The development of highly potent and selective small molecule correctors of Z α

Crystallization Drug Design Drug Development / methods Drug Evaluation, Preclinical Endoplasmic Reticulum / metabolism Gene Library Hepatocytes / metabolism Humans Models, Molecular Protein Conformation Protein Folding alpha 1-Antitrypsin / genetics
2-Oxindole Misfolding α1-Antitrypsin

Journal

Bioorganic & medicinal chemistry letters
ISSN: 1464-3405
Titre abrégé: Bioorg Med Chem Lett
Pays: England
ID NLM: 9107377

Informations de publication

Date de publication:
01 06 2021
Historique:
received: 02 12 2020
revised: 05 03 2021
accepted: 13 03 2021
pubmed: 24 3 2021
medline: 26 8 2021
entrez: 23 3 2021
Statut: ppublish

Résumé

α1-antitrypsin deficiency is characterised by the misfolding and intracellular polymerisation of mutant α1-antitrypsin protein within the endoplasmic reticulum (ER) of hepatocytes. Small molecules that bind and stabilise Z α

Identifiants

DOI: 10.1016/j.bmcl.2021.127973 PMID: 33753261
pubmed: 33753261
pii: S0960-894X(21)00199-2
doi: 10.1016/j.bmcl.2021.127973
pii:
doi:

Substances chimiques

alpha 1-Antitrypsin 0

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

127973

Informations de copyright

Copyright © 2021 Elsevier Ltd. All rights reserved.

Auteurs

John Liddle (J)

GlaxoSmithKline, Gunnels Wood Road, Stevenage, Herts SG1 2NY, United Kingdom.

Andrew C Pearce (AC)

GlaxoSmithKline, Gunnels Wood Road, Stevenage, Herts SG1 2NY, United Kingdom.

Christopher Arico-Muendel (C)

GlaxoSmithKline, Cambridge Park Drive, 6th Floor, Cambridge, MA 02140, USA.

Svetlana Belyanskaya (S)

GlaxoSmithKline, Cambridge Park Drive, 6th Floor, Cambridge, MA 02140, USA.

Andrew Brewster (A)

GlaxoSmithKline, Gunnels Wood Road, Stevenage, Herts SG1 2NY, United Kingdom.

Murray Brown (M)

GlaxoSmithKline, Gunnels Wood Road, Stevenage, Herts SG1 2NY, United Kingdom.

Chun-Wa Chung (CW)

GlaxoSmithKline, Gunnels Wood Road, Stevenage, Herts SG1 2NY, United Kingdom.

Alexis Denis (A)

GlaxoSmithKline, Avenue du Quebec, Paris 91140, France.

Nerina Dodic (N)

GlaxoSmithKline, Avenue du Quebec, Paris 91140, France.

Anthony Dossang (A)

GlaxoSmithKline, Gunnels Wood Road, Stevenage, Herts SG1 2NY, United Kingdom.

Peter Eddershaw (P)

GlaxoSmithKline, Gunnels Wood Road, Stevenage, Herts SG1 2NY, United Kingdom.

Diana Klimaszewska (D)

GlaxoSmithKline, Gunnels Wood Road, Stevenage, Herts SG1 2NY, United Kingdom.

Imran Haq (I)

UCL Respiratory, Rayne Institute, University College London, London WC1E 6JF, United Kingdom.

Duncan S Holmes (DS)

GlaxoSmithKline, Gunnels Wood Road, Stevenage, Herts SG1 2NY, United Kingdom.

Alistair Jagger (A)

UCL Respiratory, Rayne Institute, University College London, London WC1E 6JF, United Kingdom.

Toral Jakhria (T)

GlaxoSmithKline, Gunnels Wood Road, Stevenage, Herts SG1 2NY, United Kingdom.

Emilie Jigorel (E)

GlaxoSmithKline, Avenue du Quebec, Paris 91140, France.

Ken Lind (K)

GlaxoSmithKline, Cambridge Park Drive, 6th Floor, Cambridge, MA 02140, USA.

Jeff Messer (J)

GlaxoSmithKline, Cambridge Park Drive, 6th Floor, Cambridge, MA 02140, USA.

Margaret Neu (M)

GlaxoSmithKline, Gunnels Wood Road, Stevenage, Herts SG1 2NY, United Kingdom.

Allison Olszewski (A)

GlaxoSmithKline, Cambridge Park Drive, 6th Floor, Cambridge, MA 02140, USA.

Riccardo Ronzoni (R)

UCL Respiratory, Rayne Institute, University College London, London WC1E 6JF, United Kingdom.

James Rowedder (J)

GlaxoSmithKline, Gunnels Wood Road, Stevenage, Herts SG1 2NY, United Kingdom.

Martin Rüdiger (M)

GlaxoSmithKline, Gunnels Wood Road, Stevenage, Herts SG1 2NY, United Kingdom.

Steve Skinner (S)

GlaxoSmithKline, Cambridge Park Drive, 6th Floor, Cambridge, MA 02140, USA.

Kathrine J Smith (KJ)

GlaxoSmithKline, Gunnels Wood Road, Stevenage, Herts SG1 2NY, United Kingdom.

Lionel Trottet (L)

GlaxoSmithKline, Avenue du Quebec, Paris 91140, France.

Iain Uings (I)

GlaxoSmithKline, Gunnels Wood Road, Stevenage, Herts SG1 2NY, United Kingdom.

Zhengrong Zhu (Z)

GlaxoSmithKline, Cambridge Park Drive, 6th Floor, Cambridge, MA 02140, USA.

James A Irving (JA)

UCL Respiratory, Rayne Institute, University College London, London WC1E 6JF, United Kingdom.

David A Lomas (DA)

UCL Respiratory, Rayne Institute, University College London, London WC1E 6JF, United Kingdom. Electronic address: d.lomas@ucl.ac.uk.

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Classifications MeSH

questionsmedicales.fr › Phénomènes chimiques › Cristallisation › The development of highly potent and selective...
questionsmedicales.fr › Techniques d'investigation › Développement de médicament › Découverte de médicament › Conception de médicament › The development of highly potent and selective...
questionsmedicales.fr › Techniques d'investigation › Développement de médicament › The development of highly potent and selective...
questionsmedicales.fr › Techniques d'investigation › Évaluation préclinique de médicament › The development of highly potent and selective...
questionsmedicales.fr › Cellules › Structures cellulaires › Espace intracellulaire › Cytoplasme › Structures cytoplasmiques › Organites › Réticulum endoplasmique › The development of highly potent and selective...
questionsmedicales.fr › Phénomènes génétiques › Structures génétiques › Banque de gènes › The development of highly potent and selective...
questionsmedicales.fr › Cellules › Cellules épithéliales › Hépatocytes › The development of highly potent and selective...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › The development of highly potent and selective...
questionsmedicales.fr › Techniques d'investigation › Modèles théoriques › Modèles moléculaires › The development of highly potent and selective...
questionsmedicales.fr › Phénomènes chimiques › Phénomènes biochimiques › Conformation moléculaire › Conformation des protéines › The development of highly potent and selective...
questionsmedicales.fr › Phénomènes chimiques › Phénomènes biochimiques › Pliage des protéines › The development of highly potent and selective...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › alpha-1-Antitrypsine › The development of highly potent and selective...