From Small to Powerful: The Fragments Universe and its “Chem-Appeal”

ISSN: 1875-533X (Online)
ISSN: 0929-8673 (Print)

Volume 24, 42 Issues, 2017

Download PDF Flyer

Current Medicinal Chemistry

This journal supports open access

Aims & ScopeAbstracted/Indexed in

Ranking and Category:
  • 10th of 59 in Chemistry & Medicinal
  • 63rd of 253 in Pharmacology & Pharmacy
  • 100th of 289 in Biochemistry & Molecular Biology

Submit Abstracts Online Submit Manuscripts Online

Atta-ur-Rahman, FRS
Honorary Life Fellow
Kings College
University of Cambridge

View Full Editorial Board

Subscribe Purchase Articles Order Reprints

Current: 3.455
5 - Year: 3.792

From Small to Powerful: The Fragments Universe and its “Chem-Appeal”

Current Medicinal Chemistry, 20(11): 1355-1381.

Author(s): Luca Sancineto, Serena Massari, Nunzio Iraci and Oriana Tabarrini.

Affiliation: Department of Chemistry and Technology of Drug, University of Perugia, Via del Liceo 1, 06123, Perugia, Italy.


While increasing expertise in molecular biology and proteomics is markedly speeding up the target elucidation process, various strategies have been proposed that improve the chances of identifying active molecules. Among them, the Fragment Based Drug Design (FBDD) is surely worth noting. The FBDD entails the screening of a small number of low molecular weight compounds in the hopes of finding even low affine but high ligand efficient fragments that have high probability to became drug candidates. Since 1996, when the first paper on FBDD was reported, the potentialities of this strategy became progressively more apparent as testified by the growing number of publications. Many drug discovery projects started with the identification of fragments which after the optimization gave many molecules close to the approval and one marketed drug Vemurafenib, approved in 2011.

A preamble that highlights the advantages of dealing with simple and “very small” molecules over conventional drug-like compounds will be herein given prior to discussing the canonical FBDD stages, from fragment library design, to the different screening methods concluding with the various optimization strategies, in an attempt to illustrate the whole FBDD workflow while discussing the most recent and successful applications.

While this review is a tribute to the success achieved by the researchers in this field, it is particularly addressed to scientists who want to become aware of the versatility and potentiality of FBDD.


FBDD, fragment library design, fragment optimization, NMR screening, SPR-based screening, X-ray crystallography.

Purchase Online Order Reprints Order Eprints Rights and Permissions

Author video for this article

Watch what auhtors say about their articles

Article Details

Volume: 20
Issue Number: 11
First Page: 1355
Last Page: 1381
Page Count: 27
DOI: 10.2174/09298673113209990111
Price: $58
Global Biotechnology Congress 2017Drug Discovery and Therapy World Congress 2017Drug Discovery 2017

Related Journals

Related eBooks

Webmaster Contact: Copyright © 2017 Bentham Science