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The Chemistry and Biology of Alkannin, Shikonin, and Related Naphthazarin Natural Products.
Wound healing properties of plant extracts that contain the naphthoquinone natural products alkannin (1) and shikonin (2) have been known for many centuries. More recently, the biological propertiesExpand
Aldehyde Dehydrogenase Inhibitors: a Comprehensive Review of the Pharmacology, Mechanism of Action, Substrate Specificity, and Clinical Application
Aldehyde dehydrogenases (ALDHs) belong to a superfamily of enzymes that play a key role in the metabolism of aldehydes of both endogenous and exogenous derivation. The human ALDH superfamilyExpand
A common pharmacophore for epothilone and taxanes: molecular basis for drug resistance conferred by tubulin mutations in human cancer cells.
The epothilones are naturally occurring antimitotic drugs that share with the taxanes a similar mechanism of action without apparent structural similarity. Although photoaffinity labeling andExpand
A chemical, genetic, and structural analysis of the nuclear bile acid receptor FXR.
The farnesoid X receptor (FXR) functions as a bile acid (BA) sensor coordinating cholesterol metabolism, lipid homeostasis, and absorption of dietary fats and vitamins. However, BAs are poor reagentsExpand
Strategic applications of named reactions in organic synthesis: background and detailed mechanisms
I. Foreword by E. J. Corey II Introduction by K. C. Nicolaou III. Expand
Interaction of epothilone analogs with the paclitaxel binding site: relationship between binding affinity, microtubule stabilization, and cytotoxicity.
The interactions of epothilone analogs with the paclitaxel binding site of microtubules were studied. The influence of chemical modifications in the C15 side chain and in C12 on binding affinity andExpand
Total synthesis of taxol
TAXOL1–4, a substance originally isolated from the Pacific yew tree (Taxus brevifolia) more than two decades ago, has recently been approved for the clinical treatment of cancer patients. Hailed asExpand
Enhanced microtubule-dependent trafficking and p53 nuclear accumulation by suppression of microtubule dynamics
The tumor suppressor protein p53 localizes to microtubules (MT) and, in response to DNA damage, is transported to the nucleus via the MT minus-end-directed motor protein dynein. Dynein is alsoExpand
Identification of a Novel Small Molecule HIF-1α Translation Inhibitor
Purpose: Hypoxia inducible factor-1 (HIF-1), the central mediator of the cellular response to low oxygen, functions as a transcription factor for a broad range of genes that provide adaptiveExpand
Chasing molecules that were never there: misassigned natural products and the role of chemical synthesis in modern structure elucidation.
Over the course of the past half century, the structural elucidation of unknown natural products has undergone a tremendous revolution. Before World War II, a chemist would have relied almostExpand