Cryo-EM structures of human OAT1 reveal drug binding and inhibition mechanisms [0.03%]
人类OAT1的 cryo-EM结构揭示了药物结合和抑制机制
Hyung-Min Jeon,Jisung Eun,Kelly H Kim et al.
Hyung-Min Jeon et al.
The organic anion transporter 1 (OAT1) plays a key role in excreting waste from organic drug metabolism and contributes significantly to drug-drug interactions and drug disposition. However, the structural basis of specific substrate and in...
Nanobodies restore stability to cancer-associated mutants of tumor suppressor protein p16INK4a [0.03%]
纳米抗体可恢复肿瘤抑制蛋白p16INK4a相关癌变突变的稳定性
Owen Burbidge,Martyna W Pastok,Diana Papini et al.
Owen Burbidge et al.
We describe the generation and characterization of camelid single-domain antibodies (nanobodies) raised against tumor suppressor protein p16INK4a (p16). p16 is a cell cycle regulator that inhibits cyclin-dependent kinases CDK4 and CDK6 and ...
The N terminus of H3-influenza hemagglutinin as a site-of-vulnerability to neutralizing antibody [0.03%]
流感病毒血凝素H3的N端末是中和抗体的作用位点
Reda Rawi,Nicholas C Morano,Crystal Sao-Fong Cheung et al.
Reda Rawi et al.
The N terminus of the H3 subtype of influenza virus hemagglutinin is ∼10 residues longer than the N termini of most other hemagglutinins. As conserved, exposed, and linear regions may be good vaccine targets, we investigated the vaccine ut...
Integrating protein sequence design and evolutionary sequence conservation to uncover spectral tuning sites in red-light photoreceptors [0.03%]
结合蛋白质序列设计和进化序列保守性揭示红光受体中的调谐位点
Oliver Maximilian Eder,Massimo Gregorio Totaro,Stefan Minnich et al.
Oliver Maximilian Eder et al.
Protein structure and function are defined by non-covalent interactions of the polypeptide backbone and amino acid side chains providing specific chemical environments. Understanding how these interactions impact stability and/or functional...
Crystallographic fragment screening of CDK2-cyclin A: FragLites map sites of protein-protein interaction [0.03%]
针对CDK2-细胞周期蛋白A的晶体学片段筛选：FragLites绘制蛋白质-蛋白质相互作用位点
Ian Hope,Mathew P Martin,Ziwei Jiang et al.
Ian Hope et al.
Sites of protein-protein interaction (PPI) are potentially more selective binding sites for therapeutics than protein substrate-binding sites. PPIs include distinct regions frequently called "hotspots," sites of key amino acid interactions....
Cryo-EM structure of the vault from human brain reveals symmetry mismatch at its caps [0.03%]
来自人类大脑的vault蛋白的低温电镜结构揭示其帽部的不对称性匹配问题
Sofia Lövestam,Sjors H W Scheres
Sofia Lövestam
The vault protein is expressed in most eukaryotic cells, where it is assembled on polyribosomes into large hollow barrel-shaped complexes. Despite its widespread and abundant presence in cells, the biological function of the vault remains u...
Small molecule dysregulation of ClpP activity via bidirectional allosteric pathways [0.03%]
小分子通过双向别构途径调控ClpP活性
Marim M Barghash,Mark F Mabanglo,Samuel E Hoff et al.
Marim M Barghash et al.
The bacterial ClpP protease is essential for the virulence and infectivity of many human pathogens and has emerged as a novel antibacterial drug target. Several classes of small molecules dysregulate or activate ClpP, leading to uncontrolle...
Structural insights into the binding modes of Arrestin-3 finger loop to the neuropeptide Y1 and Y2 receptors [0.03%]
逮捕蛋白3手指环对神经肽Y1和Y2受体结合模式的结构见解
Varsha Gupta,Jeannette M Laugwitz,Mateusz Sklodowski et al.
Varsha Gupta et al.
The interaction of the finger loop sequence of arrestin-3 with the neuropeptide Y1 and Y2 G protein-coupled receptors was studied. In cell assays, the finger loop part of arrestin was shown to be essential for Y2R internalization, but had n...
Ernesto J Fuentes
Ernesto J Fuentes
PDZ (PSD-95/Discs-large/ZO-1) domains canonically interact with the C termini of partner proteins; however, they also bind internal motifs. In this issue of Structure, Kumar et al.1 uncover a novel function of PDZ domains, revealing a dynam...
Linda Makhlouf,Elton Zeqiraj
Linda Makhlouf
In this issue of Structure, Chen et al.1 reveal how STAMBP/AMSH, a key deubiquitinase (DUB) in endosomal sorting, is autoinhibited by its microtubule-interacting and transport (MIT) domain blocking the catalytic site. STAM and ubiquitin cha...