Leveraging the cruzain S3 subsite to increase affinity for reversible covalent inhibitors.
Sign Up to like & getrecommendations! Published in 2018 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2018.04.006
Abstract: Cruzain is the major cysteine protease of Trypanosoma cruzi, the etiological agent of Chagas disease. Reversible covalent cruzain inhibitors can block the steps of cell differentiation in the parasite and kill the organism. To this… read more here.
Keywords: affinity; leveraging cruzain; cruzain; cruzain subsite ... See more keywords
Polymer engineering based on reversible covalent chemistry: A promising innovative pathway towards new materials and new functionalities
Sign Up to like & getrecommendations! Published in 2018 at "Progress in Polymer Science"
DOI: 10.1016/j.progpolymsci.2018.03.002
Abstract: Abstract Reversible covalent polymers are able to change their bond arrangement and structure via reversible reaction triggered by external stimuli including heating, light and pH, while retaining the stability of irreversible covalent polymers in the… read more here.
Keywords: engineering; chemistry; covalent polymers; covalent chemistry ... See more keywords
Molecular Biodynamers: Dynamic Covalent Analogues of Biopolymers
Sign Up to like & getrecommendations! Published in 2017 at "Accounts of Chemical Research"
DOI: 10.1021/acs.accounts.6b00594
Abstract: Conspectus Constitutional dynamic chemistry (CDC) features the use of reversible linkages at both molecular and supramolecular levels, including reversible covalent bonds (dynamic covalent chemistry, DCC) and noncovalent interactions (dynamic noncovalent chemistry, DNCC). Due to its… read more here.
Keywords: molecular biodynamers; analogues biopolymers; chemistry; dynamic covalent ... See more keywords
Fabrication of a Smart Nanofluidic Biosensor Through a Reversible Covalent Bond Strategy for High-efficiency Bisulfite Sensing and Removal.
Sign Up to like & getrecommendations! Published in 2020 at "Analytical chemistry"
DOI: 10.1021/acs.analchem.0c00131
Abstract: Bioinspired nanochannel based biosensors have been widely applied for sensing ions, small molecules and biomolecules. However, the low selectivity and difficulty in recycle sensing still heavily hamper their widespread applications. Herein, we designed and fabricated… read more here.
Keywords: high efficiency; biosensor; covalent bond; sensing removal ... See more keywords
A Potent Fluorescent Reversible-Covalent Inhibitor of Cardiac Muscle Contraction.
Sign Up to like & getrecommendations! Published in 2021 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.1c00366
Abstract: Compounds that directly modulate the response of the cardiac sarcomere have potential in the treatment of cardiac disease. While a number of sarcomere activators have been discovered and extensively studied, very few inhibitors have been… read more here.
Keywords: potent fluorescent; muscle; cardiac muscle; troponin ... See more keywords
Structural basis for the inhibitory effects of a novel reversible covalent ligand on PPARγ phosphorylation
Sign Up to like & getrecommendations! Published in 2019 at "Scientific Reports"
DOI: 10.1038/s41598-019-47672-w
Abstract: Peroxisome proliferator-activated receptor γ (PPARγ) is a major therapeutic target for the treatment of type 2 diabetes. However, the use of PPARγ-targeted drugs, such as rosiglitazone and pioglitazone, is limited owing to serious side effects… read more here.
Keywords: ppar; ppar phosphorylation; novel reversible; phosphorylation ... See more keywords
Characterization of FGF401 as a reversible covalent inhibitor of fibroblast growth factor receptor 4.
Sign Up to like & getrecommendations! Published in 2019 at "Chemical communications"
DOI: 10.1039/c9cc02052g
Abstract: Biochemical and structural studies provide information on the mode of action of FGF401 as a selective, reversible covalent inhibitor of FGFR4. Kinase and proliferation assays reveal that FGF401 has the ability to overcome gatekeeper mutations… read more here.
Keywords: covalent inhibitor; characterization fgf401; reversible covalent; fgf401 reversible ... See more keywords