40542-90-3Relevant academic research and scientific papers
PROTAC-mediated degradation of class i histone deacetylase enzymes in corepressor complexes
Adams, Grace E.,Cowley, Shaun Michael,Hodgkinson, James T.,Millard, Christopher J.,Norris, James K. S.,Schwabe, John W. R.,Smalley, Joshua P.,Song, Yun
supporting information, p. 4476 - 4479 (2020/05/13)
We have identified a proteolysis targeting chimera (PROTAC) of class I HDACs 1, 2 and 3. The most active degrader consists of a benzamide HDAC inhibitor, an alkyl linker, and the von Hippel-Lindau E3 ligand. Our PROTAC increased histone acetylation levels and compromised colon cancer HCT116 cell viability, establishing a degradation strategy as an alternative to class I HDAC inhibition.
Engineered peptidic constructs metabolize amyloid β by self-assembly-driven reactions
Mondal, Tanmay,Mandal, Bhubaneswar
supporting information, p. 4933 - 4936 (2019/05/21)
Inspired by the unique mechanism of proteolytic maturation of host cell factor-1, we designed small peptide-based constructs that selectively recognized amyloid β (Aβ) and cleaved it in a non-catalytic manner initially around the α-secretase cleavage-site, thus termed as "artificial α-secretases". "Artificial α-secretases" also cleaved Aβ on the cleavage-sites of other Aβ processing enzymes by prolonged treatment, as evidenced by time-resolved MALDI-TOF-mass analyses.
FIBER COATED NANOPORES
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Paragraph 0475, (2016/07/05)
Provided herein are compositions, compounds, processes, and methods of use of 3D porous coating(s) on or near a nanopore(s) for analysis or detection of charged polymers such as nucleic acids, proteins, protein-nucleic acid complexes, small molecule-biological complexes, polymer-biological complexes, and/or polyelectrolytes.
Hybrids of acylated homoserine lactone and nitric oxide donors as inhibitors of quorum sensing and virulence factors in Pseudomonas aeruginosa
Kutty, Samuel K.,Barraud, Nicolas,Ho, Kitty K. K.,Iskander, George M.,Griffith, Renate,Rice, Scott A.,Bhadbhade, Mohan,Willcox, Mark D. P.,Black, David Stc,Kumar, Naresh
, p. 9850 - 9861 (2015/10/05)
Pseudomonas aeruginosa is an opportunistic pathogen causing a variety of life-threatening diseases such as cystic fibrosis and nosocomial infections in burn victims. The ability of P. aeruginosa to cause infection is attributed to the production of virulence factors such as pyocyanin and elastases. These virulence factors are under the control of quorum sensing (QS) a cell to cell communication process controlled by small diffusible signalling molecules based on N-acyl-homoserine lactones (AHLs) known as autoinducers. The inhibition of QS and thereby virulence factors is seen as a potential new anti-infective strategy. Additionally, the role of nitric oxide (NO) in downstream processes in bacteria such as biofilm dispersal, motility, virulence and antimicrobial defence systems is gaining attention and could be used to control bacterial. Herein we report the design and synthesis of hybrid compounds based on AHL signalling molecules and NO donors as anti-infective agents. A series of AHL-NO hybrids were synthesised and potent inhibitors of QS and virulence factors of P. aeruginosa were identified. This research has led to conversion of agonist AHLs to antagonist AHLs with dual properties of QS inhibition and NO release.
NOVEL FLAVONOID COMPOUNDS AND USES THEREOF
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Paragraph 123; 156-157, (2014/05/07)
The present disclosure provides a compound of the following formula, racemates, enantiomers, prodrugs and salts thereof: Formula (I). Also provided is the use of these compounds for the treatment of ischemia and reperfusion injuries. Further applications include the treatment of diseases caused by cell apoptosis and / or cell necrosis.
The non-metathetic role of Grubbs' carbene complexes: From hydrogen-free reduction of α,β-unsaturated alkenes to solid-supported sequential cross-metathesis/reduction
Poeylaut-Palena, Andres A.,Testero, Sebastian A.,Mata, Ernesto G.
supporting information; experimental part, p. 1565 - 1567 (2011/03/20)
An efficient and high-yielding "hydrogen-free" reduction of α,β-unsaturated alkenes was carried out employing Grubbs' catalyst in a non-metathetic role and Et3SiH. Conditions were optimized under microwave irradiation. Application to the solid-phase organic synthesis allows a facile construction of sp3-sp3 carbon bonds through a sequential cross metathesis/olefin reduction.
Synthesis of cellulose adipate derivatives
Kar, Nilanjana,Liu, Haoyu,Edgar, Kevin J.
experimental part, p. 1106 - 1115 (2012/03/08)
Cellulose esters containing adipates and other ester groups are synthesized by the reaction of commercially available cellulose esters in solution with the benzyl monoester of adipoyl chloride. The products, cellulose adipate esters in which the distal en
Drug release from hydrazone-containing peptide amphiphiles
Matson, John B.,Stupp, Samuel I.
supporting information; experimental part, p. 7962 - 7964 (2011/09/13)
Hydrolytically-labile hydrazones in peptide amphiphiles were studied as degradable tethers for release of the drug nabumetone from nanofiber gels. On-resin addition of the novel compound tri-Boc-hydrazido adipic acid to a lysine ε-amine allowed for precis
Esterification of dicarboxylic acids with benzyl alcohol under the action of the microwave radiation
Aver'yanov,Batrakova,Samuilov,Spiridonova,Kochnev,Galibeev,Gnezdilov
experimental part, p. 1920 - 1923 (2009/02/08)
Reaction of dicarboxylic acid with benzyl alcohol under the microwave irradiation proceeds faster as compared to the thermal conditions. The main reaction products are alkyl dicarboxylates, and the monoester and dibenzyl ether are formed as the side products. A proposal about the nature of the nonthermal effect in the reactions stimulated by the microwave irradiation is considered.
Films and Particles
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Page/Page column 41, (2008/06/13)
Described herein are compounds and processes that can be used to prepare polymer-based films, particles, gels and related compositions, and processes for delivery of agents, and other uses.
