Design, synthesis and antitumor activity of pentacyclic triterpenoid Asiatic acid derivatives as Sp1 inhibitors [0.03%]
五环三萜酸 asiatic acid 衍生物的设计、合成及其作为 SP1 抑制剂的抗肿瘤活性研究
Xue-Hao Lu,Xin-Ru Yu,Liang-Feng Zhang et al.
Xue-Hao Lu et al.
Asiatic acid (AA) was used as the lead compound and 22 inhibitors of specificity protein 1 (Sp1) were designed and synthesized with modification at A ring and C-28 position of AA, whose structures were confirmed by HRMS, 1H NMR and 13C NMR....
Structure activity relationship exploration of imidazo[1,2-a]pyridine series to reverse isoform selectivity and identify potent SIK1 selective inhibitors [0.03%]
用于逆转异构体选择性并鉴定有效的SIK1选择性抑制剂的咪唑并吡啶系列结构活性关系研究
Christophe Peixoto,Elsa De Lemos,Laëtitia Cherel et al.
Christophe Peixoto et al.
The salt-inducible kinase (SIK) family encompasses three isoforms, SIK1, SIK2, and SIK3, which are members of the AMP-activated protein kinase (AMPK) family of serine/threonine protein kinases. SIK inhibition has emerged as a potential ther...
Andrew Gutierrez,Jason Archdeacon,Brian S J Blagg
Andrew Gutierrez
The mitochondrial Hsp90 isoform, Tumor Necrosis Factor Receptor Associated Protein 1 (TRAP1), is central to the pathogenesis of disease states that include cancer, ischemic retinopathy, and diabetic kidney disease among others. TRAP1 contri...
Rational design and translational advancement of phospholipid-based nanocarriers for targeted cancer therapy [0.03%]
基于合理设计的靶向癌症治疗的磷脂基纳米载体的转化研究进展
Kateryna Mykhailivna Doroshenko,Oleksander Ivanovich Shefchenko
Kateryna Mykhailivna Doroshenko
Phospholipid-derived nanocarriers represent a versatile and chemically customizable class of drug delivery systems that self-assemble into bilayered vesicles due to their intrinsic amphiphilicity. These systems can encapsulate both hydrophi...
A concise review on MDM2 inhibitors and recent progress in radiopharmaceutical development for imaging MDM2 expression in tumors with PET or SPECT [0.03%]
MDM2抑制剂的简要综述及利用正电子发射断层成像或单光子发射计算机断层扫描技术开发放射性药物以检测肿瘤中MDM2表达的最新研究进展
Atchimnaidu Siriki,Graham Ragland,Janardhan Vasireddy et al.
Atchimnaidu Siriki et al.
Murine double minute 2 (MDM2, also known as human double minute 2 or HDM2) is a negative regulator of the tumor suppressor protein p53 and is overexpressed in many cancers. Over the past two decades, substantial progress has been made in de...
Targeting virulence to disarm the pathogen: Enzyme-activated-substrate inhibition of Anthrax edema factor [0.03%]
针对致病性来解除病原体：汉他水肿因子的酶活底物抑制法
Seongjin Kim,Lynne Cregar-Hernandez,Mahtab Moayeri et al.
Seongjin Kim et al.
Since the discovery by Fleming that a mold could inhibit the growth of bacteria, each new antibiotic developed to treat infections quickly lost its efficacy due to the emergence of resistant strains. As a result, the ongoing threat by antib...
Discovery of A20 with 4-(2-methoxyphenyl)-1H-pyrazole scaffold as a potent and selective ROCK2 inhibitor [0.03%]
新型ROCK2选择性抑制剂A20及其类似物的发现与研究
Junzheng Wang,Bin Peng,Guodong Liang et al.
Junzheng Wang et al.
Rho-associated protein kinase 2 (ROCK2) has become a promising therapeutic target for diseases such as neurological disorders and fibrosis. In this study, structural optimization based on the binding mode of lead compound M214 and ROCK2 was...
Design, synthesis and evaluation of clickable photoaffinity probes for nuclear lamins [0.03%]
核纤层的设计、合成与可点击的光亲和探针的评估
Julia Warren,Jian Wang,Bingbing X Li et al.
Julia Warren et al.
Nuclear lamins are type V intermediate filament proteins to support the mechanical stability of mammalian cell nucleus. They also participate in various signaling activities in the cells. We recently discovered substituted pyrroloquinazolin...
Synthesis and evaluation of acyl-AMP phosphate isosteres as inhibitors of fungal acetyl CoA synthetase [0.03%]
氨基甲酸磷酸类似物的合成与评估作为真菌乙酰辅酶A合成酶的抑制剂
Drashti G Daraji,Andrew J Jezewski,Katy M Alden et al.
Drashti G Daraji et al.
Acetyl-CoA synthetase (ACS) is a member of the adenylate-forming enzymes superfamily. This enzyme plays a crucial role in cellular metabolism. While ACS enzymes are non-essential in mammals, they are essential in some fungal species and par...
Tunable spontaneous release of a carboxylic acid via a β-eliminative cleavable linker [0.03%]
通过β消解可裂解连接物调节羧酸的自发释放
Brenno Masina,Nicola R F Knowles,Ronald T Raines
Brenno Masina
Self-cleavable linkers offer controlled payload release without the need for external stimuli, making them valuable for applications in chemical biology and clinical settings. In this work, we expand the scope of the β-eliminative cleavabl...