Targeted elimination of mutated mitochondrial DNA by a multi-functional conjugate capable of sequence-specific adenine alkylation [0.03%]
一种多功能缀合物通过特异性腺嘌呤烷基化靶向清除突变线粒体DNA
Takuya Hidaka,Kaori Hashiya,Toshikazu Bando et al.
Takuya Hidaka et al.
Mutations in mitochondrial DNA (mtDNA) cause mitochondrial diseases, characterized by abnormal mitochondrial function. Although eliminating mutated mtDNA has potential to cure mitochondrial diseases, no chemical-based drugs in clinical tria...
Algal p-coumaric acid induces oxidative stress and siderophore biosynthesis in the bacterial symbiont Phaeobacter inhibens [0.03%]
藻类对羟基苯甲酸诱导细菌内共生体产氧胁迫和色氨酸下游代谢产物铁载体类水杨酸的生物合成
Rurun Wang,Étienne Gallant,Maxwell Z Wilson et al.
Rurun Wang et al.
The marine alpha-proteobacterium Phaeobacter inhibens engages in intermittent symbioses with microalgae. The symbiosis is biphasic and concludes in a parasitic phase, during which the bacteria release algaecidal metabolites in response to a...
Stuck on UUUU: New splicing inhibitors enhance U2AF2-RNA binding [0.03%]
UUUU受阻：新的剪接抑制剂可增强U2AF2与RNA的结合
Sierra L Love,Aaron A Hoskins
Sierra L Love
In this issue of Cell Chemical Biology, Chatrikhi et al. (2021) identify a small molecule that enhances U2AF2 association with RNA to block pre-mRNA splicing during early stages of spliceosome assembly. This provides a mechanism of splicing...
TPC2 targeting evolution: Leveraging therapeutic opportunities for cancer [0.03%]
靶向TP53通路的癌症治疗：机遇与挑战
Abeer F Alharbi,John Parrington
Abeer F Alharbi
Growing evidence implicates a vital role for TPC2/Ca2+ signaling in pathophysiological processes attributed to cancer, raising questions regarding the utility of TPC2 as a cancer therapeutic target. In this issue of Cell Chemical Biology, M...
An antitubercular prodrug leaves Mycobacterium tuberculosis facing a difficult choice, poisoning or starvation? [0.03%]
抗结核药物让结核分支杆菌面临两难选择：中毒还是饥饿？
Mary Jackson
Mary Jackson
In this issue of Cell Chemical Biology, Libardo et al. (2021) identify prodrugs that kill Mtb through poisoning of its L-tryptophan biosynthetic pathway. Determination of the mechanisms of resistance evolved by the bacterium highlights the ...
TREM2 is thyroid hormone regulated making the TREM2 pathway druggable with ligands for thyroid hormone receptor [0.03%]
甲状腺激素调控TREM2的表达，可以用甲状腺激素受体配体药物来治疗与TREM2相关的疾病
Skylar J Ferrara,Priya Chaudhary,Margaret J DeBell et al.
Skylar J Ferrara et al.
Triggering receptor expressed on myeloid cells-2 (TREM2) is a cell surface receptor on macrophages and microglia that senses and responds to disease-associated signals to regulate the phenotype of these innate immune cells. The TREM2 signal...
Engineered protein-small molecule conjugates empower selective enzyme inhibition [0.03%]
工程化蛋白质-小分子缀合物能够实现特异性酶抑制作用
Andrew K Lewis,Abbigael Harthorn,Sadie M Johnson et al.
Andrew K Lewis et al.
Potent, specific ligands drive precision medicine and fundamental biology. Proteins, peptides, and small molecules constitute effective ligand classes. Yet greater molecular diversity would aid the pursuit of ligands to elicit precise biolo...
Artemisinin inhibits NRas palmitoylation by targeting the protein acyltransferase ZDHHC6 [0.03%]
青蒿素通过靶向蛋白酰基转移酶ZDHHC6抑制NRAS棕榈酰化
Nan Qiu,Daniel Abegg,Mara Guidi et al.
Nan Qiu et al.
Protein S-palmitoylation is a post-translational modification that plays a crucial role in cancer cells by regulating the function and localization of oncoproteins and tumor suppressor proteins. Here, we identify artemisinin (ART), a clinic...
Ronak Tilvawala,Venkatesh V Nemmara,Archie C Reyes et al.
Ronak Tilvawala et al.
Aberrant protein citrullination is associated with many pathologies; however, the specific effects of this modification remain unknown. We have previously demonstrated that serine protease inhibitors (SERPINs) are highly citrullinated in rh...
Chemogenomics identifies acetyl-coenzyme A synthetase as a target for malaria treatment and prevention [0.03%]
化学基因组学确定乙酰辅酶A合酶是疟疾治疗和预防的目标
Robert L Summers,Charisse Flerida A Pasaje,Joao P Pisco et al.
Robert L Summers et al.
We identify the Plasmodium falciparum acetyl-coenzyme A synthetase (PfAcAS) as a druggable target, using genetic and chemical validation. In vitro evolution of resistance with two antiplasmodial drug-like compounds (MMV019721 and MMV084978)...