Fluorescence activation mechanism and imaging of drug permeation with new sensors for smoking-cessation ligands

Autor: Aaron L Nichols, Zack Blumenfeld, Chengcheng Fan, Laura Luebbert, Annet EM Blom, Bruce N Cohen, Jonathan S Marvin, Philip M Borden, Charlene H Kim, Anand K Muthusamy, Amol V Shivange, Hailey J Knox, Hugo Rego Campello, Jonathan H Wang, Dennis A Dougherty, Loren L Looger, Timothy Gallagher, Douglas C Rees, Henry A Lester

Publikováno v: eLife, Vol 11 (2022)

Nicotinic partial agonists provide an accepted aid for smoking cessation and thus contribute to decreasing tobacco-related disease. Improved drugs constitute a continued area of study. However, there remains no reductionist method to examine the cell

Externí odkaz: https://doaj.org/article/4b4e86491b454335b0724b76381431a8

Characterization of Binding Site Interactions and Selectivity Principles in the α3β4 Nicotinic Acetylcholine Receptor

Autor: Hailey J. Knox, Hugo Rego Campello, Henry A. Lester, Timothy Gallagher, Dennis A. Dougherty

Publikováno v: Journal of the American Chemical Society. 144(35)

Nicotinic acetylcholine receptors (nAChRs) play an important role in neurotransmission and are also involved in addiction and several disease states. There is significant interest in therapeutic targeting of nAChRs; however, achieving selectivity for

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9d2093e3427e6a8fcb92fbecf1c279c3
https://pubmed.ncbi.nlm.nih.gov/36006801

Author response: Fluorescence activation mechanism and imaging of drug permeation with new sensors for smoking-cessation ligands

Autor: Laura Luebbert, Chengcheng Fan, Zack Blumenfeld, Aaron L Nichols, Annet EM Blom, Bruce N Cohen, Jonathan S Marvin, Philip M Borden, Charlene H Kim, Anand K Muthusamy, Amol V Shivange, Hailey J Knox, Hugo Rego Campello, Jonathan H Wang, Dennis A Dougherty, Loren L Looger, Timothy Gallagher, Douglas C Rees, Henry A Lester

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::6ba6d7547914bb271a0936a614e02ac3
https://doi.org/10.7554/elife.74648.sa2

Iridium-Catalysed C–H Borylation of 2-Pyridones; Bisfunctionalisation of CC4

Autor: Aurélien Honraedt, Hugo Rego Campello, Timothy Gallagher, Cecilia Gotti, Worawat Niwetmarin

Publikováno v: Honraedt, A, Niwetmarin, W, Gotti, C, Campello, H R & Gallagher, T 2018, ' Iridium-Catalysed C-H Borylation of 2-Pyridones; Bisfunctionalisation of CC4 ', Synthesis (Germany), vol. 50, no. 17, ss-2018-t0235-op, pp. 3420-3429 . https://doi.org/10.1055/s-0036-1591594

The high regioselectivity associated with the iridium-catalysed borylation of pyridones has been exploited to provide a very direct and efficient entry to C(10) doubly substituted CC4 variants of cytisine. Two approaches have been evaluated based on

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cd777a514c5ee25539184b8f1ca079b3
https://doi.org/10.1055/s-0036-1591594

Identification of the Initial Steps in Signal Transduction in the α4β2 Nicotinic Receptor:Insights from Equilibrium and Nonequilibrium Simulations

Autor: Timothy Gallagher, Susan Wonnacott, A. Sofia F. Oliveira, Hugo Rego Campello, Richard B. Sessions, Adrian J. Mulholland, Deborah K. Shoemark

Publikováno v: Oliveira, A S F, Shoemark, D K, Campello, H R, Wonnacott, S, Gallagher, T, Sessions, R B & Mulholland, A J 2019, ' Identification of the Initial Steps in Signal Transduction in the α4β2 Nicotinic Receptor : Insights from Equilibrium and Nonequilibrium Simulations ', Structure, vol. 27, no. 7, pp. 1171-1183.e3 . https://doi.org/10.1016/j.str.2019.04.008

Summary Nicotinic acetylcholine receptors (nAChRs) modulate synaptic transmission in the nervous system. These receptors have emerged as therapeutic targets in drug discovery for treating several conditions, including Alzheimer's disease, pain, and n

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9d362a4545aa1e939eccb1ff767a433e
https://hdl.handle.net/1983/f964cae0-6415-4233-9e61-653d656538bb