scholarly journals Screening of DNA-Encoded Small Molecule Libraries inside a Living Cell

2021 ◽  
Vol 143 (7) ◽  
pp. 2751-2756
Author(s):  
Lars K. Petersen ◽  
Allan B. Christensen ◽  
Jacob Andersen ◽  
Charlotta G. Folkesson ◽  
Ole Kristensen ◽  
...  
Keyword(s):  
Small Molecule ◽  
Living Cell ◽  
Small Molecule Libraries

Pentaerythritol and Its Congeners: Versatile Building Blocks for the Construction of Oligomeric Bioconjugates and Small Molecule Libraries on a Solid Support

2004 ◽  
Vol 8 (11) ◽  
pp. 977-992 ◽  
Author(s):  
Johanna Katajisto ◽  
Petri Heinonen ◽  
Harri Lonnberg
Keyword(s):  
Small Molecule ◽  
Building Blocks ◽  
Solid Support ◽  
Small Molecule Libraries

Towards drugging the ‘undruggable’: enhancing the scaffold diversity of synthetic small molecule screening collections using diversity-oriented synthesis

2013 ◽  
Vol 1 (1) ◽  
Author(s):  
Warren R.J.D. Galloway ◽  
David R. Spring
Keyword(s):  
Small Molecule ◽  
Structural Diversity ◽  
Library Size ◽  
Diversity Oriented Synthesis ◽  
Biological Targets ◽  
Small Molecule Screening ◽  
Chemistry Research ◽  
Large Numbers ◽  
Small Molecule Libraries ◽  
Scaffold Diversity

AbstractMedicinal chemistry research has traditionally focused upon a limited set of biological targets. Many other human disease-related targets have been termed ‘undruggable’ as they have proved largely impervious to modulation by small molecules. However, it is becoming increasingly evident that such targets can indeed be modulated; they are simply being challenged with the wrong types of molecules. Traditionally, screening libraries were composed of large numbers of structurally similar compounds. However, library size is not everything; the structural diversity of the library, which is largely dictated by the range of molecular scaffolds present, is crucial. Diversity-oriented synthesis (DOS) generates small molecule libraries with high levels of scaffold, and thus structural, diversity. Such collections should provide hits against a broad range of targets with high frequency, including ‘undruggable’ targets. Examples in the area of scaffold diversity generation taken from the author’s laboratories are given.

Carbohydrate-Derived Small-Molecule Libraries

2006 ◽  
pp. 165-184
Author(s):  
Armen M. Boldi
Keyword(s):  
Small Molecule ◽  
Small Molecule Libraries

Synthetic approaches toward small molecule libraries

2020 ◽  
pp. 1-34
Author(s):  
Elena Lenci ◽  
Andrea Trabocchi
Keyword(s):  
Small Molecule ◽  
Small Molecule Libraries ◽  
Synthetic Approaches

scholarly journals Sensitive ADAR editing reporter in cancer cells enables high-throughput screening of small molecule libraries

2018 ◽  
Vol 47 (4) ◽  
pp. e22-e22 ◽  
Author(s):  
Kajsa Fritzell ◽  
Li-Di Xu ◽  
Magdalena Otrocka ◽  
Claes Andréasson ◽  
Marie Öhman
Keyword(s):  
Cancer Cells ◽  
Small Molecule ◽  
High Throughput ◽  
High Throughput Screening ◽  
Small Molecule Libraries ◽  
Adar Editing

Using the gini coefficient to measure the chemical diversity of small-molecule libraries

2016 ◽  
Vol 37 (22) ◽  
pp. 2091-2097 ◽  
Author(s):  
Iwona E. Weidlich ◽  
Igor V. Filippov
Keyword(s):  
Small Molecule ◽  
Gini Coefficient ◽  
Chemical Diversity ◽  
The Gini Coefficient ◽  
Small Molecule Libraries

scholarly journals Gypsum-DL: an open-source program for preparing small-molecule libraries for structure-based virtual screening

2019 ◽  
Vol 11 (1) ◽  
Author(s):  
Patrick J. Ropp ◽  
Jacob O. Spiegel ◽  
Jennifer L. Walker ◽  
Harrison Green ◽  
Guillermo A. Morales ◽  
...  
Keyword(s):  
Virtual Screening ◽  
Open Source ◽  
Small Molecule ◽  
Open Source Program ◽  
Source Program ◽  
Small Molecule Libraries

scholarly journals Identification of Bis-Cyclic Guanidines as Antiplasmodial Compounds from Positional Scanning Mixture-Based Libraries

Molecules ◽  
2019 ◽  
Vol 24 (6) ◽  
pp. 1100 ◽  
Author(s):  
David Perry ◽  
Bracken Roberts ◽  
Ginamarie Debevec ◽  
Heather Michaels ◽  
Debopam Chakrabarti ◽  
...  
Keyword(s):  
Small Molecule ◽  
Parallel Synthesis ◽  
Variable Position ◽  
Positional Scanning ◽  
Small Molecule Libraries ◽  
The Individual

The screening of more than 30 million compounds derived from 81 small molecule libraries built on 81 distinct scaffolds identified pyrrolidine bis-cyclic guanidine library (TPI-1955) to be one of the most active and selective antiplasmodial libraries. The screening of the positional scanning library TPI-1955 arranged on four sets of sublibraries (26 + 26 + 26 + 40), totaling 120 samples for testing provided information about the most important groups of each variable position in the TPI-1955 library containing 738,192 unique compounds. The parallel synthesis of the individual compounds derived from the deconvolution of the positional scanning library led to the identification of active selective antiplasmodial pyrrolidine bis-cyclic guanidines.

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