Drug discovery on natural products: from ion channels to nAChRs, from nature to libraries, from analytics to assays
RA Otvos, KBM Still, GW Somsen… - … Life Sciences R&D, 2019 - journals.sagepub.com
Natural extracts are complex mixtures that may be rich in useful bioactive compounds and
therefore are attractive sources for new leads in drug discovery. This review describes drug …
therefore are attractive sources for new leads in drug discovery. This review describes drug …
Pharmacological chaperoning of nAChRs: a therapeutic target for Parkinson's disease
Chronic exposure to nicotine results in an upregulation of neuronal nicotinic acetylcholine
receptors (nAChRs) at the cellular plasma membrane. nAChR upregulation occurs via …
receptors (nAChRs) at the cellular plasma membrane. nAChR upregulation occurs via …
[HTML][HTML] An optical neuron-astrocyte proximity assay at synaptic distance scales
Astrocytes are complex bushy cells that serve important functions through close contacts
between their processes and synapses. However, the spatial interactions and dynamics of …
between their processes and synapses. However, the spatial interactions and dynamics of …
Manipulation of subunit stoichiometry in heteromeric membrane proteins
The ability of oligomeric membrane proteins to assemble in different functional ratios of
subunits is a common feature across many systems. Recombinant expression of hetero …
subunits is a common feature across many systems. Recombinant expression of hetero …
The duplicated α7 subunits assemble and form functional nicotinic receptors with the full-length α7
Y Wang, C Xiao, T Indersmitten, R Freedman… - Journal of Biological …, 2014 - ASBMB
The α7 nicotinic acetylcholine receptor gene (CHRNA7) is linked to schizophrenia. A partial
duplication of CHRNA7 (CHRFAM7A) is found in humans on 15q13–14. Exon 6 of …
duplication of CHRNA7 (CHRFAM7A) is found in humans on 15q13–14. Exon 6 of …
Using enhanced number and brightness to measure protein oligomerization dynamics in live cells
Protein dimerization and oligomerization are essential to most cellular functions, yet
measurement of the size of these oligomers in live cells, especially when their size changes …
measurement of the size of these oligomers in live cells, especially when their size changes …
Nicotine exploits a COPI-mediated process for chaperone-mediated up-regulation of its receptors
BJ Henderson, R Srinivasan, WA Nichols… - Journal of General …, 2014 - rupress.org
Chronic exposure to nicotine up-regulates high sensitivity nicotinic acetylcholine receptors
(nAChRs) in the brain. This up-regulation partially underlies addiction and may also …
(nAChRs) in the brain. This up-regulation partially underlies addiction and may also …
FRET spectrometry: a new tool for the determination of protein quaternary structure in living cells
Förster resonance energy transfer (FRET) is an exquisitely sensitive method for detection of
molecular interactions and conformational changes in living cells. The recent advent of …
molecular interactions and conformational changes in living cells. The recent advent of …
Green apple e-cigarette flavorant farnesene triggers reward-related behavior by promoting high-sensitivity nAChRs in the ventral tegmental area
SY Cooper, AT Akers, BJ Henderson - eneuro, 2020 - eneuro.org
While combustible cigarette smoking has declined, the use of electronic nicotine delivery
systems (ENDS) has increased. ENDS are popular among adolescents, and chemical …
systems (ENDS) has increased. ENDS are popular among adolescents, and chemical …
Systemically circulating 17β-estradiol enhances the neuroprotective effect of the smoking cessation drug cytisine in female parkinsonian mice
SM Zarate, RC Garcia, G Pandey… - npj Parkinson's …, 2025 - nature.com
The smoking cessation drug cytisine exerts neuroprotection in substantia nigra pars
compacta (SNc) dopaminergic (DA) neurons of female but not male 6-hydroxydopamine (6 …
compacta (SNc) dopaminergic (DA) neurons of female but not male 6-hydroxydopamine (6 …