Dhanusha A Nalawansha,Craig M Crews
Dhanusha A Nalawansha
Targeted protein degradation (TPD) has emerged as an exciting new era in chemical biology and drug discovery. PROteolysis TArgeting Chimera (PROTAC) technology targets cellular proteins for degradation by co-opting the ubiquitin-proteasome ...
Parallel Discovery Strategies Provide a Basis for Riboswitch Ligand Design [0.03%]
并行发现策略为Riboswitch配体设计提供依据
Brandon Tran,Patricio Pichling,Logan Tenney et al.
Brandon Tran et al.
Riboswitches are mRNA domains that make gene-regulatory decisions upon binding their cognate ligands. Bacterial riboswitches that specifically recognize 5-aminoimidazole-4-carboxamide riboside 5'-monophosphate (ZMP) and 5'-triphosphate (ZTP...
Seeing (and Using) the Light: Recent Developments in Bioluminescence Technology [0.03%]
看见（并利用）光明：生物发光技术的最新发展
Anna C Love,Jennifer A Prescher
Anna C Love
Bioluminescence has long been used to image biological processes in vivo. This technology features luciferase enzymes and luciferin small molecules that produce visible light. Bioluminescent photons can be detected in tissues and live organ...
Vincent J Guen,Claude Prigent
Vincent J Guen
The primary cilium is generally a non-motile solitary organelle that protrudes from a basal body at the cell surface in various cell types in multicellular organisms. This microtubule-based structure acts as a cell signaling platform to con...
Catalytic Domain Plasticity of MKK7 Reveals Structural Mechanisms of Allosteric Activation and Diverse Targeting Opportunities [0.03%]
MKK7的催化结构域可塑性揭示了异构激活的结构机制及多样的靶向机遇
Martin Schröder,Li Tan,Jinhua Wang et al.
Martin Schröder et al.
MKK7 (MEK7) is a key regulator of the JNK stress signaling pathway and targeting MKK7 has been proposed as a chemotherapeutic strategy. Detailed understanding of the MKK7 structure and factors that affect its activity is therefore of critic...
Julie M Garlick,Anna K Mapp
Julie M Garlick
Dynamic proteins perform critical roles in cellular machines, including those that control proteostasis, transcription, translation, and signaling. Thus, dynamic proteins are prime candidates for chemical probe and drug discovery but diffic...
Triplexed Affinity Reagents to Sample the Mammalian Inositol Pyrophosphate Interactome [0.03%]
用于筛选哺乳动物肌醇焦磷酸互作组的三重复亲和试剂
David Furkert,Sarah Hostachy,Michal Nadler-Holly et al.
David Furkert et al.
The inositol pyrophosphates (PP-InsPs) are a ubiquitous group of highly phosphorylated eukaryotic messengers. They have been linked to a panoply of central cellular processes, but a detailed understanding of the discrete signaling events is...
Small Substrate or Large? Debate Over the Mechanism of Glycation Adduct Repair by DJ-1 [0.03%]
小底物还是大底物？关于DJ-1修复糖基化加合物的机制之争
Yong Woong Jun,Eric T Kool
Yong Woong Jun
Glycation, the term for non-enzymatic covalent reactions between aldehyde metabolites and nucleophiles on biopolymers, results in deleterious cellular damage and diseases. Since Parkinsonism-associated protein DJ-1 was proposed as a novel d...
Mechanism of Cell Penetration by Permeabilization of Late Endosomes: Interplay between a Multivalent TAT Peptide and Bis(monoacylglycero)phosphate [0.03%]
晚期内体透化介导的细胞穿透机制：多价TAT肽与双(单酰甘油)磷酸盐之间的相互作用
Dakota J Brock,Helena Kondow-McConaghy,Jason Allen et al.
Dakota J Brock et al.
Many cellular delivery reagents enter the cytosolic space of cells by escaping the lumen of endocytic organelles and, more specifically, late endosomes. The mechanisms involved in endosomal membrane permeation remain largely unresolved, whi...
Concise Chemoenzymatic Total Synthesis and Identification of Cellular Targets of Cepafungin I [0.03%]
丝孢菌素I的简明化学酶法全合成及其细胞靶点确认
Alexander Amatuni,Anton Shuster,Alexander Adibekian et al.
Alexander Amatuni et al.
The natural product cepafungin I was recently reported to be one of the most potent covalent inhibitors of the 20S proteasome core particle through a series of in vitro activity assays. Here, we report a short chemoenzymatic total synthesis...