An automatic pipeline for the design of irreversible derivatives identifies a potent SARS-CoV-2 Mpro inhibitor [0.03%]
一种设计不可逆衍生物的自动管道能够识别出一种有效的SARS-CoV-2 Mpro抑制剂
Daniel Zaidman,Paul Gehrtz,Mihajlo Filep et al.
Daniel Zaidman et al.
Designing covalent inhibitors is increasingly important, although it remains challenging. Here, we present covalentizer, a computational pipeline for identifying irreversible inhibitors based on structures of targets with non-covalent binde...
Directed evolution of potent neutralizing nanobodies against SARS-CoV-2 using CDR-swapping mutagenesis [0.03%]
使用CDR交换诱变进行SARS-CoV-2高效中和纳米抗体的定向进化
Jennifer M Zupancic,Alec A Desai,John S Schardt et al.
Jennifer M Zupancic et al.
There is widespread interest in facile methods for generating potent neutralizing antibodies, nanobodies, and other affinity proteins against SARS-CoV-2 and related viruses to address current and future pandemics. While isolating antibodies...
Targeting ribosomal G-quadruplexes with naphthalene-diimides as RNA polymerase I inhibitors for colorectal cancer treatment [0.03%]
靶向核糖体G-四链体：萘二酰亚胺类RNA聚合酶I抑制剂在结直肠癌治疗中的应用
Victoria Sanchez-Martin,David A Schneider,Matilde Ortiz-Gonzalez et al.
Victoria Sanchez-Martin et al.
Guanine quadruplexes (G4s) are non-canonical nucleic acid structures commonly found in regulatory genomic regions. G4 targeting has emerged as a therapeutic approach in cancer. We have screened naphthalene-diimides (NDIs), a class of G4 lig...
Intracellular H2S production is an autophagy-dependent adaptive response to DNA damage [0.03%]
细胞内H2S生成是一种依赖自噬的DNA损伤适应性反应
Xiaofeng Jiang,Michael R MacArthur,J Humberto Treviño-Villarreal et al.
Xiaofeng Jiang et al.
Hydrogen sulfide (H2S) is a gasotransmitter with broad physiological activities, including protecting cells against stress, but little is known about the regulation of cellular H2S homeostasis. We have performed a high-content small-molecul...
Activity-based, bioorthogonal imaging of phospholipase D reveals spatiotemporal dynamics of GPCR-Gq signaling [0.03%]
基于细胞的生物正交成像揭示了GPCR-Gq信号的时空动态特性
Dongjun Liang,Ross W Cheloha,Tomoyuki Watanabe et al.
Dongjun Liang et al.
Canonically, G-protein-coupled receptor (GPCR) signaling is transient and confined to the plasma membrane (PM). Deviating from this paradigm, the parathyroid hormone receptor (PTHR1) stimulates sustained Gs signaling at endosomes. In additi...
Yutong Song,Peiyuan Huang,Xiaoying Liu et al.
Yutong Song et al.
Mitochondria, the powerhouse of the cell, are dynamic organelles that undergo constant morphological changes. Increasing evidence indicates that mitochondria morphologies and functions can be modulated by mechanical cues. However, the mecha...
Shipworm symbiosis ecology-guided discovery of an antibiotic that kills colistin-resistant Acinetobacter [0.03%]
利用shipworm共生生态学指导发现一种能够杀死多黏芽孢杆菌的抗抗生素药物
Bailey W Miller,Albebson L Lim,Zhenjian Lin et al.
Bailey W Miller et al.
Teredinibacter turnerae is an intracellular bacterial symbiont in the gills of wood-eating shipworms, where it is proposed to use antibiotics to defend itself and its animal host. Several biosynthetic gene clusters are conserved in T. turne...
Ashley K Grahn,Christina J Miller,Brian K Kay
Ashley K Grahn
In this issue of Cell Chemical Biology, Hentrich et al. (2021) describe the application of the SpyCatcher technology to antibody discovery and validation. Fab-SpyTag fusion proteins can be expressed in the periplasm of protease-deficient ba...
Neil Osheroff
Neil Osheroff
Topoisomerase I is the target for a number of widely prescribed anticancer drugs that are based on camptothecin. In this issue of Cell Chemical Biology, Flor et al. (2020) demonstrate that the cellular response to camptothecin is mediated b...
Matthew Dodson,Annadurai Anandhan,Donna D Zhang
Matthew Dodson
In this issue of Cell Chemical Biology, Kuang et al. (2021) identify microsomal glutathione-S-transferase 1 (MGST1) as an NRF2 target gene that suppresses ferroptosis in pancreatic cancer cells. Mechanistically, MGST1 binds ALOX5 during fer...