Proteomic Learning of Gamma-Aminobutyric Acid (GABA) Receptor-Mediated Anesthesia

Anesthetics are crucial in surgical procedures and therapeutic interventions, but they come with side effects and varying levels of effectiveness, calling for novel anesthetic agents that offer more precise and controllable effects. Targeting Gamma-aminobutyric acid (GABA) receptors, the primary inhibitory receptors in the central nervous system, could enhance their inhibitory action, potentially reducing side effects while improving the potency of anesthetics. In this study, we introduce a proteomic learning of GABA receptor-mediated anesthesia based on 24 GABA receptor subtypes by considering over 4000 proteins in protein-protein interaction (PPI) networks and over 1.5 millions known binding compounds. We develop a corresponding drug-target interaction network to identify potential lead compounds for novel anesthetic design. To ensure robust proteomic learning predictions, we curated a dataset comprising 136 targets from a pool of 980 targets within the PPI networks. We employed three machine learning algorithms, integrating advanced natural language processing (NLP) models such as pretrained transformer and autoencoder embeddings. Through a comprehensive screening process, we evaluated the side effects and repurposing potential of over 180,000 drug candidates targeting the GABRA5 receptor. Additionally, we assessed the ADMET (absorption, distribution, metabolism, excretion, and toxicity) properties of these candidates to identify those with near-optimal characteristics. This approach also involved optimizing the structures of existing anesthetics. Our work presents an innovative strategy for the development of new anesthetic drugs, optimization of anesthetic use, and deeper understanding of potential anesthesia-related side effects.

Authors

Institutions

Publication Details

Journal
Journal of Chemical Information and Modeling
Published
2025-03-17
DOI
https://doi.org/10.1021/acs.jcim.5c00114
Citations
4
Primary Topic
Computational Drug Discovery Methods
Type
article
Field-Weighted Citation Impact
6.02

Funders

Controls
|||
ALL TIME
JAN
FEB
MAR
APR
MAY
JUN
JUL
AUG
SEP
OCT
article

Proteomic Learning of Gamma-Aminobutyric Acid (GABA) Receptor-Mediated Anesthesia

Huahai Qiu, Bengong Zhang, Guo‐Wei Wei, Tianshou Zhou et al.
4 citations
Journal of Chemical Information and Modeling
Computational Drug Discovery Methods
6.02
article

Proteomic Learning of Gamma-Aminobutyric Acid (GABA) Receptor-Mediated Anesthesia

Huahai Qiu, Bengong Zhang, Guo‐Wei Wei, Tianshou Zhou, Ya-Zhou Shi, Long Chen, Jian Jiang, Yueying Zhu
article en
4 citations

Abstract

Anesthetics are crucial in surgical procedures and therapeutic interventions, but they come with side effects and varying levels of effectiveness, calling for novel anesthetic agents that offer more precise and controllable effects. Targeting Gamma-aminobutyric acid (GABA) receptors, the primary inhibitory receptors in the central nervous system, could enhance their inhibitory action, potentially reducing side effects while improving the potency of anesthetics. In this study, we introduce a proteomic learning of GABA receptor-mediated anesthesia based on 24 GABA receptor subtypes by considering over 4000 proteins in protein-protein interaction (PPI) networks and over 1.5 millions known binding compounds. We develop a corresponding drug-target interaction network to identify potential lead compounds for novel anesthetic design. To ensure robust proteomic learning predictions, we curated a dataset comprising 136 targets from a pool of 980 targets within the PPI networks. We employed three machine learning algorithms, integrating advanced natural language processing (NLP) models such as pretrained transformer and autoencoder embeddings. Through a comprehensive screening process, we evaluated the side effects and repurposing potential of over 180,000 drug candidates targeting the GABRA5 receptor. Additionally, we assessed the ADMET (absorption, distribution, metabolism, excretion, and toxicity) properties of these candidates to identify those with near-optimal characteristics. This approach also involved optimizing the structures of existing anesthetics. Our work presents an innovative strategy for the development of new anesthetic drugs, optimization of anesthetic use, and deeper understanding of potential anesthesia-related side effects.

Journal of Chemical Information and ModelingVol. 65(7)
Sun Yat-sen University (CN), Michigan United (US), Physical Sciences (United States) (US), Wuhan Textile University (CN), Toronto Metropolitan University (CA), Michigan State University (US)
National Science Foundation, National Aeronautics and Space Administration, Bristol-Myers Squibb, Pfizer, Michigan State University Foundation, National Natural Science Foundation of China, National Institute of General Medical Sciences, National Institute of Allergy and Infectious Diseases, Division of Mathematical Sciences
Openalex Percentile: Top 5%
Computational Drug Discovery Methods
6.02
AI Navigator

Ask Laika to Summarize, Analyze, and Connect papers live on the map.

Summarize Papers & Methodologies

Extract key findings, datasets, and comparative methods across publications.

Benchmark Rankings & Visual Analytics

Rank top research institutions, authors, funders, topics, and journals by Field-Weighted Citation Impact (FWCI) and paper volume with instant charts.

Connect Distant Disciplines

Bridge topological clusters on the map to find hidden collaborative intersections.