles of variation in functional groups' in determining the inhibition efficiency; 3. Elucidating the inhibition mechanisms; and 4. Unveiling the role of intermetallic present in Al matrix and their contribution to the inhibition mechanism, particularly the long-term durability of the inhibitor systems.

104p runthenight04 02-02-2023 9 2   Download

The study "Studies on film forming corrosion inhibitors on aluminium alloy, AA2024-T3" presents key aspects of the film forming behaviour of the selected inhibitors and the test methods used to evaluate the inhibitor induced films in a chloride solution. This study also aims to provide significant insights to the film tenacity, the influence of the molecular structure as well as the film stability in the absence of inhibitors to provide a deeper understanding of the film forming and film breakdown mechanisms.

154p runthenight04 02-02-2023 11 2   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 17 3   Download

To describe the clinical and subclinical features of lung cancer patients with EGFR mutations before TKIs therapy and in the relapsed period. To identify the T790M mutation and MET amplification in patients with lung cancer and EGFR-TKIs resistance and the relationship with clinical and subclinical features.

29p cothumenhmong6 17-07-2020 13 2   Download

The selective effects of these inhibitors are governed by substituent at position 5. Kinetic studies and molecular docking simulation were performed for elucidating mechanisms of enzyme-inhibitor complex formation.

12p tocectocec 25-05-2020 7 0   Download

Regulators of G protein signaling (RGS) proteins modulate G protein-coupled receptor (GPCR) signaling networks by terminating signals produced by active Gα subunits. RGS17, a member of the RZ subfamily of RGS proteins, is typically only expressed in appreciable amounts in the human central nervous system, but previous works have shown that RGS17 expression is selectively upregulated in a number of malignancies, including lung, breast, prostate, and hepatocellular carcinoma.

10p caothientrangnguyen 09-05-2020 13 1   Download

AR-42, a new orally bioavailable, potent, hydroxamate-tethered phenylbutyrate class I/IIB histone deacetylase inhibitor currently is under evaluation in phase 1 and 2 clinical trials and has demonstrated activity in both hematologic and solid tumor malignancies. This report focuses on the preclinical characterization of the pharmacokinetics of AR-42 in mice and rats.

9p caothientrangnguyen 09-05-2020 18 3   Download

The main contents and objectives of the thesis: Synthesis of hydrotalcite bearing benzothiazolylthiosuccinic acid (BTS) modified by silane and applied in solventborne epoxy coating for corrosion protection of carbon steel.

31p xacxuoc4321 09-07-2019 26 7   Download

An optogenetic upgrade for the tet - OFF system fused the inhibitor to the blue light-responsive B-LID degron and optimized the performance of this construct with regard to the number of Med25VBD repeats. This approach resulted in an optogenetic upgrade of the popular Tet-OFF (TetR-VP64, tetO7-PhCMVmin)  system  that  allows tunable, blue light-inducible gene expression in HEK-293T  cells.

5p thuyancn 01-06-2015 30 5   Download

TÍNH CHẤT VI SINH HỌC: 2.Biến dưỡng và tăng trưởng: phụ thuộc vào tế bào ký chủ để sinh năng lượng. (ATP hoặc tái oxi hóa NADPH 3.Sức đề kháng: 60oC/10’ (Đa số ┼). -50oC→-60oC: giữ nhiều năm Phenol, Ether bất hoạt vi khuẩn Inhibitors of protein synthesis (tetracyclines, erythromycins) are effective in most clinical infections

19p shift_12 18-07-2013 115 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 41 4   Download

Certain amino acids, like glutamine and leucine, induce an anabolic response in liver. They activate p70 ribosomal protein S6 kinase (p70S6K) and acetyl-CoA carboxylase (ACC) involved in protein and fatty acids synthesis, respectively. In contrast, the AMP-activated protein kinase (AMPK), which senses the energy state of the cell and becomes activated under metabolic stress, inactivates by phosphorylation key enzymes in biosynthetic pathways thereby conserving ATP.

9p system191 01-06-2013 50 5   Download

The goal of this study was to determine the effects of a putative specific cytosolic phospholipase A2 inhibitor, arachidonyl trifluoromethyl ketone (AACOCF3), on arachidonic acid (AA) release and lipid mediator biosynthesis by ionophore-stimulated human neutrophils. Initial studies indicated that AACOCF3 at concentrations 0–10 lM did not affect AA release from neutrophils. In contrast, AACOCF3 potently inhibited leukotriene B4 formation by ionophore-stimulated neutrophils (IC50  2.5 lM).

11p system191 01-06-2013 45 4   Download

2-Aminoethoxydiphenyl Borate (2-APB) has been extensively used recently as a membrane permeable modulator of inositol-1,4,5-trisphosphate-sensitive Ca2+ channels and store-operated Ca2+ entry. Here, we report that 2-APB is also an inhibitor of sarco/endoplasmic reticulum Ca2+ATPase (SERCA) Ca2+ pumps, and additionally increases ion leakage across the phospholipid bilayer. Therefore, we advise caution in the interpretation of results when used in Ca2+ signalling experiments.

10p system191 01-06-2013 40 4   Download

The synthesis of 10 new phosphoenolpyruvate (PEP) analogues with modifications in the phosphate and the carboxylate function is described. Included are two potential irreversible inhibitors of PEP-utilizing enzymes. One incorporates a reactive chloromethylphosphonate function replacing the phosphate group of PEP. The second contains a chloromethyl group substituting for the carboxylate function of PEP. An improved procedure for the preparation of the known (Z)- and (E)-3-chloro-PEP is also given.

11p system191 01-06-2013 35 3   Download

An immuno-homologue of maize Ca2+/calmodulin (CaM)dependent protein kinase with a molecular mass of 72 kDa was identified in pea. The pea kinase (PsCCaMK) was upregulated in roots in response to low temperature and increased salinity. Exogenous Ca2+ application increased the kinase level and the response was faster than that obtained following stress application. Low temperaturemediated, but not salinity-mediated stress kinase increase was inhibited by the application of EGTA and W7, a CaM inhibitor....

12p system191 01-06-2013 39 5   Download

Venoms from crotalid and viperid snakes contain several peptide inhibitors which regulate the proteolytic activities of their snake-venom metalloproteinases (SVMPs) in a reversible manner under physiological conditions. In this report, we describe the high-resolution crystal structures of a SVMP, TM-3, from Taiwan habu (Trimeresurus mucrosquamatus) cocrystallized with the endogenous inhibitors pyroGlu-Asn-Trp (pENW), pyroGlu-Gln-Trp (pEQW) or pyroGlu-Lys-Trp (pEKW).

10p system191 01-06-2013 30 5   Download

School of Biosciences, University of Birmingham, Edgbaston, Birmingham, UK; 2Shifa College of Medicine, Islamabad, Pakistan.Curcumin is a compound derived from the spice, tumeric. It is a potent inhibitor of the SERCA Ca2þ pumps (all isoforms), inhibiting Ca2þ-dependent ATPase activity with IC50 values of between 7 and 15 mM . It also inhibits ATPdependent Ca2þ-uptake in a variety of microsomal membranes, although for cerebellar and platelet microsomes, a stimulation in Ca2þ uptake is observed at low curcumin concentrations (,10 mM )....

10p system191 01-06-2013 37 5   Download

The serpins are of general protein chemical interest due to their ability to undergo a large conformational change consisting of the insertion of the reactive centre loop (RCL) as strand 4 of the central b sheet A. To make space for the incoming RCL, the ‘shutter region’ opens by the b strands 3A and 5A sliding apart over the underlying a helix B. Loop insertion occurs during the formation of complexes of serpins with their target serine proteinases and during latency transition. This type of loop insertion is unique to plasminogen activator inhibitor-1 (PAI-1).

10p system191 01-06-2013 41 4   Download

This study reports the identification and characterization of the regulatory subunit, TbRSU, of protein kinase A of the parasitic protozoon Trypanosoma brucei. TbRSU is coded for by a single copy gene. The protein contains an unusually long N-terminal domain, the pseudosubstrate site involved in binding and inactivation of the catalytic subunit, and two C-terminally located, closely spaced cyclic nucleotide binding domains.

10p system191 01-06-2013 36 4   Download