Fragments: where are we now?
Fragment-based drug design
fragment library design
fragment screening
screening techniques
Journal
Biochemical Society transactions
ISSN: 1470-8752
Titre abrégé: Biochem Soc Trans
Pays: England
ID NLM: 7506897
Informations de publication
Date de publication:
28 02 2020
28 02 2020
Historique:
received:
13
11
2019
revised:
17
12
2019
accepted:
18
12
2019
pubmed:
28
1
2020
medline:
9
4
2020
entrez:
28
1
2020
Statut:
ppublish
Résumé
Fragment-based drug discovery (FBDD) has become a mainstream technology for the identification of chemical hit matter in drug discovery programs. To date, the food and drug administration has approved four drugs, and over forty compounds are in clinical studies that can trace their origins to a fragment-based screen. The challenges associated with implementing an FBDD approach are many and diverse, ranging from the library design to developing methods for identifying weak affinity compounds. In this article, we give an overview of current progress in fragment library design, fragment to lead optimisation and on the advancement in techniques used for screening. Finally, we will comment on the future opportunities and challenges in this field.
Identifiants
pubmed: 31985743
pii: 221949
doi: 10.1042/BST20190694
doi:
Substances chimiques
Small Molecule Libraries
0
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Review
Langues
eng
Sous-ensembles de citation
IM
Pagination
271-280Informations de copyright
© 2020 The Author(s). Published by Portland Press Limited on behalf of the Biochemical Society.