Search results for "eps"

Conformational properties of the residues connected by ester and methylated amide bonds: theoretical and solid state conformational studies

2010

Peptides produced by bacteria and fungi often contain an ester bond in the main chain. Some of them have both an ester and methylated amide bond at the same residue. A broad spectrum of biological activities makes these depsipeptides potential drug precursors. To investigate the conformational properties of such modified residues, a systematic theoretical analysis was performed on N-acetyl-L-alanine N′-methylamide (Ac-Ala-NHMe) and the analogues with the ester bond on the C-terminus (Ac-Ala-OMe), N-terminus (Ac-[psi](COO)-Ala-NHMe) as well as the analogues methylated on the N-terminus (Ac-(Me)Ala-OMe) and C-terminus (Ac-[psi](COO)-Ala-NMe2). The ϕ, ψ potential energy surfaces and the confor…

Activity of Cordycepin From Cordyceps sinensis Against Drug-Resistant Tumor Cells as Determined by Gene Expression and Drug Sensitivity Profiling

2021

Cordycepin is one of the substantial components of the parasitic fungus Cordyceps sinensis as well as other Cordyceps species. It exerts various effects such as antimetastatic, antiinflammatory, antioxidant, and neuroprotective activities. Assorted studies revealed in vitro and in vivo anticancer influence of cordycepin and put forward its potential for cancer therapy. However, the role of multidrug resistance-associated mechanisms for the antitumor effect of cordycepin has not been investigated in great detail thus far. Therefore, we searched cordycepin’s cytotoxicity with regard to well-known anticancer drug resistance mechanisms, including ABCB1, ABCB5, ABCC1, ABCG2, EGFR, and TP53, and…

Mikrobiologische C-17-Oxidation von Clavinalkaloiden

1984

Nigral control of hippocampal epilepsy: a dopaminergic hypothesis

1988

Neurotransmitters involved in the habenular control of raphe-hippocampal circuit

1989

Erythrocyte agglutinins in the blood of certain Ascidians

1975

Plasma from Ciona intestinalis, Phallusia mamillata and Ascidia malaca possess hemagglutinin for a variety of erythrocytes. Results obtained by physical and chemical treatments suggest that hemagglutinin for Phallusia mamillata and Ascidia malaca may be a protein or a protein-like substance.

(+)-α-Pinene in the defensive secretion ofNasutitermes princeps (Isoptera, Termitidae)

1990

The frontal secretion ofNasutitermes princeps consists of 89% diterpenes and 11% monoterpenes. In the samples studied, (+)-α-pinene, whose optical purity reaches 99.5%, accounts for more than 80% of the monoterpenic content.

Interfering with Host Proteases in SARS-CoV-2 Entry as a Promising Therapeutic Strategy

2020

Abstract: Due to its fast international spread and substantial mortality, the coronavirus disease COVID-19 evolved to a global threat. Since there is currently no causative drug against this viral infection available, science is striving for new drugs and other approaches to treat the new disease. Studies have shown that the cell entry of coronaviruses into host cells takes place through the binding of the viral spike (S) protein to cell receptors. Priming of the S protein occurs via hydrolysis by different host proteases. The inhibition of these proteases could impair the processing of the S protein, thereby affecting the interaction with the host-cell receptors and preventing virus cell …

Corrigendum to “Anticonvulsant effects of carbenoxolone in genetically epilepsy prone rats (GEPRs)”[Neuropharmacology 47 (2004) 1205-1216]

2009

Pentapeptides containing two dehydrophenylalanine residues - synthesis, structural studies and evaluation of their activity towards cathepsin C

2008

Synthesis, structural and biological studies of pentapeptides containing two Delta Phe residues (Z and E isomers) in position 2 and 4 in peptide chain were performed. All the investigated peptides adopted bent conformation and majority of them could exist as two different. conformers in solution. Only pentapeptides. containing free N-termini appeared to act as weak inhibitors of cathepsin C with the slow-binding, competitive mechanism of inhibition. free acids being bound slightly better than their methyl esters. Results of Molecular modeling suggested significant difference between peptides, depending of the type of amino acid residue in position 5 in peptide chain. Dehydropeptides contain…