Cyclic peptide scaffold with ability to stabilize and deliver a helical cell-impermeable cargo across membranes of cultured cancer cells [0.03%]
一种能够稳定和递送螺旋状的、不可渗透细胞膜的药物分子穿过培养癌细胞膜的环肽支架
Nicole Lawrence,Grégoire J-B Philippe,Peta J Harvey et al.
Nicole Lawrence et al.
Cell penetrating peptides (CPPs) are valuable tools for developing anticancer therapies due to their ability to access intracellular targets, including protein-protein interactions. cPF4PD is a newly described CPP designed from a transducti...
Fluorescent macrolide probes - synthesis and use in evaluation of bacterial resistance [0.03%]
荧光大环内酯抗生素探针的合成及其在细菌耐药性评价中的应用
M Rhia L Stone,Urszula Łapińska,Stefano Pagliara et al.
M Rhia L Stone et al.
The emerging crisis of antibiotic resistance requires a multi-pronged approach in order to avert the onset of a post-antibiotic age. Studies of antibiotic uptake and localisation in live cells may inform the design of improved drugs and hel...
Aquaporin-driven hydrogen peroxide transport: a case of molecular mimicry? [0.03%]
过氧化氢的水通道：分子模拟的例子？
Darren Wragg,Stefano Leoni,Angela Casini
Darren Wragg
Aquaporins (AQPs) are membrane proteins that have evolved to control cellular water uptake and efflux, and as such are amongst the most ancient biological "devices" in cellular organisms. Recently, using metadynamics, we have shown that wat...
Rosalind L Booth,Gideon Grogan,Keith S Wilson et al.
Rosalind L Booth et al.
Biocatalytic imine reduction has been a topic of intense research by the artificial metalloenzyme community in recent years. Artificial constructs, together with natural enzymes, have been engineered to produce chiral amines with high enant...
Dehydroamino acid chemical biology: an example of functional group interconversion on proteins [0.03%]
脱氢氨基酸化学生物学：蛋白质功能基团互变的一个例子
Lyn H Jones
Lyn H Jones
In nature, dehydroalanine (Dha) and dehydrobutyrine (Dhb) residues are byproducts of protein aging, intermediates in the biosynthesis of lanthipeptides and products of bacterial phospholyases that inactivate host kinase immune responses. Re...
Jonathan Cramer,Xiaohua Jiang,Wojciech Schönemann et al.
Jonathan Cramer et al.
In biological systems, polar interactions are heavily burdened by high desolvation penalties resulting from strong solute-solvent interactions. As a consequence thereof, enthalpic contributions of hydrogen bonds to the free energy of bindin...
Fluorescent small-molecule agonists as follicle-stimulating hormone receptor imaging tools [0.03%]
荧光小分子激动剂作为卵泡刺激素受体示踪工具
Sascha Hoogendoorn,Gijs H M van Puijvelde,Gijs A van der Marel et al.
Sascha Hoogendoorn et al.
Fluorescent cell surface receptor agonists allow visualization of processes that are set in motion by receptor activation. This study describes the synthesis of two fluorescent, low molecular weight ligands for the follicle-stimulating horm...
Structural and biophysical insights into the mode of covalent binding of rationally designed potent BMX inhibitors [0.03%]
关于合理设计的高效BMX抑制剂共价结合模式的结构和生物物理见解
João D Seixas,Bárbara B Sousa,Marta C Marques et al.
João D Seixas et al.
The bone marrow tyrosine kinase in chromosome X (BMX) is pursued as a drug target because of its role in various pathophysiological processes. We designed BMX covalent inhibitors with single-digit nanomolar potency with unexploited topologi...
A thorough analysis and categorization of bacterial interrupted adenylation domains, including previously unidentified families [0.03%]
包括之前未被识别的家族在内细菌中断腺苷酰化域的彻底分析和分类
Taylor A Lundy,Shogo Mori,Sylvie Garneau-Tsodikova
Taylor A Lundy
Interrupted adenylation (A) domains are key to the immense structural diversity seen in the nonribosomal peptide (NRP) class of natural products (NPs). Interrupted A domains are A domains that contain within them the catalytic portion of an...
Sub-stoichiometric inhibition of IAPP aggregation: a peptidomimetic approach to anti-amyloid agents [0.03%]
用于抗淀粉样物质的小比例胰岛素肽聚合抑制：模拟方法的研究
Debabrata Maity,Sunil Kumar,Ruyof AlHussein et al.
Debabrata Maity et al.
Membrane-catalysed misfolding of islet amyloid polypeptide is associated with the death of β-cells in type II diabetes (T2D). Most active compounds so far reported require high doses for inhibition of membrane bound IAPP fibrillation. Here...