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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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Author Correction: PI3K inhibitors are finally coming of age

Nature reviews. Drug discovery, 2021-10, Vol.20 (10), p.798-798

2021

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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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Design, Synthesis, and Biological Evaluation of MEK PROTACs

Journal of medicinal chemistry, 2020-01, Vol.63 (1), p.157-162

2020

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TECRL: connecting sequence to consequence for a new sudden cardiac death gene

EMBO molecular medicine, 2016-12, Vol.8 (12), p.1364-1365

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

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

2012

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Discovery of Highly Isoform Selective Orally Bioavailable Phosphoinositide 3‑Kinase (PI3K)‑γ Inhibitors

Journal of medicinal chemistry, 2018-06, Vol.61 (12), p.5435-5441

2018

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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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Steady-state modulation of voltage-gated K+ channels in rat arterial smooth muscle by cyclic AMP-dependent protein kinase and protein phosphatase 2B

PloS one, 2015-03, Vol.10 (3), p.e0121285

2015

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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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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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Recent advances in understanding and prevention of sudden cardiac death [version 1; peer review: 2 approved]

F1000 research, 2017, Vol.6, p.1614-1614

2017

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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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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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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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Protocol-Dependent Differences in IC50 Values Measured in Human Ether-Á-Go-Go-Related Gene Assays Occur in a Predictable Way and Can Be Used to Quantify State Preference of Drug Binding

Molecular pharmacology, 2019-05, Vol.95 (5), p.537-550

2019

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Using many different voltage protocols to characterise discrepancy in mathematical ion channel models

Biophysical journal, 2023-02, Vol.122 (3), p.242a-242a

2023

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Design and Synthesis of Soluble and Cell-Permeable PI3Kδ Inhibitors for Long-Acting Inhaled Administration

Journal of medicinal chemistry, 2017-06, Vol.60 (12), p.5057-5071

2017

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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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Spiro-fused Pyrrolidine, Piperidine, and Oxindole Scaffolds from Lactams

Organic letters, 2012-09, Vol.14 (18), p.4846-4849

2012

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PI3K inhibitors are finally coming of age

Author Correction: PI3K inhibitors are finally coming of age

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

Design, Synthesis, and Biological Evaluation of MEK PROTACs

TECRL: connecting sequence to consequence for a new sudden cardiac death gene

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

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

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

Discovery of Highly Isoform Selective Orally Bioavailable Phosphoinositide 3‑Kinase (PI3K)‑γ Inhibitors

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

Steady-state modulation of voltage-gated K+ channels in rat arterial smooth muscle by cyclic AMP-dependent protein kinase and protein phosphatase 2B

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

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

Recent advances in understanding and prevention of sudden cardiac death [version 1; peer review: 2 approved]

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

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

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

Protocol-Dependent Differences in IC50 Values Measured in Human Ether-Á-Go-Go-Related Gene Assays Occur in a Predictable Way and Can Be Used to Quantify State Preference of Drug Binding

Using many different voltage protocols to characterise discrepancy in mathematical ion channel models

Design and Synthesis of Soluble and Cell-Permeable PI3Kδ Inhibitors for Long-Acting Inhaled Administration

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

Spiro-fused Pyrrolidine, Piperidine, and Oxindole Scaffolds from Lactams

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