Discovery and Development of TMPRSS6 Inhibitors Modulating Hepcidin Levels in Human Hepatocytes [0.03%]
discovery和开发调节人肝细胞hepcidin水平的tmprrs6抑制剂
François Béliveau,Aarti Tarkar,Sébastien P Dion et al.
François Béliveau et al.
Iron overload disorders are characterized by the body's inability to regulate iron absorption and its storage which can lead to organ failures. Accumulated evidence has revealed that hepcidin, the master regulator of iron homeostasis, is ne...
Design on a Rational Basis of High-Affinity Peptides Inhibiting the Histone Chaperone ASF1 [0.03%]
基于理性的高亲和力组蛋白伴侣ASF1抑制肽的设计
May Bakail,Albane Gaubert,Jessica Andreani et al.
May Bakail et al.
Anti-silencing function 1 (ASF1) is a conserved H3-H4 histone chaperone involved in histone dynamics during replication, transcription, and DNA repair. Overexpressed in proliferating tissues including many tumors, ASF1 has emerged as a prom...
Dimiter S Dimitrov
Dimiter S Dimitrov
In this issue of Cell Chemical Biology, Hwang et al. (2019) describe a rapid, one-step, one-pot, and enzyme-free assembly strategy under mild conditions for site-specific conjugation of small molecules to antibodies. This is a promising pla...
William P Katt,Michael J Lukey,Richard A Cerione
William P Katt
Increased consumption of glucose and glutamine are metabolic hallmarks of tumorigenesis. In this issue of Cell Chemical Biology, Reckzeh et al. (2019) describe the discovery of Glutor, a potent inhibitor of cellular glucose uptake. Combinin...
How Sweet It Is: Small-Molecule Inhibitors of mTORC1 Glucose Sensing [0.03%]
天赐甘甜：mTORC1葡萄糖感受的小分子抑制剂
Junbing Zhang,Liron Bar-Peled
Junbing Zhang
In this issue of Cell Chemical Biology, Kang et al. (2019) describe the use of a high-throughput cell-based screen to identify chemical scaffolds that selectively inhibit mTORC1 nutrient sensing. Chemical proteomic-based target identificati...
A Targeted Protein Degradation Cell-Based Screening for Nanobodies Selective toward the Cellular RHOB GTP-Bound Conformation [0.03%]
一种靶向蛋白降解的细胞基于筛选体系用于特异性识别RHOB GTP结合构象的纳米抗体
Nicolas Bery,Laura Keller,Marjorie Soulié et al.
Nicolas Bery et al.
The selective downregulation of activated intracellular proteins is a key challenge in cell biology. RHO small GTPases switch between a guanosine diphosphate (GDP)-bound and a guanosine triphosphate (GTP)-bound state that drives downstream ...
Chemogenomic Analysis of the Druggable Kinome and Its Application to Repositioning and Lead Identification Studies [0.03%]
基于药物基因组学的可成药激酶组分析及其在药物再定位和苗头化合物发现研究中的应用
Balaguru Ravikumar,Sanna Timonen,Zaid Alam et al.
Balaguru Ravikumar et al.
Owing to the intrinsic polypharmacological nature of most small-molecule kinase inhibitors, there is a need for computational models that enable systematic exploration of the chemogenomic landscape underlying druggable kinome toward more ef...
Jennifer Chu,Wenhan Zhang,Regina Cencic et al.
Jennifer Chu et al.
Rocaglates share a common cyclopenta[b]benzofuran core that inhibits eukaryotic translation initiation by modifying the behavior of the RNA helicase, eIF4A. Working as interfacial inhibitors, rocaglates stabilize the association between eIF...
Light Regulation of Enzyme Allostery through Photo-responsive Unnatural Amino Acids [0.03%]
光敏非天然氨基酸介导的光调控酶变构效应
Andrea C Kneuttinger,Kristina Straub,Philipp Bittner et al.
Andrea C Kneuttinger et al.
Imidazole glycerol phosphate synthase (ImGPS) is an allosteric bienzyme complex in which substrate binding to the synthase subunit HisF stimulates the glutaminase subunit HisH. To control this stimulation with light, we have incorporated th...
Formation of the Alarmones Diadenosine Triphosphate and Tetraphosphate by Ubiquitin- and Ubiquitin-like-Activating Enzymes [0.03%]
泛素和泛素样活化酶形成报警信号二腺苷三磷酸和四磷酸
Kathrin H Götz,Martin Mex,Katrin Stuber et al.
Kathrin H Götz et al.
Diadenosine polyphosphates (ApnAs) such as diadenosine tri- and tetraphosphates are formed in prokaryotic as well as eukaryotic cells. Since upon stress intracellular ApnA concentrations increase, it was postulated that ApnAs are alarmones ...