Abstract：
:Fragment-based screening has now become an established method for the generation of lead molecules against therapeutic targets. Fragment molecules are simple, low molecular-weight compounds with few chemical functionalities. These characteristics lead to high hit rates for fragment screening as compared to the more classical High-Throughput Screening of drug-like molecules and raise the question of the specificity of fragment molecules. This review analyzes recent outcomes of fragment screenings published in the literature, showing that the specificity of the fragments can be related to their structures and physico-chemical properties. We also discuss both the concept of privileged fragment scaffolds and the role of fragment-based screening in predicting protein druggability, highlighted by recent publications in the field.
journal_name
Curr Opin Chem Bioljournal_title
Current opinion in chemical biologyauthors
Barelier S,Krimm Idoi
10.1016/j.cbpa.2011.02.020subject
Has Abstractpub_date
2011-08-01 00:00:00pages
469-74issue
4eissn
1367-5931issn
1879-0402pii
S1367-5931(11)00033-0journal_volume
15pub_type
杂志文章,评审abstract：:Although random mutagenesis and screening and evolutionary engineering have long been the gold standards for strain improvement in industry, the development of more sophisticated recombinant DNA tools has led to the introduction of alternate methods for engineering strain diversity. Here, we summarize several combinat...
journal_title：Current opinion in chemical biology
pub_type： 杂志文章,评审
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更新日期：2008-04-01 00:00:00
abstract：:Peptide natural products (PNPs) represent a unique class of compounds known for their fascinating structural motifs with important biological activities. Lately, PNPs have garnered a lot of interest for their application in drug discovery. Nevertheless, lack of diversity oriented synthetic/biosynthetic platforms to ge...
journal_title：Current opinion in chemical biology
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journal_title：Current opinion in chemical biology
pub_type： 杂志文章,评审
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journal_title：Current opinion in chemical biology
pub_type： 杂志文章,评审
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journal_title：Current opinion in chemical biology
pub_type： 杂志文章,评审
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更新日期：2010-12-01 00:00:00
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journal_title：Current opinion in chemical biology
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journal_title：Current opinion in chemical biology
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journal_title：Current opinion in chemical biology
pub_type： 杂志文章,评审
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journal_title：Current opinion in chemical biology
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journal_title：Current opinion in chemical biology
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journal_title：Current opinion in chemical biology
pub_type： 杂志文章,评审
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更新日期：2003-10-01 00:00:00
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journal_title：Current opinion in chemical biology
pub_type： 杂志文章,评审
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更新日期：1999-04-01 00:00:00
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journal_title：Current opinion in chemical biology
pub_type： 杂志文章,评审
doi：10.1016/j.cbpa.2008.08.037
更新日期：2008-12-01 00:00:00
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journal_title：Current opinion in chemical biology
pub_type： 杂志文章,评审
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更新日期：2000-12-01 00:00:00
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journal_title：Current opinion in chemical biology
pub_type： 杂志文章,评审
doi：10.1016/j.cbpa.2007.05.030
更新日期：2007-08-01 00:00:00
abstract：:The appearance of the highly pathogenic avian influenza virus H5N1 highlighted the potential impact of influenza virus on humanity. The emergence of this high profile virus stimulated much research towards a better understanding of the key determinants for successful human-to-human transmission and as such has provide...
journal_title：Current opinion in chemical biology
pub_type： 杂志文章,评审
doi：10.1016/j.cbpa.2008.01.036
更新日期：2008-02-01 00:00:00
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journal_title：Current opinion in chemical biology
pub_type： 杂志文章,评审
doi：10.1016/j.cbpa.2010.07.002
更新日期：2010-12-01 00:00:00
abstract：:Iron-binding transcription factors are widespread throughout the bacterial world and to date are known to bind several types of cofactors, such as Fe2+, heme, or iron-sulfur clusters. The known chemistry of these cofactors is exploited by transcription factors, including Fur, FNR, and NsrR, to sense molecules such as ...
journal_title：Current opinion in chemical biology
pub_type： 杂志文章,评审
doi：10.1016/j.cbpa.2011.01.006
更新日期：2011-04-01 00:00:00
abstract：:RNA editing in kinetoplastids involves post-transcriptional insertion and deletion of uridylates (Us) to produce mature mitochondrial mRNAs with sequences specified by trans acting small guide RNAs. In vitro studies indicate the reaction pathway involves endonucleolytic cleavage of the precursor mRNA at the editing si...
journal_title：Current opinion in chemical biology
pub_type： 杂志文章,评审
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journal_title：Current opinion in chemical biology
pub_type： 杂志文章,评审
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journal_title：Current opinion in chemical biology
pub_type： 杂志文章,评审
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journal_title：Current opinion in chemical biology
pub_type： 杂志文章,评审
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更新日期：2003-04-01 00:00:00
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journal_title：Current opinion in chemical biology
pub_type： 杂志文章,评审
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更新日期：2004-06-01 00:00:00
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journal_title：Current opinion in chemical biology
pub_type： 杂志文章,评审
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更新日期：2020-10-01 00:00:00
abstract：:Covalent attachment of glycosylphosphatidylinositols (GPIs) to the protein C-terminus is one of the most common posttranslational modifications in eukaryotic cells. In addition to anchoring surface proteins to the cell membrane, GPIs also have many other important biological functions, determined by their unique struc...
journal_title：Current opinion in chemical biology
pub_type： 杂志文章,评审
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更新日期：2013-12-01 00:00:00
abstract：:Protein citrullination is a post-translational modification of arginine that is catalyzed by the Protein Arginine Deiminase (PAD) family of enzymes. Aberrantly increased citrullination is associated with a host of inflammatory diseases and cancer and PAD inhibitors have shown remarkable efficacy in a range of diseases...
journal_title：Current opinion in chemical biology
pub_type： 杂志文章,评审
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abstract：:The number of new chemical entities has remained rather constant (averaging 37 per year) in the past decade, despite the multiple-fold increase in the number of compounds that are being made and tested. Chemical space requires novel methods that can handle the increasing number of potentially accessible molecules. Nei...
journal_title：Current opinion in chemical biology
pub_type： 杂志文章,评审
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更新日期：2002-06-01 00:00:00
abstract：:Recent uses of phage-displayed combinatorial peptide and cDNA libraries have proven invaluable in mapping protein-protein interactions, protein-drug interactions, and the generation of 'molecular therapeutics'. This article reviews some of the findings of the past year and points out some of the pros and cons of phage...
journal_title：Current opinion in chemical biology
pub_type： 杂志文章,评审
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更新日期：2002-02-01 00:00:00
abstract：:Signal amplification in conventional enzyme-based biosensors is not high enough to achieve the ultrasensitive detection of biomolecules. In recent years, signal amplification has been improved by combining enzymatic reactions with redox cycling or employing multienzyme labels per detection probe. Electrochemical-chemi...
journal_title：Current opinion in chemical biology
pub_type： 杂志文章,评审
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更新日期：2012-08-01 00:00:00
abstract：:There is currently intense interest in unravelling the modus operandi of type I modular polyketide synthases in order to lay the ground work for their use in the combinatorial biosynthesis of new bioactive molecules. Much of our knowledge is derived from studies on 6-deoxyerythronolide B (DEBS), the enzyme assembling ...
journal_title：Current opinion in chemical biology
pub_type： 杂志文章,评审
doi：10.1016/s1367-5931(99)00014-9
更新日期：1999-10-01 00:00:00
