Inhibiting a dynamic viral protease by targeting a non-catalytic cysteine [0.03%]
通过靶向非催化半胱氨酸抑制动态病毒蛋白酶
Kaitlin R Hulce,Priyadarshini Jaishankar,Gregory M Lee et al.
Kaitlin R Hulce et al.
Viruses are responsible for some of the most deadly human diseases, yet available vaccines and antivirals address only a fraction of the potential viral human pathogens. Here, we provide a methodology for managing human herpesvirus (HHV) in...
Glycopeptidolipid glycosylation controls surface properties and pathogenicity in Mycobacterium abscessus [0.03%]
麻风分枝杆菌甘氨糖肽脂质糖基化控制表面特性及致病性
Wassim Daher,Louis-David Leclercq,Matt D Johansen et al.
Wassim Daher et al.
Mycobacterium abscessus is an emerging and difficult-to-manage mycobacterial species that exhibits smooth (S) or rough (R) morphotypes. Disruption of glycopeptidolipid (GPL) production results in transition from S to R and severe lung disea...
Small-molecule HIV-1 entry inhibitors targeting the epitopes of broadly neutralizing antibodies [0.03%]
靶向广谱中和抗体表位的HIV-1进入抑制剂小分子药物
Shibo Jiang,Alexander Tuzikov,Alexander Andrianov
Shibo Jiang
Highly active antiretroviral therapy currently used for HIV/AIDS has significantly increased the life expectancy of HIV-infected individuals. It has also improved the quality of life, reduced mortality, and decreased the incidence of AIDS a...
A selective PPM1A inhibitor activates autophagy to restrict the survival of Mycobacterium tuberculosis [0.03%]
一种选择性的PPM1A抑制剂通过激活自噬限制结核分枝杆菌的生存能力
Stefania Berton,Lu Chen,Yi Chu Liang et al.
Stefania Berton et al.
Metal-dependent protein phosphatases (PPMs) have essential roles in a variety of cellular processes, including inflammation, proliferation, differentiation, and stress responses, which are intensively investigated in cancer and metabolic di...
Suzanne G Mays,Emma H D&#x;Agostino,Autumn R Flynn et al.
Suzanne G Mays et al.
Phospholipids are ligands for nuclear hormone receptors (NRs) that regulate transcriptional programs relevant to normal physiology and disease. Here, we demonstrate that mimicking phospholipid-NR interactions is a robust strategy to improve...
Adam I Green,George M Burslem
Adam I Green
Preventing uncontrolled gene expression is a powerful therapeutic strategy for the treatment of cancers. In this issue of Cell Chemical Biology, Xu et al. (2022) describe a series of proteolysis targeting chimeras that induce the degradatio...
Sarah M Chang,Matthew G Vander Heiden
Sarah M Chang
In this issue of Cell Chemical Biology, Olszewski et al. (2022) address the challenge of developing small molecules to inhibit glucose uptake in cancer. They characterize a novel pan-GLUT inhibitor that suppresses tumor growth and uncover h...
Mishtu Dey
Mishtu Dey
Resolving the deceptive isoform and complex selectivity of HDAC1/2 inhibitors [0.03%]
表观遗传药物HDAC1/2抑制剂的欺骗性异构体及复杂选择性解析
N Connor Payne,Ralph Mazitschek
N Connor Payne
The histone deacetylase paralogs HDAC1/2/3 and their corepressor complexes serve as epigenetic master regulators of chromatin function. Over the past decades, HDACs have been widely pursued as pharmacological targets, and considerable effor...
Yanghao Zhong,Xin Zhou,Kun-Liang Guan et al.
Yanghao Zhong et al.
The small GTPase Ras homolog enriched in brain (Rheb) plays a critical role in activating the mechanistic target of rapamycin complex 1 (mTORC1), a signaling hub that regulates various cellular functions. We recently observed nuclear mTORC1...