408316-46-1Relevant academic research and scientific papers
SNP discrimination by tolane-modified peptide nucleic acids: Application for the detection of drug resistance in pathogens
Ebara, Yasuhito,Hayashi, Tenko,Hori, Sakiko,Kaihatsu, Kunihiro,Kato, Nobuo,Ogata, Katsuya,Okazaki, Miku,Sawada, Shinjiro,Takagi, Kenji
, (2020/02/26)
During the treatment of viral or bacterial infections, it is important to evaluate any resistance to the therapeutic agents used. An amino acid substitution arising from a single base mutation in a particular gene often causes drug resistance in pathogens. Therefore, molecular tools that discriminate a single base mismatch in the target sequence are required for achieving therapeutic success. Here, we synthesized peptide nucleic acids (PNAs) derivatized with tolane via an amide linkage at the N-terminus and succeeded in improving the sequence specificity, even with a mismatched base pair located near the terminal region of the duplex. We assessed the sequence specificities of the tolane-PNAs for single-strand DNA and RNA by UV-melting temperature analysis, thermodynamic analysis, an in silico conformational search, and a gel mobility shift assay. As a result, all of the PNA-tolane derivatives stabilized duplex formation to the matched target sequence without inducing mismatch target binding. Among the different PNA-tolane derivatives, PNA that was modified with a naphthyl-type tolane could efficiently discriminate a mismatched base pair and be utilized for the detection of resistance to neuraminidase inhibitors of the influenza A/H1N1 virus. Therefore, our molecular tool can be used to discriminate single nucleotide polymorphisms that are related to drug resistance in pathogens.
PROTEIN KINASE C AGONISTS
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, (2020/09/12)
The present disclosure relates generally to certain diacylglycerol lactone compounds, pharmaceutical compositions comprising said compounds, and methods of making and using said compounds and pharmaceutical compositions. The compounds and compositions disclosed herein may be used for the treatment or prevention of diseases, disorders, or infections modifiable by protein kinase C (PKC) agonists, such as HIV.
PHENYL-(AZA)CYCLOALKYL CARBOXYLIC ACID GPR120 MODULATORS
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, (2016/04/20)
The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR120 G protein-coupled receptor modulators which may be used as medicaments.
Synthesis of meta- and paracyclophanes containing unsaturated amino acid residues
Gibson, Susan E.,Jones, Jerome O.,Kalindjian, S. Barret,Knight, Jamie D.,Mainolfi, Nello,Rudd, Matthew,Steed, Jonathan W.,Tozer, Matthew J.,Wright, Paul T.
, p. 6945 - 6958 (2007/10/03)
[7.7], [8.8], [9.9] and [13.13] Paracyclophanes and [9.9] and [13.13] metacyclophanes containing two unsaturated amino acid residues have been synthesised. An X-ray crystallographic study of three of the paracyclophanes and molecular modelling of two para
Synthesis of a novel diarylphosphinic acid: A distorted ground state mimic and transition state analogue for amide hydrolysis
Schuman, Marc,Lopez, Xabier,Karplus, Martin,Gouverneur, Véronique
, p. 10299 - 10307 (2007/10/03)
We describe herein the synthesis of a new unsymmetrical diarylphosphinic acid, a hapten aimed to produce catalytic antibodies for the hydrolysis of heterocyclic amides. The phosphinate functionality was selected as a mimic both of the tetrahedral intermed
