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Carbohydrate-active enzyme-catalyzed stereoselective glycosylation of complex natural product glycosides.
Enzyme Microb Technol
January 2025
Chengdu Institute of Biology, Chinese Academy of Sciences, Chengdu 610213, China. Electronic address:
Natural products and their derivatives are precious resources with extensive applications in various industrial fields. Enzymatic glycosylation is an efficient approach for chemical structure diversification and biological activity alternation of natural products. Herein, we reported a stereoselective glycosylation of complex natural product glycosides catalyzed by two carbohydrate-active enzymes (CAZys).
View Article and Find Full Text PDFDiscovery of novel EGFR-PROTACs capable of degradation of multiple EGFR-mutated proteins.
Eur J Med Chem
June 2024
State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, 210009, China; Jiangsu Key Laboratory of Drug Design and Optimization, Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 211198, China. Electronic address:
Article Synopsis
- Scientists have been trying to treat lung cancer with drugs that target EGFR, but some patients develop resistance to these drugs and have side effects.
- A new technology called PROTAC can help solve this problem by getting rid of the bad mutant forms of EGFR.
- The study created a new drug called IV-3, which worked much better than an earlier version and showed promise in stopping cancer without harming healthy cells.
A new sensitive spectrofluorimetric method for measurement of activity and kinetic study of cholinesterases.
Biochim Biophys Acta Proteins Proteom
January 2020
Kazan Federal University, Neuropharmacology Laboratory, 18 ul. Kremlevskaya, 480002 Kazan, Russian Federation. Electronic address:
A new spectrofluorimetric method more sensitive than the Ellman method was developed for determination of both acetylcholinesterase and butyrylcholinesterase activity and for kinetic analysis of these enzymes and their mutants. Two selected mutants of human butyrylcholinesterase (E197Q and E197G) were included in this work. As for the Ellman's method, substrates are thiocholine esters, but the chromogenic reagent, DTNB (dithio-bisnitro benzoic acid) is replaced by a fluorogenic probe, "Calbiochem Probe IV", (3-(7-Hydroxy-2-oxo-2H-chromen-3-ylcarbamoyl)acrylic acid methylester).
View Article and Find Full Text PDFRelative stability of the S isomers of the oxygen evolving complex of photosystem II.
Photosynth Res
September 2019
Department of Chemistry, The Graduate Center of the City University of New York, New York, NY, 10016, USA.
The oxidation of water to O is catalyzed by the Oxygen Evolving Complex (OEC), a MnCaO complex in Photosystem II (PSII). The OEC is sequentially oxidized from state S to S. The S state, (Mn)(Mn), coexists in two redox isomers: S, where Mn4 is Mn and S, where Mn1 is Mn.
View Article and Find Full Text PDFFrequency of BRAF V600E mutations in 969 central nervous system neoplasms.
Diagn Pathol
June 2016
Department of Neuropathology, Eberhard-Karls University, Calwer Str. 3, 72076, Tübingen, Germany.
Background: Treatment options for oncological diseases have been enhanced by the advent of targeted therapies. The point mutation of the BRAF gene at codon 600 (BRAF V600E) is found in several tumor entities and can be approached with selective inhibitory antibodies. The BRAF inhibitor vemurafenib has demonstrated clinical efficacy in patients with BRAF V600E-mutant melanoma brain metastases and in other cancer diseases.
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