Isolation of High‐Affinity Trypsin Inhibitors from a DNA‐Encoded Chemical Library

Melkko, Samu; Zhang, Yixin; Dumelin, Christoph E.; Scheuermann, Jörg; Neri, Dario

doi:10.1002/anie.200700654

Cited by 104 publications

(72 citation statements)

References 18 publications

(27 reference statements)

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“…These fragments are then covalently coupled using a variety of linkers, and the resulting compounds are assayed without the DNA barcodes to discover linker architectures optimal for binding. Using ESAC, Neri and coworkers discovered higher-affinity inhibitors of trypsin [26] and MMP-3 [9]. …”

Section: In Vitro Selection Methods For Ligand Discoverymentioning

confidence: 99%

Novel selection methods for DNA-encoded chemical libraries

Chan

McGregor

Liu

2015

Current Opinion in Chemical Biology

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Driven by the need for new compounds to serve as biological probes and leads for therapeutic development and the growing accessibility of DNA technologies including high-throughput sequencing, many academic and industrial groups have begun to use DNA-encoded chemical libraries as a source of bioactive small molecules. In this review, we describe the technologies that have enabled the selection of compounds with desired activities from these libraries. These methods exploit the sensitivity of in vitro selection coupled with DNA amplification to overcome some of the limitations and costs associated with conventional screening methods. In addition, we highlight newer techniques with the potential to be applied to the high-throughput evaluation of DNA-encoded chemical libraries.

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Section: In Vitro Selection Methods For Ligand Discoverymentioning

confidence: 99%

Novel selection methods for DNA-encoded chemical libraries

Chan

McGregor

Liu

2015

Current Opinion in Chemical Biology

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“…Following addition of a small molecule building block to the scaffold core, another DNA tag which encodes the identity of the chemical building block is ligated to the headpiece. This process is repeated for several cycles to produce vary large combinatorial libraries each containing unique DNA tags [17].…”

Section: Nucleic Acid Based Methodsmentioning

confidence: 99%

Molecular Nanobiotechnological Approaches for the Detection and Therapy of Prion Related Diseases

P¹,

Thampy²,

Venugopalan³

et al. 2012

Nano BioMed ENG

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Prion diseases are associated with the accumulation in the brain of an abnormal, protease resistant isoform of a host encoded glycoprotein known as prion protein (PrP). Nanotechnology in combination with biotechniques promises a broad spectrum of highly innovative approaches for overcoming the challenges posed by the prions. Recent advances in molecular nanobiotechnology have brought in the potential of molecular targeting in diagnosis and therapies of various diseases. Their high binding sensitivity and specificity added by their small size have favored the identification by in vitro protocols. Molecular targeting has initiated exciting technologies based on conjugation of biomolecules to nanoparticles. This review article is an extensive study of various research oriented nanobiotechnological protocols for rapid identification and cure for prion diseases both at in vivo and in vitro options.

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“…Once pairs of protein-binding head-groups are identified by the DNA assembly method, then the binding moieties can be incorporated into short covalent scaffolds. This strategy has been successfully used to identify strong-binding bidentate ligands for a variety of proteins, including streptavidin (86), matrix metalloproteinase-3 (87), trypsin (88), human serum albumin and carbonic anhydrase-II (89), and a variety of kinases including VEGFR2 (90). …”

Section: Multivalent Protein Binding Via On Self Assemblymentioning

confidence: 99%

Oligonucleotide-based systems for input-controlled and non-covalently regulated protein binding

Battle¹,

Chu²,

Jayawickramarajah³

2013

Supramolecular Chemistry

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Supramolecular chemists continuously take inspiration from complex biological systems to develop functional molecules involved in molecular recognition and self-assembly. In this regard, “smart” synthetic molecules that emulate allosteric proteins are both exciting and challenging, since many allosteric proteins can be considered as molecular switches that bind to other protein targets in a non-covalent fashion, and importantly, are capable of having their output activity controlled by prior binding to input molecules. This review discusses the foundations and passage toward the development of non-covalently operated oligonucleotide-based systems with protein-binding capacity that can be precisely regulated in an input-controlled manner.

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Isolation of High‐Affinity Trypsin Inhibitors from a DNA‐Encoded Chemical Library

Cited by 104 publications

References 18 publications

Novel selection methods for DNA-encoded chemical libraries

Novel selection methods for DNA-encoded chemical libraries

Molecular Nanobiotechnological Approaches for the Detection and Therapy of Prion Related Diseases

Oligonucleotide-based systems for input-controlled and non-covalently regulated protein binding

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