Inhibition of acid sphingomyelinase links sphingolipid remodeling to necroptotic cell death [0.03%]
酸性鞘氨醇磷脂酶的抑制与凋亡坏死相关细胞死亡之间的联系
Luis Agustin E Pilapil,Shweta Chitkara,G Ekin Atilla-Gokcumen
Luis Agustin E Pilapil
Necroptosis is a lytic form of programmed cell death that requires activation of the RIPK1/3-MLKL complex and results in plasma membrane permeabilization. Although the protein components governing necroptosis are well defined, the lipid det...
Discovery and characterization of a novel class of cyclic peptidic compounds inhibiting the subunit interaction of the protein kinase CK2α2β2 holoenzyme [0.03%]
一类新的环状多肽化合物的发现及其对蛋白激酶CK2α2β2全酶亚基相互作用抑制作用的研究
Christian Werner,Sophia Eimermacher,Miriam Lauwers et al.
Christian Werner et al.
CK2 belongs to the eukaryotic protein kinase superfamily and has a distinctive heterotetrameric quaternary structure. In the so-called CK2α2β2 holoenzyme, which is the main form of CK2 in human cells, two catalytic subunits (CK2α) are at...
Chemical basis of fluorogenic substrate probe design: revisiting the past to discover the new in biochemistry [0.03%]
荧光底物探针设计的化学基础：回顾过去，展望生物化学的新发现
Toru Komatsu,Yasuteru Urano
Toru Komatsu
Enzyme activity, rather than mere protein abundance, defines the functional state of the proteome. Fluorogenic probes are molecules that are designed to directly report the "activity" of enzymes by fluorescence changes. In this review, we p...
Rational design of an acridine-derived click chemistry-based artificial metallo-nuclease [0.03%]
基于咔唑衍生物的“点击化学”人工金属核酶的理性设计
Oliver Gould,Alex Gibney,Rebecca Lynn et al.
Oliver Gould et al.
Artificial metallo-nucleases (AMNs) are metal complexes capable of cleaving nucleic acids and represent a promising therapeutic class. We recently established that copper(i)-catalysed azide-alkyne cycloaddition (CuAAC) click chemistry offer...
Probing sulfotransferase binding and inhibition with synthetic PAPS analogs reveals the role of the 3'-phosphate and informs molecular tool design [0.03%]
合成PAPS类似物探测硫转移酶结合与抑制作用揭示了3'-磷酸的作用并为分子工具设计提供信息
Maria Matveeva,Agnieszka Młynarska-Cieślak,Mikołaj Chromiński et al.
Maria Matveeva et al.
Sulfotransferases (STs) are a class of enzymes that catalyze the transfer of the sulfuryl group (-SO3 -), most commonly from the universal cofactor 3'-phosphoadenosine 5'-phosphosulfate (PAPS), to nucleophilic acceptors bearing hydroxyl or ...
David W Christianson
David W Christianson
The hallmark of a mechanism-based inhibitor is a chemical transformation that occurs upon binding in an enzyme active site that typically yields a more potent inhibitory species. A mechanism-based enzyme inhibitor can be a closely-related a...
Engineering a light-controllable fluorescent protein for peroxynitrite detection via genetic code expansion [0.03%]
利用遗传密码扩展技术开发一种可光控的荧光蛋白用以检测过氧亚硝酸盐
Gloricelly M Roman Arocho,Parthasarathi Das,Sachin C Tennakoon et al.
Gloricelly M Roman Arocho et al.
We report a noncanonical amino acid-containing photoconvertible fluorescent protein for selective peroxynitrite detection. Incorporation of p-borono-l-phenylalanine into circularly permuted mEos2 affords a peroxynitrite-responsive sensor th...
Protein digestion using a cysteine-specific backbone cleavage reagent [0.03%]
一种半胱氨酸特异性骨架切割试剂的蛋白质裂解法
Yu-De Chuang,Tsung-Jung Yang,Yu-Chi Chih et al.
Yu-De Chuang et al.
Mass spectrometry (MS)-based protein analysis is an indispensable tool in modern biomedical research. A key step in sample preparation is proteolytic digestion using enzymes with well-defined amino acid specificity, such as trypsin, chymotr...
Alex Hoose,Javier Garcia-Ruiz,Ciara C M Lally et al.
Alex Hoose et al.
Gramicidin S continues to inspire antibiotic designs. It exhibits a conserved two-fold (C 2) symmetry postulated to underpin its biological activity. Here we probe the C 3 symmetry of gramicidin S and its impact on the folding and antibacte...
Mikołaj Chromiński,Mikołaj Żmudziński,Jacek Jemielity
Mikołaj Chromiński
Sulfur(vi) fluoride exchange (SuFEx) reactions were introduced as next-generation click transformations that form robust sulfur(vi)-based linkages under mild conditions. Their defining feature is the unusual behaviour of the S-F bond: it is...