Discerning conformational dynamics and binding kinetics of GPCRs by < sup > 19 < /sup > F NMR
Curr Opin Pharmacol. 2023 Apr 17:102377. doi: 10.1016/j.coph.2023.102377. Online ahead of print.ABSTRACT19F NMR provides a way of monitoring conformational dynamics of G-protein coupled receptors (GPCRs) from the perspective of an ensemble. While X-ray crystallography provides exquisitely resolved high-resolution structures of specific states, it generally does not recapitulate the true ensemble of functional states. Fluorine (19F) NMR provides a highly sensitive spectroscopic window into the conformational ensemble, generally permitting the direct quantification of resolvable states. Moreover, straightforward T1- and T2-b...
Source: Current Opinion in Pharmacology - August 23, 2023 Category: Drugs & Pharmacology Authors: R S Prosser Nicolas A Alonzi Source Type: research
Illuminating GPCR signaling mechanisms by NMR spectroscopy with stable-isotope labeled receptors
Curr Opin Pharmacol. 2023 Mar 21:102364. doi: 10.1016/j.coph.2023.102364. Online ahead of print.ABSTRACTG protein-coupled receptors (GPCRs) exhibit remarkable structural plasticity, which underlies their capacity to recognize a wide range of extracellular molecules and interact with intracellular partner proteins. Nuclear magnetic resonance (NMR) spectroscopy is uniquely well-suited to investigate GPCR structural plasticity, enabled by stable-isotope "probes" incorporated into receptors that inform on structure and dynamics. Progress with stable-isotope labeling methods in Eukaryotic expression systems has enabled producti...
Source: Current Opinion in Pharmacology - August 23, 2023 Category: Drugs & Pharmacology Authors: Beining Jin Naveen Thakur Anuradha V Wijesekara Matthew T Eddy Source Type: research
Illuminating GPCR signaling mechanisms by NMR spectroscopy with stable-isotope labeled receptors
Curr Opin Pharmacol. 2023 Mar 21:102364. doi: 10.1016/j.coph.2023.102364. Online ahead of print.ABSTRACTG protein-coupled receptors (GPCRs) exhibit remarkable structural plasticity, which underlies their capacity to recognize a wide range of extracellular molecules and interact with intracellular partner proteins. Nuclear magnetic resonance (NMR) spectroscopy is uniquely well-suited to investigate GPCR structural plasticity, enabled by stable-isotope "probes" incorporated into receptors that inform on structure and dynamics. Progress with stable-isotope labeling methods in Eukaryotic expression systems has enabled producti...
Source: Current Opinion in Pharmacology - August 23, 2023 Category: Drugs & Pharmacology Authors: Beining Jin Naveen Thakur Anuradha V Wijesekara Matthew T Eddy Source Type: research
Discerning conformational dynamics and binding kinetics of GPCRs by < sup > 19 < /sup > F NMR
Curr Opin Pharmacol. 2023 Apr 17:102377. doi: 10.1016/j.coph.2023.102377. Online ahead of print.ABSTRACT19F NMR provides a way of monitoring conformational dynamics of G-protein coupled receptors (GPCRs) from the perspective of an ensemble. While X-ray crystallography provides exquisitely resolved high-resolution structures of specific states, it generally does not recapitulate the true ensemble of functional states. Fluorine (19F) NMR provides a highly sensitive spectroscopic window into the conformational ensemble, generally permitting the direct quantification of resolvable states. Moreover, straightforward T1- and T2-b...
Source: Current Opinion in Pharmacology - August 23, 2023 Category: Drugs & Pharmacology Authors: R S Prosser Nicolas A Alonzi Source Type: research
Spinal and bulbar muscular atrophy: From molecular pathogenesis to pharmacological intervention targeting skeletal muscle
Curr Opin Pharmacol. 2023 Aug;71:102394. doi: 10.1016/j.coph.2023.102394. Epub 2023 Jul 16.ABSTRACTThe clinical characteristics of SBMA, also known as Kennedy's disease (OMIM 313200), were initially documented by Dr. H Kawahara in the 18th century and a hundred years later by Dr. W. Kennedy. SBMA is a neuromuscular disease caused by expansions of a CAG microsatellite tandem repeat in exon 1 of the androgen receptor (AR) gene located on the X chromosome. These expansions result in the production of AR with an aberrantly expanded polyglutamine (polyQ) tract. In this review, we explore recent advancements in the significance ...
Source: Current Opinion in Pharmacology - July 18, 2023 Category: Drugs & Pharmacology Authors: Caterina Marchioretti Roberta Andreotti Emanuela Zuccaro Andrew P Lieberman Manuela Basso Maria Pennuto Source Type: research
Spinal and bulbar muscular atrophy: From molecular pathogenesis to pharmacological intervention targeting skeletal muscle
Curr Opin Pharmacol. 2023 Aug;71:102394. doi: 10.1016/j.coph.2023.102394. Epub 2023 Jul 16.ABSTRACTThe clinical characteristics of SBMA, also known as Kennedy's disease (OMIM 313200), were initially documented by Dr. H Kawahara in the 18th century and a hundred years later by Dr. W. Kennedy. SBMA is a neuromuscular disease caused by expansions of a CAG microsatellite tandem repeat in exon 1 of the androgen receptor (AR) gene located on the X chromosome. These expansions result in the production of AR with an aberrantly expanded polyglutamine (polyQ) tract. In this review, we explore recent advancements in the significance ...
Source: Current Opinion in Pharmacology - July 18, 2023 Category: Drugs & Pharmacology Authors: Caterina Marchioretti Roberta Andreotti Emanuela Zuccaro Andrew P Lieberman Manuela Basso Maria Pennuto Source Type: research
Spinal and bulbar muscular atrophy: From molecular pathogenesis to pharmacological intervention targeting skeletal muscle
Curr Opin Pharmacol. 2023 Aug;71:102394. doi: 10.1016/j.coph.2023.102394. Epub 2023 Jul 16.ABSTRACTThe clinical characteristics of SBMA, also known as Kennedy's disease (OMIM 313200), were initially documented by Dr. H Kawahara in the 18th century and a hundred years later by Dr. W. Kennedy. SBMA is a neuromuscular disease caused by expansions of a CAG microsatellite tandem repeat in exon 1 of the androgen receptor (AR) gene located on the X chromosome. These expansions result in the production of AR with an aberrantly expanded polyglutamine (polyQ) tract. In this review, we explore recent advancements in the significance ...
Source: Current Opinion in Pharmacology - July 18, 2023 Category: Drugs & Pharmacology Authors: Caterina Marchioretti Roberta Andreotti Emanuela Zuccaro Andrew P Lieberman Manuela Basso Maria Pennuto Source Type: research
Spinal and bulbar muscular atrophy: From molecular pathogenesis to pharmacological intervention targeting skeletal muscle
Curr Opin Pharmacol. 2023 Aug;71:102394. doi: 10.1016/j.coph.2023.102394. Epub 2023 Jul 16.ABSTRACTThe clinical characteristics of SBMA, also known as Kennedy's disease (OMIM 313200), were initially documented by Dr. H Kawahara in the 18th century and a hundred years later by Dr. W. Kennedy. SBMA is a neuromuscular disease caused by expansions of a CAG microsatellite tandem repeat in exon 1 of the androgen receptor (AR) gene located on the X chromosome. These expansions result in the production of AR with an aberrantly expanded polyglutamine (polyQ) tract. In this review, we explore recent advancements in the significance ...
Source: Current Opinion in Pharmacology - July 18, 2023 Category: Drugs & Pharmacology Authors: Caterina Marchioretti Roberta Andreotti Emanuela Zuccaro Andrew P Lieberman Manuela Basso Maria Pennuto Source Type: research
Spinal and bulbar muscular atrophy: From molecular pathogenesis to pharmacological intervention targeting skeletal muscle
Curr Opin Pharmacol. 2023 Aug;71:102394. doi: 10.1016/j.coph.2023.102394. Epub 2023 Jul 16.ABSTRACTThe clinical characteristics of SBMA, also known as Kennedy's disease (OMIM 313200), were initially documented by Dr. H Kawahara in the 18th century and a hundred years later by Dr. W. Kennedy. SBMA is a neuromuscular disease caused by expansions of a CAG microsatellite tandem repeat in exon 1 of the androgen receptor (AR) gene located on the X chromosome. These expansions result in the production of AR with an aberrantly expanded polyglutamine (polyQ) tract. In this review, we explore recent advancements in the significance ...
Source: Current Opinion in Pharmacology - July 18, 2023 Category: Drugs & Pharmacology Authors: Caterina Marchioretti Roberta Andreotti Emanuela Zuccaro Andrew P Lieberman Manuela Basso Maria Pennuto Source Type: research
Spinal and bulbar muscular atrophy: From molecular pathogenesis to pharmacological intervention targeting skeletal muscle
Curr Opin Pharmacol. 2023 Aug;71:102394. doi: 10.1016/j.coph.2023.102394. Epub 2023 Jul 16.ABSTRACTThe clinical characteristics of SBMA, also known as Kennedy's disease (OMIM 313200), were initially documented by Dr. H Kawahara in the 18th century and a hundred years later by Dr. W. Kennedy. SBMA is a neuromuscular disease caused by expansions of a CAG microsatellite tandem repeat in exon 1 of the androgen receptor (AR) gene located on the X chromosome. These expansions result in the production of AR with an aberrantly expanded polyglutamine (polyQ) tract. In this review, we explore recent advancements in the significance ...
Source: Current Opinion in Pharmacology - July 18, 2023 Category: Drugs & Pharmacology Authors: Caterina Marchioretti Roberta Andreotti Emanuela Zuccaro Andrew P Lieberman Manuela Basso Maria Pennuto Source Type: research
Spinal and bulbar muscular atrophy: From molecular pathogenesis to pharmacological intervention targeting skeletal muscle
Curr Opin Pharmacol. 2023 Aug;71:102394. doi: 10.1016/j.coph.2023.102394. Epub 2023 Jul 16.ABSTRACTThe clinical characteristics of SBMA, also known as Kennedy's disease (OMIM 313200), were initially documented by Dr. H Kawahara in the 18th century and a hundred years later by Dr. W. Kennedy. SBMA is a neuromuscular disease caused by expansions of a CAG microsatellite tandem repeat in exon 1 of the androgen receptor (AR) gene located on the X chromosome. These expansions result in the production of AR with an aberrantly expanded polyglutamine (polyQ) tract. In this review, we explore recent advancements in the significance ...
Source: Current Opinion in Pharmacology - July 18, 2023 Category: Drugs & Pharmacology Authors: Caterina Marchioretti Roberta Andreotti Emanuela Zuccaro Andrew P Lieberman Manuela Basso Maria Pennuto Source Type: research
Spinal and bulbar muscular atrophy: From molecular pathogenesis to pharmacological intervention targeting skeletal muscle
Curr Opin Pharmacol. 2023 Aug;71:102394. doi: 10.1016/j.coph.2023.102394. Epub 2023 Jul 16.ABSTRACTThe clinical characteristics of SBMA, also known as Kennedy's disease (OMIM 313200), were initially documented by Dr. H Kawahara in the 18th century and a hundred years later by Dr. W. Kennedy. SBMA is a neuromuscular disease caused by expansions of a CAG microsatellite tandem repeat in exon 1 of the androgen receptor (AR) gene located on the X chromosome. These expansions result in the production of AR with an aberrantly expanded polyglutamine (polyQ) tract. In this review, we explore recent advancements in the significance ...
Source: Current Opinion in Pharmacology - July 18, 2023 Category: Drugs & Pharmacology Authors: Caterina Marchioretti Roberta Andreotti Emanuela Zuccaro Andrew P Lieberman Manuela Basso Maria Pennuto Source Type: research
Spinal and bulbar muscular atrophy: From molecular pathogenesis to pharmacological intervention targeting skeletal muscle
Curr Opin Pharmacol. 2023 Aug;71:102394. doi: 10.1016/j.coph.2023.102394. Epub 2023 Jul 16.ABSTRACTThe clinical characteristics of SBMA, also known as Kennedy's disease (OMIM 313200), were initially documented by Dr. H Kawahara in the 18th century and a hundred years later by Dr. W. Kennedy. SBMA is a neuromuscular disease caused by expansions of a CAG microsatellite tandem repeat in exon 1 of the androgen receptor (AR) gene located on the X chromosome. These expansions result in the production of AR with an aberrantly expanded polyglutamine (polyQ) tract. In this review, we explore recent advancements in the significance ...
Source: Current Opinion in Pharmacology - July 18, 2023 Category: Drugs & Pharmacology Authors: Caterina Marchioretti Roberta Andreotti Emanuela Zuccaro Andrew P Lieberman Manuela Basso Maria Pennuto Source Type: research
Spinal and bulbar muscular atrophy: From molecular pathogenesis to pharmacological intervention targeting skeletal muscle
Curr Opin Pharmacol. 2023 Aug;71:102394. doi: 10.1016/j.coph.2023.102394. Epub 2023 Jul 16.ABSTRACTThe clinical characteristics of SBMA, also known as Kennedy's disease (OMIM 313200), were initially documented by Dr. H Kawahara in the 18th century and a hundred years later by Dr. W. Kennedy. SBMA is a neuromuscular disease caused by expansions of a CAG microsatellite tandem repeat in exon 1 of the androgen receptor (AR) gene located on the X chromosome. These expansions result in the production of AR with an aberrantly expanded polyglutamine (polyQ) tract. In this review, we explore recent advancements in the significance ...
Source: Current Opinion in Pharmacology - July 18, 2023 Category: Drugs & Pharmacology Authors: Caterina Marchioretti Roberta Andreotti Emanuela Zuccaro Andrew P Lieberman Manuela Basso Maria Pennuto Source Type: research
Spinal and bulbar muscular atrophy: From molecular pathogenesis to pharmacological intervention targeting skeletal muscle
Curr Opin Pharmacol. 2023 Aug;71:102394. doi: 10.1016/j.coph.2023.102394. Epub 2023 Jul 16.ABSTRACTThe clinical characteristics of SBMA, also known as Kennedy's disease (OMIM 313200), were initially documented by Dr. H Kawahara in the 18th century and a hundred years later by Dr. W. Kennedy. SBMA is a neuromuscular disease caused by expansions of a CAG microsatellite tandem repeat in exon 1 of the androgen receptor (AR) gene located on the X chromosome. These expansions result in the production of AR with an aberrantly expanded polyglutamine (polyQ) tract. In this review, we explore recent advancements in the significance ...
Source: Current Opinion in Pharmacology - July 18, 2023 Category: Drugs & Pharmacology Authors: Caterina Marchioretti Roberta Andreotti Emanuela Zuccaro Andrew P Lieberman Manuela Basso Maria Pennuto Source Type: research
