ReviewFuture medicinal chemistry2025
Research status of small molecule inhibitors, probes, and degraders of NSDs: a comprehensive review.
Review in Future medicinal chemistry, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
0 citing papers in PubMed.
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Authors and funding
6 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The nuclear receptor binding SET domain (NSD) family of histone methyltransferases, which comprised NSD1, NSD2, and NSD3. They play a pivotal role in catalyzing mono- and dimethylation of histone H3 at lysine 36 (H3K36me1/2), a modification critical for maintaining chromatin structure and transcriptional fidelity. Dysregulation of NSD enzymes, often through overexpression, mutation, or chromosomal translocation, has been implicated in a broad spectrum of malignancies and various diseases. Due to their critical role in disease pathogenesis and recent technological advances, NSD proteins have become attractive targets for therapeutic intervention. This review highlights recent progress in developing small molecule inhibitors and chemical probes targeting NSD family members, focusing on the catalytic SET domain, the PWWP domain, and other functional motifs. Among these, several chemical classes have been investigated, including quinoline-5,8-dione, 2-aminobenzothiazole, 5-aminonaphthalene, quinazoline, purine, benzoxazinone-cyclopropylamide, and imidazole derivatives. In addition, novel strategies such as protein degradation via PROTACs and dual-target inhibitors are discussed. By systematically summarizing recent advances, this review seeks to facilitate and accelerate the development of effective NSD modulators, ultimately advancing therapeutic options for diseases driven by NSD dysregulation.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.