[HTML][HTML] Why 90% of clinical drug development fails and how to improve it?

D Sun, W Gao, H Hu, S Zhou - Acta Pharmaceutica Sinica B, 2022 - Elsevier
Ninety percent of clinical drug development fails despite implementation of many successful
strategies, which raised the question whether certain aspects in target validation and drug …

Translating biased agonists from molecules to medications: Serotonin 5-HT1A receptor functional selectivity for CNS disorders

A Newman-Tancredi, RY Depoortère… - Pharmacology & …, 2022 - Elsevier
Biased agonism (or “functional selectivity”) at G-protein-coupled receptors has attracted
rapidly increasing interest as a means to improve discovery of more efficacious and safer …

Engineered biological neural networks on high density CMOS microelectrode arrays

J Duru, J Küchler, SJ Ihle, C Forró, A Bernardi… - Frontiers in …, 2022 - frontiersin.org
In bottom-up neuroscience, questions on neural information processing are addressed by
engineering small but reproducible biological neural networks of defined network topology …

[HTML][HTML] Recent advances of PROTACs technology in neurodegenerative diseases

C Wang, Y Zhang, S Yang, D Xing - Arabian Journal of Chemistry, 2023 - Elsevier
Neurodegenerative diseases, like Alzheimer's disease, Huntington's disease, Parkinson's
disease, progressive supranuclear palsy, and frontotemporal dementia are among the …

CNSMolGen: A Bidirectional Recurrent Neural Network-Based Generative Model for De Novo Central Nervous System Drug Design

R Gou, J Yang, M Guo, Y Chen… - Journal of Chemical …, 2024 - ACS Publications
Central nervous system (CNS) drugs have had a significant impact on treating a wide range
of neurodegenerative and psychiatric disorders. In recent years, deep learning-based …

[HTML][HTML] Structure‒tissue exposure/selectivity relationship (STR) correlates with clinical efficacy/safety

W Gao, H Hu, L Dai, M He, H Yuan, H Zhang… - … Pharmaceutica Sinica B, 2022 - Elsevier
Drug optimization, which improves drug potency/specificity by structure‒activity relationship
(SAR) and drug-like properties, is rigorously performed to select drug candidates for clinical …

[HTML][HTML] Submitted for the special issue:“The multifaceted activities of nervous and non-nervous neuronal nicotinic acetylcholine receptors in physiology and pathology …

P Sinclair, N Kabbani - Pharmacological Research, 2023 - Elsevier
Nicotinic acetylcholine receptors (nAChRs) belong to a superfamily of cys-loop receptors
characterized by the assembly of five subunits into a multi-protein channel complex. Ligand …

Automated assays to identify modulators of transcription factor EB translocation and autophagy

A da Costa, C Picoli, F Mouthon… - ASSAY and Drug …, 2022 - liebertpub.com
Autophagy is a process leading to the degradation of cellular material, in organelles called
lysosomes, to supply energy or generate building blocks for the synthesis of new materials …

Use of real‐world evidence in translational pharmacology research

M Charvériat, SJ Darmoni, V Lafon… - Fundamental & …, 2022 - Wiley Online Library
Real‐world evidence (RWE) refers to observational data gathered outside the formalism of
randomized controlled trials, in real life situations, on marketed drugs. While clinical trials …

Multimodal MRI Analysis of Brain Metabolism in Maintenance Hemodialysis Patients Based on Cognitive Computing

Y Zhang, H Ma, X Lv, Q Han - Journal of Healthcare …, 2021 - Wiley Online Library
This paper investigates cognitive computation of brain metabolism in maintenance
hemodialysis patients with multimodal MRI therapy assessment. This paper constructs a …