Pharmacologic treatment of gastroparesis: What is (still) on the horizon?
Curr Opin Pharmacol. 2023 Aug 26;72:102395. doi: 10.1016/j.coph.2023.102395. Online ahead of print.ABSTRACTGastroparesis is a neuromuscular disorder of the upper gastrointestinal tract. Patients typically complain about early satiety, postprandial fullness, nausea and vomiting. Etiology is multifactorial. Treatment strategies include nutritional support, pharmacologic agents or surgery for refractory cases. Metoclopramide is the first and only FDA approved pharmacologic agent for (diabetic) Gastroparesis. A couple of compounds are currently in clinical testing. Some beacons of hope have failed recently, however. Here we pr...
Source: Current Opinion in Pharmacology - August 28, 2023 Category: Drugs & Pharmacology Authors: D Schweckendiek D Pohl Source Type: research
Pharmacologic treatment of gastroparesis: What is (still) on the horizon?
Curr Opin Pharmacol. 2023 Aug 26;72:102395. doi: 10.1016/j.coph.2023.102395. Online ahead of print.ABSTRACTGastroparesis is a neuromuscular disorder of the upper gastrointestinal tract. Patients typically complain about early satiety, postprandial fullness, nausea and vomiting. Etiology is multifactorial. Treatment strategies include nutritional support, pharmacologic agents or surgery for refractory cases. Metoclopramide is the first and only FDA approved pharmacologic agent for (diabetic) Gastroparesis. A couple of compounds are currently in clinical testing. Some beacons of hope have failed recently, however. Here we pr...
Source: Current Opinion in Pharmacology - August 28, 2023 Category: Drugs & Pharmacology Authors: D Schweckendiek D Pohl Source Type: research
Pharmacologic treatment of gastroparesis: What is (still) on the horizon?
Curr Opin Pharmacol. 2023 Aug 26;72:102395. doi: 10.1016/j.coph.2023.102395. Online ahead of print.ABSTRACTGastroparesis is a neuromuscular disorder of the upper gastrointestinal tract. Patients typically complain about early satiety, postprandial fullness, nausea and vomiting. Etiology is multifactorial. Treatment strategies include nutritional support, pharmacologic agents or surgery for refractory cases. Metoclopramide is the first and only FDA approved pharmacologic agent for (diabetic) Gastroparesis. A couple of compounds are currently in clinical testing. Some beacons of hope have failed recently, however. Here we pr...
Source: Current Opinion in Pharmacology - August 28, 2023 Category: Drugs & Pharmacology Authors: D Schweckendiek D Pohl Source Type: research
Pharmacologic treatment of gastroparesis: What is (still) on the horizon?
Curr Opin Pharmacol. 2023 Aug 26;72:102395. doi: 10.1016/j.coph.2023.102395. Online ahead of print.ABSTRACTGastroparesis is a neuromuscular disorder of the upper gastrointestinal tract. Patients typically complain about early satiety, postprandial fullness, nausea and vomiting. Etiology is multifactorial. Treatment strategies include nutritional support, pharmacologic agents or surgery for refractory cases. Metoclopramide is the first and only FDA approved pharmacologic agent for (diabetic) Gastroparesis. A couple of compounds are currently in clinical testing. Some beacons of hope have failed recently, however. Here we pr...
Source: Current Opinion in Pharmacology - August 28, 2023 Category: Drugs & Pharmacology Authors: D Schweckendiek D Pohl Source Type: research
Pharmacologic treatment of gastroparesis: What is (still) on the horizon?
Curr Opin Pharmacol. 2023 Aug 26;72:102395. doi: 10.1016/j.coph.2023.102395. Online ahead of print.ABSTRACTGastroparesis is a neuromuscular disorder of the upper gastrointestinal tract. Patients typically complain about early satiety, postprandial fullness, nausea and vomiting. Etiology is multifactorial. Treatment strategies include nutritional support, pharmacologic agents or surgery for refractory cases. Metoclopramide is the first and only FDA approved pharmacologic agent for (diabetic) Gastroparesis. A couple of compounds are currently in clinical testing. Some beacons of hope have failed recently, however. Here we pr...
Source: Current Opinion in Pharmacology - August 28, 2023 Category: Drugs & Pharmacology Authors: D Schweckendiek D Pohl Source Type: research
Pharmacologic treatment of gastroparesis: What is (still) on the horizon?
Curr Opin Pharmacol. 2023 Aug 26;72:102395. doi: 10.1016/j.coph.2023.102395. Online ahead of print.ABSTRACTGastroparesis is a neuromuscular disorder of the upper gastrointestinal tract. Patients typically complain about early satiety, postprandial fullness, nausea and vomiting. Etiology is multifactorial. Treatment strategies include nutritional support, pharmacologic agents or surgery for refractory cases. Metoclopramide is the first and only FDA approved pharmacologic agent for (diabetic) Gastroparesis. A couple of compounds are currently in clinical testing. Some beacons of hope have failed recently, however. Here we pr...
Source: Current Opinion in Pharmacology - August 28, 2023 Category: Drugs & Pharmacology Authors: D Schweckendiek D Pohl Source Type: research
Pharmacologic treatment of gastroparesis: What is (still) on the horizon?
Curr Opin Pharmacol. 2023 Aug 26;72:102395. doi: 10.1016/j.coph.2023.102395. Online ahead of print.ABSTRACTGastroparesis is a neuromuscular disorder of the upper gastrointestinal tract. Patients typically complain about early satiety, postprandial fullness, nausea and vomiting. Etiology is multifactorial. Treatment strategies include nutritional support, pharmacologic agents or surgery for refractory cases. Metoclopramide is the first and only FDA approved pharmacologic agent for (diabetic) Gastroparesis. A couple of compounds are currently in clinical testing. Some beacons of hope have failed recently, however. Here we pr...
Source: Current Opinion in Pharmacology - August 28, 2023 Category: Drugs & Pharmacology Authors: D Schweckendiek D Pohl 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
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
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
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
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
