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PI3K inhibitors are finally coming of age

Nature reviews. Drug discovery, 2021-10, Vol.20 (10), p.741-769

2021

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hERG K(+) channels: structure, function, and clinical significance

Physiological reviews, 2012-07, Vol.92 (3), p.1393-1478

2012

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Impact of Stereospecific Intramolecular Hydrogen Bonding on Cell Permeability and Physicochemical Properties

Journal of medicinal chemistry, 2014-03, Vol.57 (6), p.2746-2754

2014

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Development of a robust induced pluripotent stem cell atrial cardiomyocyte differentiation protocol to model atrial arrhythmia

Stem cell research & therapy, 2023-07, Vol.14 (1), p.183-183

2023

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Evolution of PI3Kγ and δ Inhibitors for Inflammatory and Autoimmune Diseases

Journal of medicinal chemistry, 2019-05, Vol.62 (10), p.4783-4814

2019

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Multiple Interactions between Cytoplasmic Domains Regulate Slow Deactivation of Kv11.1 Channels

The Journal of biological chemistry, 2014-09, Vol.289 (37), p.25822-25832

2014

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The S4-S5 linker acts as a signal integrator for HERG K+ channel activation and deactivation gating

PloS one, 2012-02, Vol.7 (2), p.e31640-e31640

2012

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Getting to the heart of hERG K+ channel gating

The Journal of physiology, 2015-06, Vol.593 (12), p.2575-2585

2015

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The S1 helix critically regulates the finely tuned gating of Kv11.1 channels

The Journal of biological chemistry, 2017-05, Vol.292 (18), p.7688-7705

2017

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Structural and conformational determinants of macrocycle cell permeability

Nature chemical biology, 2016-12, Vol.12 (12), p.1065

2016

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The N-terminal tail of hERG contains an amphipathic α-helix that regulates channel deactivation

PloS one, 2011-01, Vol.6 (1), p.e16191

2011

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Voltage-sensing domain mode shift is coupled to the activation gate by the N-terminal tail of hERG channels

The Journal of general physiology, 2012-09, Vol.140 (3), p.293-306

2012

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Stabilization of protein-protein interactions in drug discovery

Expert opinion on drug discovery, 2017-09, Vol.12 (9), p.925-940

2017

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A class of highly selective inhibitors bind to an active state of PI3Kγ

Nature chemical biology, 2019-04, Vol.15 (4), p.348

2019

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Scaffold-hopping with zwitterionic CCR3 antagonists: Identification and optimisation of a series with good potency and pharmacokinetics leading to the discovery of AZ12436092

Bioorganic & medicinal chemistry letters, 2012-11, Vol.22 (21), p.6694-6699

2012

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C-terminal β9-strand of the cyclic nucleotide-binding homology domain stabilizes activated states of Kv11.1 channels

PloS one, 2013-10, Vol.8 (10), p.e77032-e77032

2013

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Co-expression of calcium and hERG potassium channels reduces the incidence of proarrhythmic events

Cardiovascular research, 2021-08, Vol.117 (10), p.2216-2227

2021

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Identification of Phosphate-Containing Compounds as New Inhibitors of 14-3-3/c-Abl Protein–Protein Interaction

ACS chemical biology, 2020-04, Vol.15 (4), p.1026-1035

2020

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Pathophysiological metabolic changes associated with disease modify the proarrhythmic risk profile of drugs with potential to prolong repolarisation

British journal of pharmacology, 2022-06, Vol.179 (11), p.2631-2646

2022

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Pharmacological activation of IKr in models of long QT Type 2 risks overcorrection of repolarization

Cardiovascular research, 2020-07, Vol.116 (8), p.1434-1445

2020

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High-throughput phenotyping of heteromeric human ether-à-go-go-related gene potassium channel variants can discriminate pathogenic from rare benign variants

Heart rhythm, 2020-03, Vol.17 (3), p.492-500

2020

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Action Potential Morphology Accurately Predicts Proarrhythmic Risk for Drugs With Potential to Prolong Cardiac Repolarization

Circulation. Arrhythmia and electrophysiology, 2023-07, Vol.16 (7), p.399

2023

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Convergence of models of human ventricular myocyte electrophysiology after global optimization to recapitulate clinical long QT phenotypes

Journal of molecular and cellular cardiology, 2016-11, Vol.100, p.25-34

2016

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Pore Helices Play a Dynamic Role as Integrators of Domain Motion during Kv11.1 Channel Inactivation Gating

The Journal of biological chemistry, 2013-04, Vol.288 (16), p.11482-11491

2013

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PI3K inhibitors are finally coming of age

hERG K(+) channels: structure, function, and clinical significance

Impact of Stereospecific Intramolecular Hydrogen Bonding on Cell Permeability and Physicochemical Properties

Development of a robust induced pluripotent stem cell atrial cardiomyocyte differentiation protocol to model atrial arrhythmia

Evolution of PI3Kγ and δ Inhibitors for Inflammatory and Autoimmune Diseases

Multiple Interactions between Cytoplasmic Domains Regulate Slow Deactivation of Kv11.1 Channels

The S4-S5 linker acts as a signal integrator for HERG K+ channel activation and deactivation gating

Getting to the heart of hERG K+ channel gating

The S1 helix critically regulates the finely tuned gating of Kv11.1 channels

Structural and conformational determinants of macrocycle cell permeability

The N-terminal tail of hERG contains an amphipathic α-helix that regulates channel deactivation

Voltage-sensing domain mode shift is coupled to the activation gate by the N-terminal tail of hERG channels

Stabilization of protein-protein interactions in drug discovery

A class of highly selective inhibitors bind to an active state of PI3Kγ

Scaffold-hopping with zwitterionic CCR3 antagonists: Identification and optimisation of a series with good potency and pharmacokinetics leading to the discovery of AZ12436092

Discovery of AZD8154, a Dual PI3Kγδ Inhibitor for the Treatment of Asthma

C-terminal β9-strand of the cyclic nucleotide-binding homology domain stabilizes activated states of Kv11.1 channels

Co-expression of calcium and hERG potassium channels reduces the incidence of proarrhythmic events

Identification of Phosphate-Containing Compounds as New Inhibitors of 14-3-3/c-Abl Protein–Protein Interaction

Pathophysiological metabolic changes associated with disease modify the proarrhythmic risk profile of drugs with potential to prolong repolarisation

Pharmacological activation of IKr in models of long QT Type 2 risks overcorrection of repolarization

High-throughput phenotyping of heteromeric human ether-à-go-go-related gene potassium channel variants can discriminate pathogenic from rare benign variants

Action Potential Morphology Accurately Predicts Proarrhythmic Risk for Drugs With Potential to Prolong Cardiac Repolarization

Convergence of models of human ventricular myocyte electrophysiology after global optimization to recapitulate clinical long QT phenotypes

Pore Helices Play a Dynamic Role as Integrators of Domain Motion during Kv11.1 Channel Inactivation Gating

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