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Page 1
Inside-out neuropharmacology of nicotinic drugs.
Henderson BJ, Lester HA. Henderson BJ, et al. Among authors: lester ha. Neuropharmacology. 2015 Sep;96(Pt B):178-93. doi: 10.1016/j.neuropharm.2015.01.022. Epub 2015 Feb 4. Neuropharmacology. 2015. PMID: 25660637 Free PMC article. Review.
Because these processes depend on pharmacological chaperoning within intracellular organelles, we group them as "inside-out pharmacology". ...This article is part of the Special Issue entitled 'The Nicotinic Acetylcholine Receptor: From Molecular Biology to Cognitio …
Because these processes depend on pharmacological chaperoning within intracellular organelles, we group them as "inside-out pharmacol …
Pharmacological chaperoning of nAChRs: a therapeutic target for Parkinson's disease.
Srinivasan R, Henderson BJ, Lester HA, Richards CI. Srinivasan R, et al. Among authors: lester ha. Pharmacol Res. 2014 May;83:20-9. doi: 10.1016/j.phrs.2014.02.005. Epub 2014 Mar 1. Pharmacol Res. 2014. PMID: 24593907 Free PMC article. Review.
Chaperoning-induced changes in cell physiology exert an overall inhibitory effect on the ER stress/unfolded protein response. Cell autonomous factors such as the repertoire of nAChR subtypes expressed by neurons and the pharmacological properties of nicotinic ligands (full
Chaperoning-induced changes in cell physiology exert an overall inhibitory effect on the ER stress/unfolded protein response. Cell au
Nicotine is a selective pharmacological chaperone of acetylcholine receptor number and stoichiometry. Implications for drug discovery.
Lester HA, Xiao C, Srinivasan R, Son CD, Miwa J, Pantoja R, Banghart MR, Dougherty DA, Goate AM, Wang JC. Lester HA, et al. AAPS J. 2009 Mar;11(1):167-77. doi: 10.1208/s12248-009-9090-7. Epub 2009 Mar 12. AAPS J. 2009. PMID: 19280351 Free PMC article. Review.
If the hypothesis is proven, (1) SePhaChARNS is the molecular mechanism of the first step in neuroadaptation to chronic nicotine; and (2) nicotine addiction is partially a disease of excessive chaperoning. The chaperone is a pharmacological one, nicotine; and …
If the hypothesis is proven, (1) SePhaChARNS is the molecular mechanism of the first step in neuroadaptation to chronic nicotine; and …
Psychiatric drugs bind to classical targets within early exocytotic pathways: therapeutic effects.
Lester HA, Miwa JM, Srinivasan R. Lester HA, et al. Biol Psychiatry. 2012 Dec 1;72(11):907-15. doi: 10.1016/j.biopsych.2012.05.020. Epub 2012 Jul 6. Biol Psychiatry. 2012. PMID: 22771239 Free PMC article. Review.
Consequences of such binding may include pharmacological chaperoning: the nascent drug targets are stabilized against degradation and can therefore exit the ER more readily. ...In contrast, the antidepressant effects of ketamine and other N-methyl-D-aspartate receptor liga …
Consequences of such binding may include pharmacological chaperoning: the nascent drug targets are stabilized against degradation and …
Pharmacological chaperoning of nicotinic acetylcholine receptors reduces the endoplasmic reticulum stress response.
Srinivasan R, Richards CI, Xiao C, Rhee D, Pantoja R, Dougherty DA, Miwa JM, Lester HA. Srinivasan R, et al. Among authors: lester ha. Mol Pharmacol. 2012 Jun;81(6):759-69. doi: 10.1124/mol.112.077792. Epub 2012 Feb 29. Mol Pharmacol. 2012. PMID: 22379121 Free PMC article.
We report the first observation that endoplasmic reticulum (ER) stress and the unfolded protein response (UPR) can decrease when a central nervous system drug acts as an intracellular pharmacological chaperone for its classic receptor. Transient expression of alpha4beta2 n …
We report the first observation that endoplasmic reticulum (ER) stress and the unfolded protein response (UPR) can decrease when a central n …
Nicotine up-regulates alpha4beta2 nicotinic receptors and ER exit sites via stoichiometry-dependent chaperoning.
Srinivasan R, Pantoja R, Moss FJ, Mackey ED, Son CD, Miwa J, Lester HA. Srinivasan R, et al. Among authors: lester ha. J Gen Physiol. 2011 Jan;137(1):59-79. doi: 10.1085/jgp.201010532. J Gen Physiol. 2011. PMID: 21187334 Free PMC article.
The experimental data are simulated with a model incorporating two mechanisms: (1) nicotine acts as a stabilizing pharmacological chaperone for nascent alpha4beta2 nAChRs in the ER, eventually increasing PM receptors despite a bottleneck(s) in ER export; and (2) removal of …
The experimental data are simulated with a model incorporating two mechanisms: (1) nicotine acts as a stabilizing pharmacological chapero
Human α6β4 Nicotinic Acetylcholine Receptor: Heterologous Expression and Agonist Behavior Provide Insights into the Immediate Binding Site.
Maldifassi MC, Rego Campello H, Gallagher T, Lester HA, Dougherty DA. Maldifassi MC, et al. Among authors: lester ha. Mol Pharmacol. 2023 Jun;103(6):339-347. doi: 10.1124/molpharm.123.000672. Epub 2023 Mar 31. Mol Pharmacol. 2023. PMID: 37001996
In 2020, Knowland and collaborators identified BARP (beta-anchoring and regulatory protein), a previously known voltage-gated calcium channel suppressor, as a novel human alpha6beta4 chaperone. Here, we establish that co-expression of human BARP with human alpha6beta4 in X …
In 2020, Knowland and collaborators identified BARP (beta-anchoring and regulatory protein), a previously known voltage-gated calcium channe …
Nicotine exploits a COPI-mediated process for chaperone-mediated up-regulation of its receptors.
Henderson BJ, Srinivasan R, Nichols WA, Dilworth CN, Gutierrez DF, Mackey ED, McKinney S, Drenan RM, Richards CI, Lester HA. Henderson BJ, et al. Among authors: lester ha. J Gen Physiol. 2014 Jan;143(1):51-66. doi: 10.1085/jgp.201311102. J Gen Physiol. 2014. PMID: 24378908 Free PMC article.
The discovery that nicotine exploits a COPI-dependent process to chaperone high sensitivity nAChRs is novel and suggests that this may be a common mechanism in the up-regulation of nAChRs in response to chronic nicotine....
The discovery that nicotine exploits a COPI-dependent process to chaperone high sensitivity nAChRs is novel and suggests that this ma …
Smoking-Relevant Nicotine Concentration Attenuates the Unfolded Protein Response in Dopaminergic Neurons.
Srinivasan R, Henley BM, Henderson BJ, Indersmitten T, Cohen BN, Kim CH, McKinney S, Deshpande P, Xiao C, Lester HA. Srinivasan R, et al. Among authors: lester ha. J Neurosci. 2016 Jan 6;36(1):65-79. doi: 10.1523/JNEUROSCI.2126-15.2016. J Neurosci. 2016. PMID: 26740650 Free PMC article.
Thus, nicotine, at a concentration too low to activate an appreciable fraction of plasma membrane nAChRs, induces two sequelae of pharmacological chaperoning in the ER: UPR suppression and nAChR upregulation. Therefore, one mechanism of neuroprotection by nicotine is pharm …
Thus, nicotine, at a concentration too low to activate an appreciable fraction of plasma membrane nAChRs, induces two sequelae of pharmacolo …
Determining the pharmacokinetics of nicotinic drugs in the endoplasmic reticulum using biosensors.
Shivange AV, Borden PM, Muthusamy AK, Nichols AL, Bera K, Bao H, Bishara I, Jeon J, Mulcahy MJ, Cohen B, O'Riordan SL, Kim C, Dougherty DA, Chapman ER, Marvin JS, Looger LL, Lester HA. Shivange AV, et al. Among authors: lester ha. J Gen Physiol. 2019 Jun 3;151(6):738-757. doi: 10.1085/jgp.201812201. Epub 2019 Feb 4. J Gen Physiol. 2019. PMID: 30718376 Free PMC article.
In the ER, the inside-out pathway begins when nicotine becomes a stabilizing pharmacological chaperone for some nAChR subtypes, even at concentrations as low as 10 nM. Such concentrations would persist during the 12 h of a typical smoker's day, continually activating the i …
In the ER, the inside-out pathway begins when nicotine becomes a stabilizing pharmacological chaperone for some nAChR subtypes, even …
12 results