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The Chemistry and Biology of Alkannin, Shikonin, and Related Naphthazarin Natural Products.
- V. Papageorgiou, A. Assimopoulou, E. Couladouros, D. Hepworth, K. Nicolaou
- ChemistryAngewandte Chemie
- 1 February 1999
Wound healing properties of plant extracts that contain the naphthoquinone natural products alkannin and shikonin have been known for many centuries and their production both by cell cultures and chemical synthesis has been studied extensively.
Aldehyde Dehydrogenase Inhibitors: a Comprehensive Review of the Pharmacology, Mechanism of Action, Substrate Specificity, and Clinical Application
The purpose of this review is to establish the current status of pharmacological inhibition of the ALDHs, provide a rationale for the continued development of ALDH isozyme-selective inhibitors, and identify the challenges and potential therapeutic rewards associated with the creation of such agents.
A common pharmacophore for epothilone and taxanes: molecular basis for drug resistance conferred by tubulin mutations in human cancer cells.
- P. Giannakakou, R. Gussio, T. Fojo
- Biology, ChemistryProceedings of the National Academy of Sciences…
- 14 March 2000
The unification of taxane, epothilone, and sarcodictyin chemistries in a single pharmacophore provides a framework to study drug-tubulin interactions that should assist in the rational design of agents targeting tubulin.
A chemical, genetic, and structural analysis of the nuclear bile acid receptor FXR.
Strategic applications of named reactions in organic synthesis: background and detailed mechanisms
This main section includes 250 two-page entries about Named Organic Reactions, which lists the Named Reactions by Synthetic Type and by their Utility.
Cortistatin A is a high-affinity ligand of protein kinases ROCK, CDK8, and CDK11.
- V. Cee, David Y. Chen, Matthew R. Lee, K. Nicolaou
- Biology, ChemistryAngewandte Chemie
- 9 November 2009
It is reported that cortistatin A is a highaffinity ligand for a small set of protein kinases including Rhoassociated, coiled-coil containing protein kinase (ROCK), cyclin-dependent kinase 8 (CDK8), andcyclin- dependent kinase 11 (CDk11) and high affinity for CDK11, which stems from their potential to serve as lead compounds for drug discovery in antiangiogenic cancer chemotherapy.
Identification of a Novel Small Molecule HIF-1α Translation Inhibitor
Results show that KC7F2 is a potent HIF-1 pathway inhibitor and its potential as a cancer therapy agent warrants further study.
Total synthesis of taxol
The total synthesis of taxol is reported by a convergent strategy, which opens a chemical pathway for the production of both the natural product itself and a variety of designed taxoids.
Chasing molecules that were never there: misassigned natural products and the role of chemical synthesis in modern structure elucidation.
It is made the case that imaginative detective work and chemical synthesis still have important roles to play in the process of solving nature's most intriguing molecular puzzles.
Enhanced microtubule-dependent trafficking and p53 nuclear accumulation by suppression of microtubule dynamics
- P. Giannakakou, M. Nakano, T. Fojo
- BiologyProceedings of the National Academy of Sciences…
- 26 July 2002
It is proposed that suppression of MT dynamics by low concentrations of MTCs enhances MT-dependent trafficking toward the minus ends of MTs and facilitates nuclear targeting.