Heterogeneity of tethered agonist signaling in adhesion G protein-coupled receptors [0.03%]
粘附G蛋白偶联受体中固定激动剂信号的异质性
Andrew N Dates,Daniel T D Jones,Jeffrey S Smith et al.
Andrew N Dates et al.
Adhesion G protein-coupled receptor (aGPCR) signaling influences development and homeostasis in a wide range of tissues. In the current model for aGPCR signaling, ligand binding liberates a conserved sequence that acts as an intramolecular,...
Identification of an inhibitory pocket in falcilysin provides a new avenue for malaria drug development [0.03%]
在疟原虫丝氨酸蛋白酶falcilysin中发现的抑制性口袋为开发新的抗疟药物提供了新思路
Grennady Wirjanata,Jianqing Lin,Jerzy Michal Dziekan et al.
Grennady Wirjanata et al.
Identification of new druggable protein targets remains the key challenge in the current antimalarial development efforts. Here we used mass-spectrometry-based cellular thermal shift assay (MS-CETSA) to identify potential targets of several...
A light-controlled phospholipase C for imaging of lipid dynamics and controlling neural plasticity [0.03%]
一种光控磷脂酶C用于脂质动力学的成像及神经可塑性的调控
Yeon-Jeong Kim,Suguru Tohyama,Takashi Nagashima et al.
Yeon-Jeong Kim et al.
Phospholipase C (PLC) is a key enzyme that regulates physiological processes via lipid and calcium signaling. Despite advances in protein engineering, no tools are available for direct PLC control. Here, we developed a novel optogenetic too...
Multiparatopic antibodies induce targeted downregulation of programmed death-ligand 1 [0.03%]
多价抗体诱导程序性死亡配体-1的靶向下调作用
Seth D Ludwig,Bunyarit Meksiriporn,Jiacheng Tan et al.
Seth D Ludwig et al.
Programmed death-ligand 1 (PD-L1) drives inhibition of antigen-specific T cell responses through engagement of its receptor programmed death-1 (PD-1) on activated T cells. Overexpression of these immune checkpoint proteins in the tumor micr...
Discovery of YAP1/TAZ pathway inhibitors through phenotypic screening with potent anti-tumor activity via blockade of Rho-GTPase signaling [0.03%]
通过表型筛选发现具有Rho-GTP酶信号阻滞活性的YAP1/TAZ通路抑制剂
Keith Graham,Philip Lienau,Benjamin Bader et al.
Keith Graham et al.
This study describes the identification and target deconvolution of small molecule inhibitors of oncogenic Yes-associated protein (YAP1)/TAZ activity with potent anti-tumor activity in vivo. A high-throughput screen (HTS) of 3.8 million com...
Identification of clickable HIV-1 capsid-targeting probes for viral replication inhibition [0.03%]
鉴定出可作用于HIV-1衣壳的病毒复制抑制探针
William M McFadden,Mary C Casey-Moore,Grant A L Bare et al.
William M McFadden et al.
Of the targets for HIV-1 therapeutics, the capsid core is a relatively unexploited but alluring drug target due to its indispensable roles throughout virus replication. Because of this, we aimed to identify "clickable" covalent modifiers of...
Chemical proteomics to study metabolism, a reductionist approach applied at the systems level [0.03%]
基于化学蛋白质组学的代谢研究：系统水平上的还原论方法
Md Yousuf Ali,Liron Bar-Peled
Md Yousuf Ali
Cellular metabolism encompasses a complex array of interconnected biochemical pathways that are required for cellular homeostasis. When dysregulated, metabolism underlies multiple human pathologies. At the heart of metabolic networks are en...
Alexander F Russell,Madeline F Currie,Champak Chatterjee
Alexander F Russell
In this issue of Cell Chemical Biology, Peng and Weerapana1 report the combination of chemoproteomic and proximity-based labeling approaches to identify cysteines in nuclear proteins that are reactive toward electrophilic probe compounds. T...
Ku-Lung Hsu,Ben Schumann,Ellen Sletten et al.
Ku-Lung Hsu et al.
Bioorthogonal chemistry was deservedly recognized with the 2022 Nobel Prize in Chemistry, having transformed the way chemists and biologists interrogate biological systems in the past twenty years. This Voices piece asks researchers from a ...
Sigrid Nachtergaele
Sigrid Nachtergaele
In this Stories piece, Sigrid Nachtergaele-an assistant professor at the Yale University Department of Molecular, Cellular, and Developmental Biology-shares her experience and efforts to cut barriers for the next generation of aspiring scie...