Advances in targeting 'undruggable'transcription factors with small molecules

MJ Henley, AN Koehler - Nature Reviews Drug Discovery, 2021 - nature.com
Transcription factors (TFs) represent key biological players in diseases including cancer,
autoimmunity, diabetes and cardiovascular disease. However, outside nuclear receptors …

[HTML][HTML] Chemical probes and drug leads from advances in synthetic planning and methodology

CJ Gerry, SL Schreiber - Nature Reviews Drug Discovery, 2018 - nature.com
Screening of small-molecule libraries is a productive method for identifying both chemical
probes of disease-related targets and potential starting points for drug discovery. In this …

Catalytic in vivo protein knockdown by small-molecule PROTACs

DP Bondeson, A Mares, IED Smith, E Ko… - Nature chemical …, 2015 - nature.com
The current predominant therapeutic paradigm is based on maximizing drug-receptor
occupancy to achieve clinical benefit. This strategy, however, generally requires excessive …

Pyrrolidinyl‐spirooxindole natural products as inspirations for the development of potential therapeutic agents

CV Galliford, KA Scheidt - Angewandte Chemie International …, 2007 - Wiley Online Library
Abstract The 3, 3′‐pyrrolidinyl‐spirooxindole unit is a privileged heterocyclic motif that
forms the core of a large family of alkaloid natural products with strong bioactivity profiles …

The emerging role of RNA as a therapeutic target for small molecules

CM Connelly, MH Moon, JS Schneekloth - Cell chemical biology, 2016 - cell.com
Recent advances in understanding different RNAs and unique features of their biology have
revealed a wealth of information. However, approaches to identify small molecules that …

Small molecules of different origins have distinct distributions of structural complexity that correlate with protein-binding profiles

PA Clemons, NE Bodycombe, HA Carrinski… - Proceedings of the …, 2010 - pnas.org
Using a diverse collection of small molecules generated from a variety of sources, we
measured protein-binding activities of each individual compound against each of 100 …

Natürliche pyrrolidinylspirooxindole als vorlagen für die entwicklung medizinischer wirkstoffe

CV Galliford, KA Scheidt - Angewandte Chemie, 2007 - Wiley Online Library
Abstract Das 3, 3′‐Pyrrolidinylspirooxindol‐System ist ein privilegiertes heterocyclisches
Strukturmotiv, das die zentrale Einheit bei einer großen Familie von natürlichen Alkaloiden …

A small molecule that binds Hedgehog and blocks its signaling in human cells

BZ Stanton, LF Peng, N Maloof, K Nakai… - Nature chemical …, 2009 - nature.com
Small-molecule inhibition of extracellular proteins that activate membrane receptors has
proven to be extremely challenging. Diversity-oriented synthesis and small-molecule …

Synthetic ligands for PreQ1 riboswitches provide structural and mechanistic insights into targeting RNA tertiary structure

CM Connelly, T Numata, RE Boer, MH Moon… - Nature …, 2019 - nature.com
Riboswitches are naturally occurring RNA aptamers that regulate gene expression by
binding to specific small molecules. Riboswitches control the expression of essential …

Small-molecule modulators of the Sonic Hedgehog signaling pathway

BZ Stanton, LF Peng - Molecular BioSystems, 2010 - pubs.rsc.org
Sonic hedgehog (Shh) is the most widely characterized of the three vertebrate
Hedgehoghomologs, and is essential for proper embryonic development. Shh binds to its …