Comprehensive review of mechanisms of pathogenesis involved in Alzheimer's disease and potential therapeutic strategies

P Sharma, P Srivastava, A Seth, PN Tripathi… - Progress in …, 2019 - Elsevier
AD is a progressive neurodegenerative disorder and a leading cause of dementia in an
aging population worldwide. The enormous challenge which AD possesses to global …

New evolutions in the BACE1 inhibitor field from 2014 to 2018

CC Hsiao, F Rombouts, HJM Gijsen - Bioorganic & medicinal chemistry …, 2019 - Elsevier
Abstract β-Site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors offer the
potential of disease-modifying treatment for Alzheimer's disease (AD). Since 2014, major …

Small-molecule BACE1 inhibitors: a patent literature review (2011 to 2020)

F Rombouts, K Kusakabe, CC Hsiao… - Expert Opinion on …, 2021 - Taylor & Francis
Introduction Inhibition of β-site amyloid precursor protein cleaving enzyme 1 (BACE1) has
been extensively pursued as potential disease-modifying treatment for Alzheimer's disease …

Alzheimer's disease and β-secretase inhibition: an update with a focus on computer-aided inhibitor design

SC Ugbaja, IA Lawal, HM Kumalo… - Current drug …, 2022 - ingentaconnect.com
Introduction: Alzheimer's disease (AD) is an intensifying neurodegenerative illness due to its
irreversible nature. Identification of β128; site Amyloid Precursor Protein (APP) cleaving en …

Toward β-secretase-1 inhibitors with improved isoform selectivity

P Johansson, K Kaspersson, IK Gurrell… - Journal of Medicinal …, 2018 - ACS Publications
BACE1 is responsible for the first step in APP proteolysis, leading to toxic Aβ production, and
has been indicated to play a key role in the pathogenesis of Alzheimer's disease. The …

Exploiting structural dynamics to design open-flap inhibitors of malarial aspartic proteases

R Bobrovs, K Jaudzems… - Journal of Medicinal …, 2019 - ACS Publications
Malaria is a life-threatening infectious disease caused by Plasmodium parasites.
Plasmepsins (proteolytic enzymes of the parasite) have been considered as promising …

Prospecting and structural insight into the binding of novel plant-derived molecules of Leea indica as inhibitors of BACE1

SMZ Hosen, M Rubayed, R Dash… - Current …, 2018 - ingentaconnect.com
Background: Alzheimer disease (AD) can be considered as the most common age related
neurodegenerative disorder and also an important cause of death in elderly patients. A …

Pepsin-like aspartic proteases (PAPs) as model systems for combining biomolecular simulation with biophysical experiments

S Bhakat - RSC advances, 2021 - pubs.rsc.org
Pepsin-like aspartic proteases (PAPs) are a class of aspartic proteases which shares
tremendous structural similarity with human pepsin. One of the key structural features of …

Flap dynamics in pepsin-like aspartic proteases: a computational perspective using Plasmepsin-II and BACE-1 as model systems

S Bhakat, P Soderhjelm - Journal of Chemical Information and …, 2022 - ACS Publications
The flexibility of β hairpin structure known as the flap plays a key role in catalytic activity and
substrate intake in pepsin-like aspartic proteases. Most of these enzymes share structural …

Understanding the Hsp90 N-Terminal Dynamics: Structural and Molecular Insights into the Therapeutic Activities of Anticancer Inhibitors Radicicol (RD) and Radicicol …

AM Magwenyane, NN Mhlongo, MM Lawal… - Molecules, 2020 - mdpi.com
Heat shock protein 90 (Hsp90) is a crucial component in carcinogenesis and serves as a
molecular chaperone that facilitates protein maturation whilst protecting cells against …