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Fragment-based discovery enables direct targeting of the melanoma oncogene MITF

In this work, fragments identified by 19F-NMR are optimized into submicromolar binders of the MITF transcription factor. These results support direct targeting of bHLH-LZ DNA binding domains and provide a foundation for the development of new melanoma therapies.

Deborah Castelletti
Jürgen Hinrichs
Wolfgang Jahnke
ResearchOpen Access09 Dec 2025
Nature Communications

Volume: 17, P: 1-18
Discovery of a selective and biologically active low-molecular weight antagonist of human interleukin-1β

Interleukin-1β is a pro-inflammatory cytokine of medical importance. Here the authors describe the discovery of a low-molecular weight compound that antagonizes hIL-1β function in cells, demonstrating the relevance of this discovery for future development of hIL-1β directed therapeutics.

Ulrich Hommel
Konstanze Hurth
Frédéric Bornancin
ResearchOpen Access07 Sept 2023
Nature Communications

Volume: 14, P: 1-13
Author Correction: DCAF1-based PROTACs with activity against clinically validated targets overcoming intrinsic- and acquired-degrader resistance

Martin Schröder
Martin Renatus
Claudio R. Thoma
Amendments and CorrectionsOpen Access19 Aug 2024
Nature Communications

Volume: 15, P: 1-5
DCAF1-based PROTACs with activity against clinically validated targets overcoming intrinsic- and acquired-degrader resistance

Targeted protein degradation (TPD) is a key modality for drug discovery. Here the authors present the discovery and analysis of reversible DCAF1-PROTACs, which show efficacy in cellular environments resistant to VHL-PROTACs or with acquired resistance to CRBN-PROTACs.

Martin Schröder
Martin Renatus
Claudio R. Thoma
ResearchOpen Access04 Jan 2024
Nature Communications

Volume: 15, P: 1-19
Small-molecule factor D inhibitors targeting the alternative complement pathway

A fragment-based design approach identifies reversible inhibitors targeting human protease complement factor D (FD), which is required for amplification of complement C3 signaling. FD inhibitors act as systemic regulators of complement activation in vivo.

Jürgen Maibaum
Sha-Mei Liao
Karen Anderson
Research24 Oct 2016
Nature Chemical Biology

Volume: 12, P: 1105-1110

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Fragment-based discovery enables direct targeting of the melanoma oncogene MITF

Discovery of a selective and biologically active low-molecular weight antagonist of human interleukin-1β

Author Correction: DCAF1-based PROTACs with activity against clinically validated targets overcoming intrinsic- and acquired-degrader resistance

DCAF1-based PROTACs with activity against clinically validated targets overcoming intrinsic- and acquired-degrader resistance

Small-molecule factor D inhibitors targeting the alternative complement pathway

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