What is the future for fragment-based drug discovery?

2017 ◽  
Vol 9 (13) ◽  
pp. 1457-1460 ◽  
Author(s):  
György M Keserű ◽  
Michael M Hann
Keyword(s):  
Drug Discovery ◽  
The Future ◽  
Fragment Based Drug Discovery

scholarly journals Is it time for biocatalysis in fragment-based drug discovery?

2020 ◽  
Vol 11 (41) ◽  
pp. 11104-11112
Author(s):  
Jeremy I. Ramsden ◽  
Sebastian C. Cosgrove ◽  
Nicholas J. Turner
Keyword(s):  
Drug Discovery ◽  
The Future ◽  
Fragment Based Drug Discovery

This perspective discusses how biocatalysis could play an important role in the future fragment-based drug discovery.

Fragments: where are we now?

2020 ◽  
Vol 48 (1) ◽  
pp. 271-280 ◽  
Author(s):  
James Osborne ◽  
Stanislava Panova ◽  
Magdalini Rapti ◽  
Tatsuya Urushima ◽  
Harren Jhoti
Keyword(s):  
Drug Discovery ◽  
Drug Administration ◽  
Clinical Studies ◽  
Food And Drug Administration ◽  
Library Design ◽  
Lead Optimisation ◽  
Fragment Library ◽  
The Future ◽  
Fragment Based Drug Discovery

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.

scholarly journals Ubiquitination, Biotech Startups, and the Future of TRIM Family Proteins: A TRIM-Endous Opportunity

Cells ◽  
2021 ◽  
Vol 10 (5) ◽  
pp. 1015
Author(s):  
Utsa Bhaduri ◽  
Giuseppe Merla
Keyword(s):  
Drug Discovery ◽  
Protein Degradation ◽  
Ubiquitin Ligase ◽  
Genetic Disorders ◽  
E3 Ubiquitin Ligase ◽  
Ubiquitin Ligases ◽  
E3 Ubiquitin Ligases ◽  
Post Translational Modification ◽  
Disease Biology ◽  
The Future

Ubiquitination is a post-translational modification that has pivotal roles in protein degradation and diversified cellular processes, and for more than two decades it has been a subject of interest in the biotech or biopharmaceutical industry. Tripartite motif (TRIM) family proteins are known to have proven E3 ubiquitin ligase activities and are involved in a multitude of cellular and physiological events and pathophysiological conditions ranging from cancers to rare genetic disorders. Although in recent years many kinds of E3 ubiquitin ligases have emerged as the preferred choices of big pharma and biotech startups in the context of protein degradation and disease biology, from a surface overview it appears that TRIM E3 ubiquitin ligases are not very well recognized yet in the realm of drug discovery. This article will review some of the blockbuster scientific discoveries and technological innovations from the world of ubiquitination and E3 ubiquitin ligases that have impacted the biopharma community, from biotech colossuses to startups, and will attempt to evaluate the future of TRIM family proteins in the province of E3 ubiquitin ligase-based drug discovery.

scholarly journals Validating Fragment-Based Drug Discovery for Biological RNAs: Lead Fragments Bind and Remodel the TPP Riboswitch Specifically

2014 ◽  
Vol 21 (5) ◽  
pp. 591-595 ◽  
Author(s):  
Katherine Deigan Warner ◽  
Philip Homan ◽  
Kevin M. Weeks ◽  
Alison G. Smith ◽  
Chris Abell ◽  
...  
Keyword(s):  
Drug Discovery ◽  
Fragment Based Drug Discovery
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