Kaczor, Przemyslaw T Michałowski, Michał A Mozrzymas, Jerzy W
Published in
ACS chemical neuroscience
Cys-loop receptors are a superfamily of transmembrane, pentameric receptors that play a crucial role in mammalian CNS signaling. Physiological activation of these receptors is typically initiated by neurotransmitter binding to the orthosteric binding site, located at the extracellular domain (ECD), which leads to the opening of the channel pore (ga...
Benhamou Goldfajn, Nadav Tang, Huayuan Ding, Feng
Published in
ACS chemical neuroscience
Substoichiometric aggregation inhibition of human islet amyloid polypeptide (IAPP), the hallmark of type 2 diabetes impacting millions of people, is crucial for developing clinic therapies, yet it remains challenging given that many candidate inhibitors require high doses. Intriguingly, insulin, the key regulatory polypeptide on blood glucose level...
Singh, Gurpreet Liu, Peng Yao, Katherine R Strasser, Jessica M Hlynialuk, Chris Leinonen-Wright, Kailee Teravskis, Peter J Choquette, Jessica M Ikramuddin, Junaid Bresinsky, Merlin
...
Published in
ACS chemical neuroscience
Synaptic and cognitive deficits mediated by a severe reduction in excitatory neurotransmission caused by a disproportionate accumulation of the neuronal protein tau in dendritic spines is a fundamental mechanism that has been found repeatedly in models of tauopathies, including Alzheimer's disease, Lewy body dementia, frontotemporal dementia, and t...
Machhi, Jatin Yeapuri, Pravin Markovic, Milica Patel, Milankumar Yan, Wenhui Lu, Yaman Cohen, Jacob D Hasan, Mahmudul Abdelmoaty, Mai Mohamed Zhou, You
...
Published in
ACS chemical neuroscience
Alzheimer's disease (AD) is the most common neurodegenerative disorder. Pathologically, the disease is characterized by the deposition of amyloid beta (Aβ) plaques and the presence of neurofibrillary tangles. These drive microglia neuroinflammation and consequent neurodegeneration. While the means to affect Aβ plaque accumulation pharmacologically ...
Shi, Na Zheng, Qingchuan Zhang, Hongxing
Published in
ACS chemical neuroscience
CYP46A1 is an important potential target for the treatment of Alzheimer's disease (AD), which is the most common neurodegenerative disease among older individuals. However, the binding mechanism between CYP46A1 and substrate cholesterol (CH) has not been clarified and will not be conducive to the research of relevant drug molecules. In this study, ...
Mandal, Subhankar Kumar Br, Prashantha Alam, Md Tanjim Tripathi, Prem Prakash Channappa, Bhavya
Published in
ACS chemical neuroscience
USP30, a deubiquitinating enzyme family, forfeits the ubiquitination of E3 ligase and Parkin on the surface of mitochondria. Inhibition of USP30 results in mitophagy and cellular clearance. Herein, by understanding structural requirements, we discovered potential USP30 inhibitors from an imidazole series of ligands via a validated ubiquitin-rhodami...
Fiala, Tomas Mosharov, Eugene V. Wang, Jihang Mendieta, Adriana M. Choi, Se Joon Fialova, Eva Hwu, Christopher Sulzer, David Sames, Dalibor
Published in
ACS chemical neuroscience
Dagher, Merel Perrotta, Katie A Erwin, Sara A Hachisuka, Ayaka Iyer, Rahul Masmanidis, Sotiris C Yang, Hongyan Andrews, Anne M
Published in
ACS chemical neuroscience
Targeting neurons with light-driven opsins is widely used to investigate cell-specific responses. We transfected midbrain dopamine neurons with the excitatory opsin Chrimson. Extracellular basal and stimulated neurotransmitter levels in the dorsal striatum were measured by microdialysis in awake mice. Optical activation of dopamine cell bodies evok...
Elghazawy, Nehal H Zaafar, Dalia Hassan, Reham R Mahmoud, Mohamed Y Bedda, Loay Bakr, Alaa F Arafa, Reem K
Published in
ACS chemical neuroscience
Finding an effective anti-Alzheimer agent is quite challenging due to its multifactorial nature. As such, multitarget directed ligands (MTDLs) could be a promising paradigm for finding potential therapeutically effective new small-molecule bioactive agents against Alzheimer's disease (AD). We herein present the design, synthesis, and biological eva...
Baig, Abdul Mannan
Published in
ACS chemical neuroscience
With emerging reports of the deleterious effects of SARS-CoV-2 reflecting as neurological deficits in COVID-19, the biochemical and morphological changes it casts on the brain are also being investigated. This is an important niche of research as it is expected to predict and relate the neurological clinical features in the acute phase and chronic ...
