Current emerging therapeutic targets and clinical investigational agents for schizophrenia: challenges and opportunities

N Ye, Q Wang, Y Li, X Zhen - Medicinal Research Reviews, 2024 - Wiley Online Library
Since the first discovery of antipsychotics in the 1950s, targeting dopaminergic drugs has
manifested to well manage the positive symptoms of schizophrenia with limited efficacy for …

TAAR1 as an emerging target for the treatment of psychiatric disorders

J Liu, R Wu, JX Li - Pharmacology & Therapeutics, 2024 - Elsevier
Trace amines, a group of amines expressed at the nanomolar level in the mammalian brain,
can modulate monoamine transmission. The discovery of and the functional research on the …

AlphaFold accelerated discovery of psychotropic agonists targeting the trace amine–associated receptor 1

A Díaz-Holguín, M Saarinen, DD Vo, A Sturchio… - Science …, 2024 - science.org
Artificial intelligence is revolutionizing protein structure prediction, providing unprecedented
opportunities for drug design. To assess the potential impact on ligand discovery, we …

Engineered odorant receptors illuminate the basis of odour discrimination

CA de March, N Ma, CB Billesbølle, J Tewari… - Nature, 2024 - nature.com
How the olfactory system detects and distinguishes odorants with diverse physicochemical
properties and molecular configurations remains poorly understood. Vertebrate animals …

Structure-based design of novel G-Protein-Coupled receptor TAAR1 agonists as potential antipsychotic drug candidates

Z Zhou, W Zhang, F Zhao, Y Sun, N Wang… - Journal of Medicinal …, 2024 - ACS Publications
The existing available antipsychotics have failed to manage the cognitive impairment of
schizophrenia and induced a number of seriously undesirable effects. Trace amine …

Newly identified structures of trace-amine associated receptor-1 (TAAR1) will aid discovery of next generation neuropsychiatric drugs

PC Nair, B Shajan, T Bastiampillai - Mol Psychiatry, 2024 - nature.com
The trace-amine associated receptor-1 (TAAR1) is a member of the G-protein coupled
receptor (GPCR) receptor family and is widely distributed across the brain and …

[HTML][HTML] The versatile binding landscape of the TAAR1 pocket for LSD and other antipsychotic drug molecules

K Jiang, Y Zheng, L Zeng, L Wang, F Li, J Pu, Y Lu… - Cell Reports, 2024 - cell.com
Increasing global concerns about psychoactive substance addiction and psychotic disorders
highlight the need for comprehensive research into the structure-function relationship …

Large language models direct automated chemistry laboratory

AL Dias, T Rodrigues - 2023 - nature.com
Large language models direct automated chemistry laboratory Skip to main content Thank you
for visiting nature.com. You are using a browser version with limited support for CSS. To obtain …

Cryo-EM structure of small-molecule agonist bound delta opioid receptor-Gi complex enables discovery of biased compound

L Cheng, Z Miao, S Liu, Z Li, H Fu, C Xu, S Hu… - Nature …, 2024 - nature.com
Delta opioid receptor (δOR) plays a pivotal role in modulating human sensation and
emotion. It is an attractive target for drug discovery since, unlike Mu opioid receptor, it is …

TAAR1 agonist ulotaront delays gastric emptying of solids in patients with schizophrenia and concurrent metabolic syndrome with prediabetes

S Milanović, N Dedic, R Lew, D Burton… - Diabetes, Obesity …, 2024 - Wiley Online Library
Abstract Background Metabolic syndrome (MetS), which can be induced or exacerbated by
the current class of antipsychotic drugs, is highly prevalent in patients with schizophrenia …