Results 101 to 110 of about 522,701 (266)

Structure-guided design and optimization of small molecules targeting the protein-protein interaction between the von hippel-lindau (VHL) E3 ubiquitin ligase and the hypoxia inducible factor (HIF) alpha subunit with in vitro nanomolar affinities [PDF]

, 2014
E3 ubiquitin ligases are attractive targets in the ubiquitin-proteasome system, however, the development of small-molecule ligands has been rewarded with limited success.
Adams J., Alessio Ciulli, Bochevarov A. D., Buckley D. L., Buckley D. L., Buckley D. L., Bunnage M. E., Carles Galdeano, Ciechanover A., Cohen P., David M. Dias, Demo S. D., Dias D. M., Hon W. C., Inge Van Molle, Ipek Birced, Louie R. J., Manalo D. J., Morgan S. Gadd, Muchnik E., Nalepa G., Pedro Soares, Pellecchia M., Rabinowitz M. H., Rentsch A., Salvatore Scaffidi, Sarah Hewitt, Semenza G.L., Tetko I. V., Van Molle I., Wells J. A., Zhang W.   +31 more
core   +5 more sources

Mutant NPM1 in Acute Myeloid Leukemia Initiation and Maintenance

Aging and Cancer, EarlyView.
NPM1 mutations drive acute myeloid leukemia by acting as neomorphic transcriptional regulators that cooperate with Menin–MLL and XPO1 to sustain HOX/MEIS1 expression and block differentiation. Targeting these mutant‐specific transcriptional dependencies provides a rational therapeutic strategy for NPM1‐mutated AML.
Yanan Jiang, Zhong Fan, Runmeng Liu, Xiaotian Zhang   +3 more
wiley   +1 more source

A DNA aptamer for binding and inhibition of DNA methyltransferase 1. [PDF]

, 2019
DNA methyltransferases (DNMTs) are enzymes responsible for establishing and maintaining DNA methylation in cells. DNMT inhibition is actively pursued in cancer treatment, dominantly through the formation of irreversible covalent complexes between small ...
Adkins, Gary Brent, Duan, Yaokai, Fang, Jian, Gao, Linfeng, Jimenez, Luis A, Lee, Ju Yong, Li, Linhui, Ren, Wendan, Song, Jikui, Wang, Linlin, Wang, Yinsheng, Yin, Jiekai, Zhong, Wenwan   +12 more
core  

In‐Depth Profiling Highlights the Effect of Efgartigimod on Peripheral Innate and Adaptive Immune Cells in Myasthenia Gravis

Annals of Clinical and Translational Neurology, EarlyView.
ABSTRACT Background Myasthenia gravis (MG) is an autoimmune disorder characterized by antibody‐mediated complement activation. Efgartigimod, a neonatal Fc receptor (FcRn) antagonist, is approved for treating generalized MG (gMG). However, its modulatory effects on upstream innate and adaptive immune cells remain largely unexplored.
Lei Jin, Liu Dong, Ying Wang, Dingxian He, Chong Yan, Jianying Xi, Haoqin Jiang, Yu Shi, Ming Guan, Chongbo Zhao, Jie Song, Sushan Luo   +11 more
wiley   +1 more source

Enabling target-aware molecule generation to follow multi objectives with Pareto MCTS

Communications Biology
Target-aware drug discovery has greatly accelerated the drug discovery process to design small-molecule ligands with high binding affinity to disease-related protein targets.
Yaodong Yang, Guangyong Chen, Jinpeng Li, Junyou Li, Odin Zhang, Xujun Zhang, Lanqing Li, Jianye Hao, Ercheng Wang, Pheng-Ann Heng   +9 more
doaj   +1 more source

Studies and analysis of drug-target interactions by affinity chromatography and related techniques: A review

Journal of Pharmaceutical Analysis
The characterization of drug-target interactions is a key component of drug discovery, testing, and development. Affinity chromatography is one approach that can be used for this type of analysis.
David S. Hage, Sadia Sharmeen, B.K. Sajeeb, Harshana Olupathage, Md Masudur Rahman, Isaac Kyei, Samiul Alim, Nigar Sultana Pinky   +7 more
doaj   +1 more source

Neuroinflammation in GAD65 Antibody‐Associated Epilepsy Measured Using [18F]DPA‐714 PET/MRI

Annals of Clinical and Translational Neurology, EarlyView.
ABSTRACT The timing for initiating immunotherapy in patients with glutamic acid decarboxylase 65 (GAD65) antibody‐associated epilepsy is a challenge. We used the translocator protein radioligand [18F]DPA‐714 and PET to evaluate brain microglial activation.
Jingjing Chen, Yuying Zhang, Heyu Zhang, Jinming Zhang, Ningning Wang, Xintong Guo, Yicong Liu, Yue Liu, Xiangsong Zhang, Ziyi Chen, Guanzhong Ni   +10 more
wiley   +1 more source

Delivering bioactive cyclic peptides that target Hsp90 as prodrugs

Journal of Enzyme Inhibition and Medicinal Chemistry, 2019
The most challenging issue facing peptide drug development is producing a molecule with optimal physical properties while maintaining target binding affinity.
Yuantao Huo, Laura K. Buckton, Jack L. Bennett, Eloise C. Smith, Frances L. Byrne, Kyle L. Hoehn, Marwa N. Rahimi, Shelli R. McAlpine   +7 more
doaj   +1 more source

Baseline Regional Cholinergic Denervation Predicts Cognitive Trajectories in Moderate Parkinson Disease

Annals of Clinical and Translational Neurology, EarlyView.
ABSTRACT Objective Cognitive decline is a disabling and variable feature of Parkinson disease (PD). While cholinergic system degeneration is linked to cognitive impairments in PD, most prior research reported cross‐sectional associations. We aimed to fill this gap by investigating whether baseline regional cerebral vesicular acetylcholine transporter ...
Taylor Brown, Giulia Carli, Prabesh Kanel, Stiven Roytman, Jaimie Barr, Nicolaas I. Bohnen, Roger L. Albin   +6 more
wiley   +1 more source

Ofatumumab in Myelin Oligodendrocyte Glycoprotein Antibody–Associated Disease: A Comparison With Rituximab

Annals of Clinical and Translational Neurology, EarlyView.
ABSTRACT Objective To evaluate the efficacy and safety of ofatumumab in patients with myelin oligodendrocyte glycoprotein antibody–associated disease (MOGAD), and compare it with rituximab. Methods We conducted a single–center, observational study including 22 MOGAD patients treated with ofatumumab and 21 treated with rituximab.
Yuxin Fan, Lei Zhou, Jingzi ZhangBao, Hongmei Tan, Zhouzhou Wang, Chao Quan   +5 more
wiley   +1 more source