Modified minimal-size fragments of heparan sulfate as inhibitors of endosulfatase-2 (Sulf-2)

文献情報

出版日 2023-11-07

DOI 10.1039/D3CC02565A

インパクトファクター 6.222

著者

Alice Kennett, Sven Epple, Gabriella van der Valk, Irene Georgiou, Evelyne Gout, Romain R. Vivès

原文を見る

要旨

Sulf-2 has been identified as a putative target for anticancer therapies. Here we report the design and synthesis of sulfated disaccharide inhibitors based on IdoA(2S)-GlcNS(6S). Trisulfated disaccharide inhibitor IdoA(2S)-GlcNS(6Sulfamate) demonstrated potent Sulf-2 inhibition. The IC50 value was determined to be 39.8 μM ± 18.3, which is comparable to a tetrasaccharide inhibitor of HSulf-1 reported in the literature. We propose that the disaccharide IdoA(2S)-GlcNS(6S) is the shortest fragment size required for effective inhibition of the Sulfs.

掲載誌

Chemical Communications

CiteScore: 8.6

自己引用率: 4.7%

年間論文数: 2458

ChemComm publishes urgent research which is of outstanding significance and interest to experts in the field, while also appealing to the journal’s broad chemistry readership. Our communication format is ideally suited to short, urgent studies that are of such importance that they require accelerated publication. Our scope covers all topics in chemistry, and research at the interface of chemistry and other disciplines (such as materials science, nanoscience, physics, engineering and biology) where there is a significant novelty in the chemistry aspects. Major topic areas covered include: Analytical Chemistry Catalysis Chemical Biology and medicinal chemistry Computational Chemistry and Machine Learning Energy and sustainable chemistry Environmental Chemistry Green Chemistry Inorganic Chemistry Materials Chemistry Nanoscience Organic Chemistry Physical Chemistry Polymer Chemistry Supramolecular Chemistry

Modified minimal-size fragments of heparan sulfate as inhibitors of endosulfatase-2 (Sulf-2)

文献情報

おすすめジャーナル

関連文献

Second-generation tricyclic pyrimido-pyrrolo-oxazine mTOR inhibitor with predicted blood–brain barrier permeability

Chemical modulation of Kv7 potassium channels

Discovery of sustainable drugs for Alzheimer's disease: cardanol-derived cholinesterase inhibitors with antioxidant and anti-amyloid properties

Synthesis and evaluation of bis(imino)anthracene derivatives as G-quadruplex ligands

Metabolically stable apelin-analogues, incorporating cyclohexylalanine and homoarginine, as potent apelin receptor activators

Contents list

Synthesis and biological evaluation of N6 derivatives of 8-azapurine as novel antiplatelet agents

Front cover

Expanding the repertoire of methanocarba nucleosides from purinergic signaling to diverse targets

An overview of the development of EED inhibitors to disable the PRC2 function

こちらもおすすめ

カルボニル基が付いた5-氰基-1-{[(2-メチル-2-プロpanyl)オキシ]カーボンイル}1H-吲哚-2-イリド-2-ボリン酸はどのように保存すればよいですか？

tert-ブチル2-クロロメチルピリジン-3-基炭酸エステルの市場動向や研究トレンドはどうですか？

聚二季戊四醇六丙烯酸酯はどの業界で使用されていますか？

1-氯-5-硝基异喹啉の市場動向や研究トレンドはどうですか？

2-チロール-5-メチルスルフェニル-3-trifルオルメチルベンゼンはどのように合成されますか？

p-トールイルマグネシウムブロミドの物理化学的性質は何ですか？

1-(5-甲基-2-硫化素基)プロパン-1-酮の市場動向や研究トレンドはどうですか？

十一碳烯酰甘氨酸を取り扱う際の実験室安全事項は何ですか？

1H,1H-全氟-3,6-二氧杂葵-1-醇を取り扱う際の実験室安全事項は何ですか？

3-(4-(フルオロメチルオキシ)フェニル)-1,2,4-オキサジアゾール-5-カルボハイドライドは安全ですか？

掲載誌

Chemical Communications

おすすめ化合物

4-Bromo-5,7-difluoro-1H-indole

6-(4-Morpholinyl)-1H-purine

Benzyl 2-{[(tert-butoxy)carbonyl]amino}acetate

(5-chloro-3-iodo-2-pyridyl)hydrazine

tert-Butyl 4-chloro-5-methoxypyridin-3-ylcarbamate

おすすめサプライヤー