Jinxia Wan,Yulong Li
Jinxia Wan
In this issue of Cell Chemical Biology, Elleman et al.1 introduce a transformative chemical approach to control neuronal activity with high spatial and temporal resolution. The authors present STX-bpc, a potent neurotoxin that naturally inh...
Blocking smoothened cholesterylation: A strategy for overcoming drug resistance in cancer [0.03%]
阻断平滑肌胆固醇酯化：克服癌症药物抗性的策略
Steven Y Cheng,Ying E Zhang
Steven Y Cheng
In this issue of Cell Chemical Biology, Liu et al.1 report the identification of Q29, a synthetic diterpenoid that blocks covalent cholesterol modification of smoothened (SMO) and inhibits hedgehog signaling. Q29 is capable of suppressing t...
Discovery of a mu-opioid receptor modulator that in combination with morphinan antagonists induces analgesia [0.03%]
发现一种μ型阿片受体调节剂可与吗啡烷类拮抗剂联用产生镇痛作用
Yi-Han Huang,Shu-Yu Lin,Li-Chin Ou et al.
Yi-Han Huang et al.
Morphinan antagonists, which block opioid effects at mu-opioid receptors, have been studied for their analgesic potential. Previous studies have suggested that these antagonists elicit analgesia with fewer adverse effects in the presence of...
The hydrophobicity of the CARD8 N-terminus tunes inflammasome activation [0.03%]
CARD8的N端疏水性调节炎性小体活化
Lydia P Tsamouri,Jeffrey C Hsiao,Qinghui Wang et al.
Lydia P Tsamouri et al.
Mounting evidence indicates that proteotoxic stress is a primary activator of the CARD8 inflammasome, but the complete array of signals that control this inflammasome have not yet been established. Notably, we recently discovered that sever...
Yu Deng,Jing Zhou,Hua-Bing Li
Yu Deng
RNA molecules undergo dynamic chemical modifications in response to various external or cellular stimuli. Some of those modifications have been demonstrated to post-transcriptionally modulate the RNA transcription, localization, stability, ...
The anti-tubercular callyaerins target the Mycobacterium tuberculosis-specific non-essential membrane protein Rv2113 [0.03%]
具有抗结核作用的多氧萘酚类通过靶向特异性非必需膜蛋白Rv2113发挥杀菌效果
David Podlesainski,Emmanuel T Adeniyi,Yvonne Gröner et al.
David Podlesainski et al.
Spread of antimicrobial resistances urges a need for new drugs against Mycobacterium tuberculosis (Mtb) with mechanisms differing from current antibiotics. Previously, callyaerins were identified as promising anti-tubercular agents, represe...
The art of designed coiled-coils for the regulation of mammalian cells [0.03%]
用于调控哺乳动物细胞的螺旋缠绕蛋白的设计艺术
Tjaša Plaper,Erik Rihtar,Taja Železnik Ramuta et al.
Tjaša Plaper et al.
Synthetic biology aims to engineer complex biological systems using modular elements, with coiled-coil (CC) dimer-forming modules are emerging as highly useful building blocks in the regulation of protein assemblies and biological processes...
Synthetic gene circuit evolution: Insights and opportunities at the mid-scale [0.03%]
合成基因线路进化：中期规模的见解与机遇
Christopher Helenek,Rafał Krzysztoń,Julia Petreczky et al.
Christopher Helenek et al.
Directed evolution focuses on optimizing single genetic components for predefined engineering goals by artificial mutagenesis and selection. In contrast, experimental evolution studies the adaptation of entire genomes in serially propagated...
C646 degrades Exportin-1 to modulate p300 chromatin occupancy and function [0.03%]
C646通过降解Exportin-1来调节p300染色质占有率和功能
Yi Fan Chen,Atikur Rahman,Joel L Sax et al.
Yi Fan Chen et al.
Molecular glues can induce proximity between a target protein and ubiquitin ligases to induce target degradation, but strategies for their discovery remain limited. We screened 3,200 bioactive small molecules and identified that C646 requir...
NAMPT-targeting PROTAC and nicotinic acid co-administration elicit safe and robust anti-tumor efficacy in NAPRT-deficient pan-cancers [0.03%]
靶向NAMPT的PROTAC与烟酸联合用药可安全高效地治疗NAPRT缺陷型泛癌种肿瘤
Xiaotong Zhu,Ye Li,Haixia Liu et al.
Xiaotong Zhu et al.
Nicotinamide phosphoribosyltransferase (NAMPT) catalyzes the biosynthesis of nicotinamide adenine dinucleotide (NAD+), making it a potential target for cancer therapy. Two challenges hinder its translation in the clinic: targeting the extra...