Accelerating multiplexed profiling of protein-ligand interactions: High-throughput plate-based reactive cysteine profiling with minimal input [0.03%]
加速蛋白质-配体相互作用的多重分析：基于平板的高通量反应性半胱氨酸分析（使用最少输入）
Ka Yang,Rebecca L Whitehouse,Shane L Dawson et al.
Ka Yang et al.
Chemoproteomics has made significant progress in investigating small-molecule-protein interactions. However, the proteome-wide profiling of cysteine ligandability remains challenging to adapt for high-throughput applications, primarily due ...
Protein semisynthesis underscores the role of a conserved lysine in activation and desensitization of acid-sensing ion channels [0.03%]
蛋白半合成表征酸感应离子通道活化和脱敏的一个保守赖氨酸的作用
Debayan Sarkar,Iacopo Galleano,Stephanie Andrea Heusser et al.
Debayan Sarkar et al.
Acid-sensing ion channels (ASICs) are trimeric ion channels that open a cation-conducting pore in response to proton binding. Excessive ASIC activation during prolonged acidosis in conditions such as inflammation and ischemia is linked to p...
Yuta Tsukamoto,Manabu Igarashi,Hiroki Kato
Yuta Tsukamoto
Methylation is one of the critical modifications that regulates numerous biological processes. Guanine capping and methylation at the 7th position (m7G) have been shown to mature mRNA for increased RNA stability and translational efficiency...
Profiling nuclear cysteine ligandability and effects on nuclear localization using proximity labeling-coupled chemoproteomics [0.03%]
利用邻近标记-联用化学蛋白质组学对核半胱氨酸配体结合能力及对定位的影响进行表征
Qianni Peng,Eranthie Weerapana
Qianni Peng
The nucleus controls cell growth and division through coordinated interactions between nuclear proteins and chromatin. Mutations that impair nuclear protein association with chromatin are implicated in numerous diseases. Covalent ligands ar...
Irreversible inhibition of TRF2TRFH recruiting functions by a covalent cyclic peptide induces telomeric replication stress in cancer cells [0.03%]
不可逆共价环形肽抑制TRF2结合位点可诱发癌细胞端粒复制应激反应
Alexander P Sobinoff,Salvatore Di Maro,Ronnie R J Low et al.
Alexander P Sobinoff et al.
The TRF2 shelterin component is an essential regulator of telomere homeostasis and genomic stability. Mutations in the TRF2TRFH domain physically impair t-loop formation and prevent the recruitment of several factors that promote efficient ...
Subtype-selective prenylated isoflavonoids disrupt regulatory drivers of MYCN-amplified cancers [0.03%]
选择性牻牛儿牻牛儿基异黄酮素可扰乱MYCN扩增癌的调节驱动因素
Michael E Stokes,Alessandro Vasciaveo,Jonnell Candice Small et al.
Michael E Stokes et al.
Transcription factors have proven difficult to target with small molecules because they lack pockets necessary for potent binding. Disruption of protein expression can suppress targets and enable therapeutic intervention. To this end, we de...
Potent and selective binders of the E3 ubiquitin ligase ZNRF3 stimulate Wnt signaling and intestinal organoid growth [0.03%]
ZNRF3(E3泛素连接酶)高效选择性结合物可刺激Wnt信号传导和肠类器官生长
Yvonne T Kschonsak,Xinxin Gao,Stephen E Miller et al.
Yvonne T Kschonsak et al.
Selective and precise activation of signaling transduction cascades is key for cellular reprogramming and tissue regeneration. However, the development of small- or large-molecule agonists for many signaling pathways has remained elusive an...
Convergent impact of vaccination and antibiotic pressures on pneumococcal populations [0.03%]
疫苗和抗生素压力对肺炎链球菌种群的收敛影响
Cydney N Johnson,Shyra Wilde,Elaine Tuomanen et al.
Cydney N Johnson et al.
Streptococcus pneumoniae is a remarkably adaptable and successful human pathogen, playing dual roles of both asymptomatic carriage in the nasopharynx and invasive disease including pneumonia, bacteremia, and meningitis. Efficacious vaccines...
Selective and brain-penetrant HCN1 inhibitors reveal links between synaptic integration, cortical function, and working memory [0.03%]
选择性和穿透大脑的HCN1抑制剂揭示了突触整合、皮层功能和工作记忆之间的联系
Eva Harde,Markus Hierl,Michael Weber et al.
Eva Harde et al.
Hyperpolarization-activated and cyclic-nucleotide-gated 1 (HCN1) ion channels are proposed to be critical for cognitive function through regulation of synaptic integration. However, resolving the precise role of HCN1 in neurophysiology and ...
HER-096 is a CDNF-derived brain-penetrating peptidomimetic that protects dopaminergic neurons in a mouse synucleinopathy model of Parkinson's disease [0.03%]
HER-096是一种CDNF衍生的穿透血脑屏障的肽模拟物，可保护帕金森病小鼠α-突触核蛋白病模型中的多巴胺能神经元
Natalia Kulesskaya,Arnab Bhattacharjee,Kira M Holmström et al.
Natalia Kulesskaya et al.
Cerebral dopamine neurotrophic factor (CDNF) is an unconventional neurotropic factor that modulates unfolded protein response (UPR) pathway signaling and alleviates endoplasmic reticulum (ER) stress providing cytoprotective effects in diffe...