Synthetic probes and chemical tools in sphingolipid research

Proteolysis-targeting chimeras are a new modality of chemical tools and potential therapeutics involving the induction of protein degradation. Cyclin-dependent kinase (CDK) protein, which is involved in cycles and transcription cycles, participates in regulation of the cell cycle, transcription and splicing. Proteolysis-targeting chimeras targeting CDKs show several advantages over traditional CDK small-molecule inhibitors in potency, selectivity and drug resistance. In addition, the discovery of molecule glues promotes the development of CDK degraders. Herein, the authors describe the existing CDK degraders and focus on the discussion of the structural characteristics and design of these degraders.

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Modulating the masters: chemical tools to dissect CBP and p300 function

Current Opinion in Chemical Biology ◽

10.1016/j.cbpa.2018.06.005 ◽

2018 ◽

Vol 45 ◽

pp. 195-203 ◽

Cited By ~ 16

Author(s):

Meghan E Breen ◽

Anna K Mapp

Keyword(s):

Chemical Tools

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Ionic liquids as bioactive chemical tools for use in agriculture and the preservation of agricultural products

Green Chemistry ◽

10.1039/c8gc01424h ◽

2018 ◽

Vol 20 (21) ◽

pp. 4764-4789 ◽

Cited By ~ 18

Author(s):

Adrian Zajac ◽

Rafal Kukawka ◽

Anna Pawlowska-Zygarowicz ◽

Olga Stolarska ◽

Marcin Smiglak

Keyword(s):

Ionic Liquids ◽

Recent Progress ◽

Agricultural Products ◽

Bioactive Components ◽

Chemical Tools ◽

Made In

The review presents the recent progress made in the field of ionic liquids bearing bioactive components, with a particular emphasis on their use as chemical tools in agriculture and the preservation of agricultural products.

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Eremophilane-type sesquiterpenes from fungi and their medicinal potential

Biological Chemistry ◽

10.1515/hsz-2017-0171 ◽

2017 ◽

Vol 399 (1) ◽

pp. 13-28 ◽

Cited By ~ 10

Author(s):

Kamila Tomoko Yuyama ◽

Diana Fortkamp ◽

Wolf-Rainer Abraham

Keyword(s):

Fatty Acids ◽

Natural Products ◽

Carbon Skeleton ◽

New Drugs ◽

Special Focus ◽

Bioactive Natural Products ◽

Pharmacokinetic Assessment ◽

Immunomodulatory Properties ◽

Chemical Tools ◽

Subsequent Improvement

AbstractEremophilanes are sesquiterpenes with a rearranged carbon skeleton formed both by plants and fungi, however, almost no plant eremophilanes are found in fungi. These eremophilanes possess mainly phytotoxic, antimicrobial, anticancer and immunomodulatory properties and in this review fungal eremophilanes with bioactivities of potential medicinal applications are reviewed and discussed. A special focus is set on natural products bearing highly functionalized fatty acids at C-1 or C-3 position of the eremophilane backbone. Many of these fatty acids seem to contribute to the bioactivity of the metabolites enhancing the activity of the sesquiterpene moieties. Several approaches for optimization of these natural products for clinical needs and testing of the resulting derivatives are presented and discussed. The combination of identification of bioactive natural products with their subsequent improvement using a variety of genetical or chemical tools and the pharmacokinetic assessment of the products is presented here as a promising approach to new drugs.

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