Introduction to Thiopeptides: Biological Activity, Biosynthesis, and Strategies for Functional Reprogramming [0.03%]
硫肽介绍：生物活性、生物合成及功能重构策略
Alexander A Vinogradov,Hiroaki Suga
Alexander A Vinogradov
Thiopeptides (also known as thiazolyl peptides) are structurally complex natural products with rich biological activities. Known for over 70 years for potent killing of Gram-positive bacteria, thiopeptides are experiencing a resurgence of i...
The Chemical Biology of Reversible Lysine Post-translational Modifications [0.03%]
可逆赖氨酸修饰的化学生物学研究进展
Zhipeng A Wang,Philip A Cole
Zhipeng A Wang
Lysine (Lys) residues in proteins undergo a wide range of reversible post-translational modifications (PTMs), which can regulate enzyme activities, chromatin structure, protein-protein interactions, protein stability, and cellular localizat...
In Vitro and Cellular Probes to Study PARP Enzyme Target Engagement [0.03%]
用于研究PARP酶靶点 engagement的体外和细胞探针
Tim J Wigle,Danielle J Blackwell,Laurie B Schenkel et al.
Tim J Wigle et al.
Poly(ADP-ribose) polymerase (PARP) enzymes use nicotinamide adenine dinucleotide (NAD+) to modify up to seven different amino acids with a single mono(ADP-ribose) unit (MARylation deposited by PARP monoenzymes) or branched poly(ADP-ribose) ...
Ploidy Leads a Molecular Motor to Walk Different Paths to Drug Resistance [0.03%]
染色体倍性引导分子马达走向不同的药物抗性路径
Alexander M Real,William M Marsiglia,Arvin C Dar
Alexander M Real
In this issue of Cell Chemical Biology, Pisa et al. (2020) find that haploid and diploid cells differentially develop resistance to the CENP-E inhibitor GSK923295. The results highlight the power of tumor cells to evade growth inhibition an...
Into the Unknown: A Chemical Biology Approach Provides Mechanistic Insight into HCV Entry [0.03%]
化未知为已知：采用化学生物学方法对HCV入胞机制的探索研究
Fang Chen,Luke L Lairson,Mansun Law
Fang Chen
In this issue of Cell Chemical Biology, Hu et al. (2020) demonstrate that chlorcyclizine blocks HCV fusion by targeting the putative fusion peptide on the viral envelope glycoprotein E1. The study provides new insights into the viral fusion...
Pathogen Interference: Targeting Virulence Factors to Tackle Intracellular Microbes [0.03%]
病原干扰：针对毒力因子以对抗胞内微生物
Michael H Lee,Sean-Paul Nuccio,Manuela Raffatellu
Michael H Lee
Infections with Salmonella enterica pose a challenge for antibiotic treatment. In this issue of Cell Chemical Biology, Tsai et al. use a chemical genomics approach to identify dephostatin as an inhibitor of intracellular Salmonella virulenc...
Kazuki Shiraiwa,Rong Cheng,Hiroshi Nonaka et al.
Kazuki Shiraiwa et al.
Protein analysis under biological conditions is now regarded as indispensable for understanding the structure and function of proteins, in addition to in vitro studies using purified target proteins. Because there are many molecules other t...
Inducible Degradation of Target Proteins through a Tractable Affinity-Directed Protein Missile System [0.03%]
一种通过可操纵的靶向蛋白质导弹系统实现目标蛋白条件性降解的方法
Luke M Simpson,Thomas J Macartney,Alice Nardin et al.
Luke M Simpson et al.
The affinity-directed protein missile (AdPROM) system utilizes specific polypeptide binders of intracellular proteins of interest (POIs) conjugated to an E3 ubiquitin ligase moiety to enable targeted proteolysis of the POI. However, a chemi...
Targeting Endogenous K-RAS for Degradation through the Affinity-Directed Protein Missile System [0.03%]
利用亲和导向蛋白质导弹系统降解内源性K-RAS
Sascha Röth,Thomas J Macartney,Agnieszka Konopacka et al.
Sascha Röth et al.
K-RAS is known as the most frequently mutated oncogene. However, the development of conventional K-RAS inhibitors has been extremely challenging, with a mutation-specific inhibitor reaching clinical trials only recently. Targeted proteolysi...
Zachary E Potter,Ho-Tak Lau,Sujata Chakraborty et al.
Zachary E Potter et al.
Solution-based structural techniques complement high-resolution structural data by providing insight into the oft-missed links between protein structure and dynamics. Here, we present Parallel Chemoselective Profiling, a solution-based stru...