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Avacopan for the Treatment of ANCA-Associated Vasculitis

The New England journal of medicine, 2021-02, Vol.384 (7), p.599-609

2021

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Development towards a novel screening method for nipecotic acid bioisosteres using molecular imprinted polymers (MIPs) as alternative to in vitro cellular uptake assays

Talanta (Oxford), 2024-10, Vol.278, p.126500, Article 126500

2024

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Avacopan: First Approval

Drugs (New York, N.Y.), 2022, Vol.82 (1), p.79-85

Lee, Arnold

2022

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Randomized Trial of C5a Receptor Inhibitor Avacopan in ANCA-Associated Vasculitis

Journal of the American Society of Nephrology, 2017-09, Vol.28 (9), p.2756-2767

2017

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Pharmacokinetic optimitzation of CCG-203971: Novel inhibitors of the Rho/MRTF/SRF transcriptional pathway as potential antifibrotic therapeutics for systemic scleroderma

Bioorganic & medicinal chemistry letters, 2017-04, Vol.27 (8), p.1744-1749

2017

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Targeting the myofibroblast genetic switch: inhibitors of myocardin-related transcription factor/serum response factor-regulated gene transcription prevent fibrosis in a murine model of skin injury

The Journal of pharmacology and experimental therapeutics, 2014-06, Vol.349 (3), p.480-486

2014

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Synthesis and biological evaluation of novel N-substituted nipecotic acid derivatives with a trans-alkene spacer as potent GABA uptake inhibitors

Bioorganic & medicinal chemistry, 2018-12, Vol.26 (22), p.5944-5961

2018

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Nipecotic acid as potential lead molecule for the development of GABA uptake inhibitors; structural insights and design strategies

European journal of medicinal chemistry, 2022-04, Vol.234, p.114269-114269, Article 114269

2022

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Development of Highly Potent GAT1 Inhibitors: Synthesis of Nipecotic Acid Derivatives by Suzuki-Miyaura Cross-Coupling Reactions

ChemMedChem, 2016-03, Vol.11 (5), p.519-538

2016

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GABAergic regulation of cerebellar NG2 cell development is altered in perinatal white matter injury

Nature neuroscience, 2015-05, Vol.18 (5), p.674-682

2015

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Inhibition of Myocardin-Related Transcription Factor/Serum Response Factor Signaling Decreases Lung Fibrosis and Promotes Mesenchymal Cell Apoptosis

The American journal of pathology, 2015-04, Vol.185 (4), p.969-986

2015

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Characterization of Pharmacologic and Pharmacokinetic Properties of CCX168, a Potent and Selective Orally Administered Complement 5a Receptor Inhibitor, Based on Preclinical Evaluation and Randomized Phase 1 Clinical Study

PloS one, 2016-10, Vol.11 (10), p.e0164646-e0164646

2016

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Pharmacological characterisation of small molecule C5aR1 inhibitors in human cells reveals biased activities for signalling and function

Biochemical pharmacology, 2020-10, Vol.180, p.114156, Article 114156

2020

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Synthesis and Biological Evaluation of Nipecotic Acid and Guvacine Derived 1,3‐Disubstituted Allenes as Inhibitors of Murine GABA Transporter mGAT1

ChemMedChem, 2019-06, Vol.14 (12), p.1135-1151

2019

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Avacopan in the treatment of ANCA-associated vasculitis

Expert opinion on investigational drugs, 2018-05, Vol.27 (5), p.491-496

2018

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Development of Highly Potent GAT1 Inhibitors: Synthesis of Nipecotic Acid Derivatives with N‐Arylalkynyl Substituents

ChemMedChem, 2017-03, Vol.12 (5), p.362-371

2017

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Synthesis and biological evaluation of novel N-substituted nipecotic acid derivatives with a cis-alkene spacer as GABA uptake inhibitors

Bioorganic & medicinal chemistry, 2019-03, Vol.27 (5), p.822-831

2019

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Potential role of selected antiepileptics used in neuropathic pain as human GABA transporter isoform 1 (GAT1) inhibitors—Molecular docking and pharmacodynamic studies

European journal of pharmaceutical sciences, 2017-01, Vol.96, p.362-372

2017

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First Photoswitchable Neurotransmitter Transporter Inhibitor: Light-Induced Control of γ‑Aminobutyric Acid Transporter 1 (GAT1) Activity in Mouse Brain

Journal of medicinal chemistry, 2014-08, Vol.57 (15), p.6809-6821

2014

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N‐Substituted Nipecotic Acids as (S)‐SNAP‐5114 Analogues with Modified Lipophilic Domains

ChemMedChem, 2020-05, Vol.15 (9), p.756-771

2020

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Pharmacoproteomics pinpoints HSP70 interaction for correction of the most frequent Wilson disease-causing mutant of ATP7B

Proceedings of the National Academy of Sciences - PNAS, 2020-12, Vol.117 (51), p.32453-32463

2020

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Optimization of novel nipecotic bis(amide) inhibitors of the Rho/MKL1/SRF transcriptional pathway as potential anti-metastasis agents

Bioorganic & medicinal chemistry letters, 2013-07, Vol.23 (13), p.3826-3832

2013

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A Binding Mode Hypothesis of Tiagabine Confirms Liothyronine Effect on γ‑Aminobutyric Acid Transporter 1 (GAT1)

Journal of medicinal chemistry, 2015-03, Vol.58 (5), p.2149-2158

2015

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Being an ADVOCATE for People with ANCA Vasculitis

Clinical journal of the American Society of Nephrology, 2021-10, Vol.16 (10), p.1581-1583

2021

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Synthesis of 4-substituted nipecotic acid derivatives and their evaluation as potential GABA uptake inhibitors

Bioorganic & medicinal chemistry, 2016-05, Vol.24 (9), p.2072-2096

2016

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Avacopan for the Treatment of ANCA-Associated Vasculitis

Development towards a novel screening method for nipecotic acid bioisosteres using molecular imprinted polymers (MIPs) as alternative to in vitro cellular uptake assays

Avacopan: First Approval

Randomized Trial of C5a Receptor Inhibitor Avacopan in ANCA-Associated Vasculitis

Pharmacokinetic optimitzation of CCG-203971: Novel inhibitors of the Rho/MRTF/SRF transcriptional pathway as potential antifibrotic therapeutics for systemic scleroderma

Targeting the myofibroblast genetic switch: inhibitors of myocardin-related transcription factor/serum response factor-regulated gene transcription prevent fibrosis in a murine model of skin injury

Synthesis and biological evaluation of novel N-substituted nipecotic acid derivatives with a trans-alkene spacer as potent GABA uptake inhibitors

Nipecotic acid as potential lead molecule for the development of GABA uptake inhibitors; structural insights and design strategies

Development of Highly Potent GAT1 Inhibitors: Synthesis of Nipecotic Acid Derivatives by Suzuki-Miyaura Cross-Coupling Reactions

GABAergic regulation of cerebellar NG2 cell development is altered in perinatal white matter injury

Inhibition of Myocardin-Related Transcription Factor/Serum Response Factor Signaling Decreases Lung Fibrosis and Promotes Mesenchymal Cell Apoptosis

Characterization of Pharmacologic and Pharmacokinetic Properties of CCX168, a Potent and Selective Orally Administered Complement 5a Receptor Inhibitor, Based on Preclinical Evaluation and Randomized Phase 1 Clinical Study

Pharmacological characterisation of small molecule C5aR1 inhibitors in human cells reveals biased activities for signalling and function

Synthesis and Biological Evaluation of Nipecotic Acid and Guvacine Derived 1,3‐Disubstituted Allenes as Inhibitors of Murine GABA Transporter mGAT1

Avacopan in the treatment of ANCA-associated vasculitis

Development of Highly Potent GAT1 Inhibitors: Synthesis of Nipecotic Acid Derivatives with N‐Arylalkynyl Substituents

Synthesis and biological evaluation of novel N-substituted nipecotic acid derivatives with a cis-alkene spacer as GABA uptake inhibitors

Potential role of selected antiepileptics used in neuropathic pain as human GABA transporter isoform 1 (GAT1) inhibitors—Molecular docking and pharmacodynamic studies

First Photoswitchable Neurotransmitter Transporter Inhibitor: Light-Induced Control of γ‑Aminobutyric Acid Transporter 1 (GAT1) Activity in Mouse Brain

N‐Substituted Nipecotic Acids as (S)‐SNAP‐5114 Analogues with Modified Lipophilic Domains

Pharmacoproteomics pinpoints HSP70 interaction for correction of the most frequent Wilson disease-causing mutant of ATP7B

Optimization of novel nipecotic bis(amide) inhibitors of the Rho/MKL1/SRF transcriptional pathway as potential anti-metastasis agents

A Binding Mode Hypothesis of Tiagabine Confirms Liothyronine Effect on γ‑Aminobutyric Acid Transporter 1 (GAT1)

Being an ADVOCATE for People with ANCA Vasculitis

Synthesis of 4-substituted nipecotic acid derivatives and their evaluation as potential GABA uptake inhibitors

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