Proximity-induced SuFEx increases the potency of cytosolic nucleotidase inhibitors and reveals a rare example of covalently targeted histidine [0.03%]
邻近诱导的SuFEx增强了细胞质核苷酸酶抑制剂的活性，并揭示了罕见的共价靶向组氨酸的例子
Mikolaj Chrominski,Marcin Warminski,Mateusz Kozarski et al.
Mikolaj Chrominski et al.
Structure-guided design is one of the most validated solutions for targeting proteins with specific ligands for therapeutic purposes. Nevertheless, it remains challenging to target enzymes with low affinity for their natural ligands and spe...
Synthesis of 4-azido sialic acid for testing against Siglec-7 and in metabolic oligosaccharide engineering [0.03%]
用于检测Siglec-7及代谢型寡糖工程技术的4-叠氮乙酰神经氨酸的合成
Taylor E Gray,Kristin B Labasan,Gour C Daskhan et al.
Taylor E Gray et al.
An important approach for tracking and visualizing sialic acid-containing glycans involves using sialic acid reporters functionalized with bioorthogonal handles. More specifically, metabolic oligosaccharide engineering (MOE) commonly employ...
Shivangi Sharma,J Trae Hampton,Tatiana G Kutateladze et al.
Shivangi Sharma et al.
Epigenetic mechanisms involve cooperative actions of enzymes that produce or remove post-translational modifications in histones and 'readers', the protein domains that bind these modifications. Methylation of lysine residues represents one...
Structural and mechanistic insights into KslB, a bacterial Pictet-Spenglerase in kitasetaline biosynthesis [0.03%]
细菌キタセタール生物合成中的Pictet-Spengler酶KslB的结构和机制研究见解
Wantae Kim,Ziyang Zheng,Kangsan Kim et al.
Wantae Kim et al.
KslB is one of the few bacterial Pictet-Spenglerases recently identified in the biosynthesis of the β-carboline compound kitasetaline. While previous in vitro studies established that KslB catalyzes the condensation between l-tryptophan an...
Enzyme-mediated proximity labeling reveals the co-translational targeting of DLGAP5 mRNA to the centrosome during mitosis [0.03%]
基于酶的邻近标记技术揭示DLGAP5 mRNA在有丝分裂中以共翻译方式靶向中心体
Gang Wang,Mo Li,Peng Zou
Gang Wang
Subcellular RNA localization is a conserved mechanism in eukaryotic cells and plays critical roles in diverse physiological processes including cell proliferation, differentiation, and embryo development. Nevertheless, the characterization ...
Photoaffinity enabled transcriptome-wide identification of splice modulating small molecule-RNA binding events in native cells [0.03%]
光亲和力实现细胞内小分子RNA结合事件的裂解调控及全长转录组识别技术
Raven Shah,Wanlin Yan,Joyce Rigal et al.
Raven Shah et al.
Splice modulating small molecules have been developed to promote the U1 snRNP to engage with pre-mRNAs with strong and altered sequence preference. Transcriptomic profiling of bulk RNA from compound treated cells enables detection of RNAs i...
Florentine U Rutaganira,Maxwell C Coyle,Maria H T Nguyen et al.
Florentine U Rutaganira et al.
Animal kinases regulate cellular responses to environmental stimuli, including cell differentiation, migration, survival, and response to stress, but the ancestry of these functions is poorly understood. Choanoflagellates, the closest livin...
Thiophosphate bioisosteres of inositol hexakisphosphate enhance binding affinity and residence time on bacterial virulence factors [0.03%]
硫代磷酸肌醇六聚物生物等排体可提高其与细菌毒力因子结合的亲和力及作用时间
Rebecca Cummer,Garvit Bhatt,Lauren M Finn et al.
Rebecca Cummer et al.
Inositol phosphates are essential for mammalian cell signalling with critical roles in cellular processes. The fully phosphorylated inositol phosphate, myo-inositol hexakisphosphate (IP6), modulates numerous eukaryotic proteins and bacteria...
3'- O-β-Glucosylation of nucleoside analogues using a promiscuous bacterial glycosyltransferase [0.03%]
利用一种多功能细菌半乳糖基转移酶对核苷类似物进行3'-O-葡萄糖基化
Jonathan P Dolan,Tessa Keenan,Aisling Ní Cheallaigh et al.
Jonathan P Dolan et al.
Nucleoside analogue therapeutics have a proven capability within drug discovery as antiviral and antineoplastic agents. However, their efficacy can be limited by poor cellular uptake, off target toxicity and low bioavailability. Glycosylati...
Cell-penetrating peptide-conjugated, splice-switching oligonucleotides mitigate the phenotype in BTK/ Tec double deficient X-linked agammaglobulinemia model [0.03%]
一种可穿透细胞的肽-缀合拼接转换寡核苷酸能够缓解BTK/Tec双缺失的X连锁无丙种球蛋白血症模型表型
Burcu Bestas,H Yesid Estupiñán,Qing Wang et al.
Burcu Bestas et al.
Splice-switching oligonucleotides (SSOs) have been developed as a treatment for various disorders, including Duchenne muscular dystrophy and spinal muscular atrophy. Here, the activity of several different SSOs was investigated as potential...