Applications of oxetanes in drug discovery and medicinal chemistry
G Huang, D Hucek, T Cierpicki, J Grembecka - European Journal of …, 2023 - Elsevier
The compact and versatile oxetane motifs have gained significant attention in drug discovery
and medicinal chemistry programs. This review presents an overview of the diverse …
and medicinal chemistry programs. This review presents an overview of the diverse …
Autophagy in Parkinson's disease
L Nechushtai, D Frenkel, R Pinkas-Kramarski - Biomolecules, 2023 - mdpi.com
Parkinson's disease (PD) is a devastating disease associated with accumulation of α-
synuclein (α-Syn) within dopaminergic neurons, leading to neuronal death. PD is …
synuclein (α-Syn) within dopaminergic neurons, leading to neuronal death. PD is …
Inhibition of Parkinson's disease–related LRRK2 by type I and type II kinase inhibitors: Activity and structures
M Sanz Murillo, A Villagran Suarez, V Dederer… - Science …, 2023 - science.org
Mutations in leucine-rich repeat kinase 2 (LRRK2) are a common cause of familial
Parkinson's disease (PD) and a risk factor for the sporadic form. Increased kinase activity …
Parkinson's disease (PD) and a risk factor for the sporadic form. Increased kinase activity …
Pharmacology of LRRK2 with type I and II kinase inhibitors revealed by cryo-EM
LRRK2 is one of the most promising drug targets for Parkinson's disease. Though type I
kinase inhibitors of LRRK2 are under clinical trials, alternative strategies like type II inhibitors …
kinase inhibitors of LRRK2 are under clinical trials, alternative strategies like type II inhibitors …
ScaffoldGVAE: scaffold generation and hopping of drug molecules via a variational autoencoder based on multi-view graph neural networks
In recent years, drug design has been revolutionized by the application of deep learning
techniques, and molecule generation is a crucial aspect of this transformation. However …
techniques, and molecule generation is a crucial aspect of this transformation. However …
Prospects for Disease Slowing in Parkinson Disease
E Menozzi, AHV Schapira - Annual Review of Pharmacology …, 2024 - annualreviews.org
The increasing prevalence of Parkinson disease (PD) highlights the need to develop
interventions aimed at slowing or halting its progression. As a result of sophisticated disease …
interventions aimed at slowing or halting its progression. As a result of sophisticated disease …
[HTML][HTML] Disruption of Dopamine Homeostasis Associated with Alteration of Proteins in Synaptic Vesicles: A Putative Central Mechanism of Parkinson's Disease …
X Jin, X Si, X Lei, H Liu, A Shao, L Li - Aging and Disease, 2024 - ncbi.nlm.nih.gov
Vestigial dopaminergic cells in PD have selectivity for a sub-class of hypersensitive neurons
with the nigrostriatal dopamine (DA) tract. DA is modulated in pre-synaptic nerve terminals to …
with the nigrostriatal dopamine (DA) tract. DA is modulated in pre-synaptic nerve terminals to …
Leucine‐rich repeat kinase 2 (LRRK2) inhibition upregulates microtubule‐associated protein 1B to ameliorate lysosomal dysfunction and parkinsonism
K Chen, F Tang, B Du, ZZ Yue, LL Jiao, XL Ding… - MedComm, 2023 - Wiley Online Library
Mutations in LRRK2 (encoding leucine‐rich repeat kinase 2 protein, LRRK2) are the most
common genetic risk factors for Parkinson's disease (PD), and increased LRRK2 kinase …
common genetic risk factors for Parkinson's disease (PD), and increased LRRK2 kinase …
Concurrent Optimizations of Efficacy and Blood–Brain Barrier Permeability in New Macrocyclic LRRK2 Inhibitors for Potential Parkinson's Disease Therapeutics
K Kim, A Jang, H Shin, I Ye, JE Lee, T Kim… - Journal of Medicinal …, 2024 - ACS Publications
The elevated activity of leucine-rich repeat kinase 2 (LRRK2) is implicated in the
pathogenesis of Parkinson's disease (PD). The quest for effective LRRK2 inhibitors has …
pathogenesis of Parkinson's disease (PD). The quest for effective LRRK2 inhibitors has …
Data‐driven disease progression model of Parkinson's disease and effect of sex and genetic variants
R Jin, H Yoshioka, H Sato… - CPT: Pharmacometrics & …, 2024 - Wiley Online Library
As Parkinson's disease (PD) progresses, there are multiple biomarker changes, and sex and
genetic variants may influence the rate of progression. Data‐driven, long‐term disease …
genetic variants may influence the rate of progression. Data‐driven, long‐term disease …