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Mechanism of substrate transport and inhibition of the human LAT1-4F2hc amino acid transporter

Renhong Yan
Yaning Li
Qiang Zhou
ResearchOpen Access23 Mar 2021
Cell Discovery

Volume: 7, P: 1-8
Unraveling a molecular target of macrolides

Leucascandrolide A and neopeltolide are structurally related natural products with potent growth inhibitory activity. The synthesis of a designed analog of leucascandrolide A and its evaluation in a yeast haploinsufficiency screen has revealed the cytochrome bc₁ complex as a molecular target of these compounds.

Karl-Heinz Altmann
Erick M Carreira
News & Views01 Jul 2008
Nature Chemical Biology

Volume: 4, P: 388-389
Structural basis of small-molecule inhibition of human multidrug transporter ABCG2

Cryo-EM structures of human ABCG2 bound to synthetic derivatives of inhibitor Ko143 or the multidrug resistance modulator tariquidar together with insight into the structure–activity relationship of the Ko143 scaffold provide a basis for the design of novel ABCG2 inhibitors.

Scott M. Jackson
Ioannis Manolaridis
Kaspar P. Locher
Research02 Apr 2018
Nature Structural & Molecular Biology

Volume: 25, P: 333-340
Pyridomycin bridges the NADH- and substrate-binding pockets of the enoyl reductase InhA

Crystal structures reveal that the antitubercular compound pyridomycin blocks binding of the NADH cofactor to the fatty acid synthesis enzyme InhA while also blocking the lipid substrate–binding pocket.

Ruben C Hartkoorn
Florence Pojer
Stewart T Cole
Research01 Dec 2013
Nature Chemical Biology

Volume: 10, P: 96-98
Taxanes convert regions of perturbed microtubule growth into rescue sites

Anticancer drugs such as Taxol can affect microtubule dynamics and organization in cells. Direct visualization of the action of such drugs has shown that they can trigger local and cooperative changes in microtubule lattice and induce formation of stable microtubule regions that promote rescues.

Ankit Rai
Tianyang Liu
Anna Akhmanova
Research09 Dec 2019
Nature Materials

Volume: 19, P: 355-365
A fluorescence anisotropy assay to discover and characterize ligands targeting the maytansine site of tubulin

Microtubule-targeting agents are used successfully as anticancer therapeutics. Here authors develop a fluorescence-anisotropy-based assay to identify and characterize ligands for the maytansine site of tubulin and provide crystal structures of identified ligands in complex with tubulin.

Grégory Menchon
Andrea E. Prota
Michel O. Steinmetz
ResearchOpen Access29 May 2018
Nature Communications

Volume: 9, P: 1-9
Targeting the actin cytoskeleton: selective antitumor action via trapping PKCɛ

F Foerster
S Braig
A M Vollmar
ResearchOpen Access28 Aug 2014
Cell Death & Disease

Volume: 5, P: e1398

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Mechanism of substrate transport and inhibition of the human LAT1-4F2hc amino acid transporter

Unraveling a molecular target of macrolides

Structural basis of small-molecule inhibition of human multidrug transporter ABCG2

Pyridomycin bridges the NADH- and substrate-binding pockets of the enoyl reductase InhA

Taxanes convert regions of perturbed microtubule growth into rescue sites

A fluorescence anisotropy assay to discover and characterize ligands targeting the maytansine site of tubulin

Targeting the actin cytoskeleton: selective antitumor action via trapping PKCɛ

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