Rashi Kahan,Dennis J Worm,Guilherme V de Castro et al.
Rashi Kahan et al.
Protein-Protein interactions (PPIs) are involved in a myriad of cellular processes in all living organisms and the modulation of PPIs is already under investigation for the development of new drugs targeting cancers, autoimmune diseases and...
Brief survey on organometalated antibacterial drugs and metal-based materials with antibacterial activity [0.03%]
有机金属抗菌药物和具有抗菌活性的金属基材料的研究进展综述
Przemysław Biegański,Łukasz Szczupak,Manuel Arruebo et al.
Przemysław Biegański et al.
Rising bacterial antibiotic resistance is a global threat. To deal with it, new antibacterial agents and antiseptic materials need to be developed. One alternative in this quest is the organometallic derivatization of well-established antib...
Wenchao Lu,Milka Kostic,Tinghu Zhang et al.
Wenchao Lu et al.
Targeted covalent inhibitors have regained widespread attention in drug discovery and have emerged as powerful tools for basic biomedical research. Fueled by considerable improvements in mass spectrometry sensitivity and sample processing, ...
Structural motifs and intramolecular interactions in non-canonical G-quadruplexes [0.03%]
非规范G-四链体中的结构基元和分子内相互作用
Jagannath Jana,Swantje Mohr,Yoanes Maria Vianney et al.
Jagannath Jana et al.
Guanine(G)-rich DNA or RNA sequences can assemble or intramolecularly fold into G-quadruplexes formed through the stacking of planar G·G·G·G tetrads in the presence of monovalent cations. These secondary nucleic acid structures have conv...
Site-specific single point mutation by anthranilic acid in hIAPP8-37 enhances anti-amyloidogenic activity [0.03%]
邻氨基苯甲酸在人IAPP8-37的特定位点诱导点突变可增强其抗淀粉样蛋白活性
Sourav Kalita,Sujan Kalita,Ashim Paul et al.
Sourav Kalita et al.
Amylin or hIAPP, together with insulin, plays a significant role in glucose metabolism. However, it undergoes β-sheet rich amyloid formation associated with pancreatic β-cell dysfunction leading to type-2 diabetes (T2D). Recent studies su...
Mapping the energy landscape of protein-ligand binding via linear free energy relationships determined by protein NMR relaxation dispersion [0.03%]
基于蛋白质NMR弛豫展宽法确定的线性自由能关系绘制蛋白质-配体结合的自由能景观
Olof Stenström,Carl Diehl,Kristofer Modig et al.
Olof Stenström et al.
Biochemical signaling is mediated by complexes between macromolecular receptors and their ligands, with the duration of the signal being directly related to the lifetime of the ligand-receptor complex. In the field of drug design, the recog...
Finding and characterizing a catalytic antibody light chain, H34, capable of degrading the PD-1 molecule [0.03%]
一种能够降解PD-1分子的催化抗体轻链H34的鉴定与表征
Emi Hifumi,Hiroaki Taguchi,Tamami Nonaka et al.
Emi Hifumi et al.
Programmed cell death 1 (PD-1) is an immune checkpoint molecule regulating T-cell function. Preventing PD-1 binding to its ligand PD-L1 has emerged as an important tool in immunotherapy. Here, we describe a unique human catalytic antibody l...
In silico peptide-directed ligand design complements experimental peptide-directed binding for protein-protein interaction modulator discovery [0.03%]
计算肽导向配体设计补充实验肽结合导向对蛋白质-蛋白质相互作用调节剂的发现
Lesley Ann Howell,Andrew Michael Beekman
Lesley Ann Howell
Using the protein-protein interaction of Mcl-1/Noxa, two methods for efficient modulator discovery are directly compared. In silico peptide-directed ligand design is evaluated against experimental peptide-directed binding, allowing for the ...
A STING-based fluorescent polarization assay for monitoring activities of cyclic dinucleotide metabolizing enzymes [0.03%]
一种基于STING的荧光偏振检测环二核苷酸代谢酶活性的方法
Caroline W Karanja,Kofi S Yeboah,Wilson W S Ong et al.
Caroline W Karanja et al.
Cyclic dinucleoties, such as cGAMP, c-di-GMP and c-di-AMP, are fascinating second messengers with diverse roles in both prokaryotes and eukaryotes. Consequently there is a need for simple and inexpensive methods for profiling these compound...
A peptidic inhibitor for PD-1 palmitoylation targets its expression and functions [0.03%]
针对PD-1棕榈酰化的肽类抑制剂可靶向其表达和功能
Han Yao,Chushu Li,Fang He et al.
Han Yao et al.
Programmed cell death protein 1 (PD-1) is a crucial anticancer target, but the relatively low response rate and acquired resistance to existing antibody drugs highlight an urgent need to develop alternative targeting strategies. Here, we re...