A combined biochemical, structural, and cell biology characterization of dictyostatin is described, which enables an improved understanding of the structural determinants responsible for the high-affinity binding of this anticancer agent to the taxane site in microtubules (MTs). The study reveals that this macrolide is highly optimized for MT binding and that only a few of the structural modifications featured in a library of synthetic analogues resulted in small gains in binding affinity. The high efficiency of the dictyostatin chemotype in overcoming various kinds of clinically relevant resistance mechanisms highlights its potential for therapeutic development for the treatment of drug-resistant tumors. A structural explanation is advance...
SummaryThe microtubule binding affinities of a series of synthetic taxanes have been measured with t...
(Chemical Equation Presented) (-)-16-Normethyldictyostatin has been made by total synthesis and is a...
PHARMACOLOGICAL AND STRUCTURE-ACTIVITY RELATIONSHIP EVALUATION OF MICROTUBULE-STABILIZING AGENTSChar...
A combined biochemical, structural, and cell biology characterization of dictyostatin is described, ...
Compounds that bind to microtubules (MTs) and alter their dynamics are highly sought as a result of ...
(-)-Dictyostatin is a sponge-derived, 22-member macrolactone natural product shown to cause cells to...
Compounds that bind to microtubules (MTs) and alter their dynamics are highly sought as a result of ...
The natural product (--)-dictyostatin is a microtubule-stabilizing agent that potently inhibits the ...
Total syntheses of (-)-dictyostatin, 6,16-bis-epi-dictyostatin, 6,14,19-tris-epi-dictyostatin and a ...
Microtubules are cellular cytoskeletal components that play an integral part in many cell functions....
Total syntheses of (-)-dictyostatin, 6,16-bis-epi-dictyostatin, 6,14,19-tris-epi-dictyostatin, and a...
The natural product ()-dictyostatin is a microtubule-stabilizing agent that potently inhibits the gr...
Dictyostatin (DCT, 1) is a complex, flexible polyketide macrolide that demonstrates potent microtubu...
Dictyostatin (DCT, 1) is a complex, flexible polyketide macrolide that demonstrates potent microtubu...
(-)-Dictyostatin, isolated from a marine sponge, shows potent cancer cell antiproliferative activity...
SummaryThe microtubule binding affinities of a series of synthetic taxanes have been measured with t...
(Chemical Equation Presented) (-)-16-Normethyldictyostatin has been made by total synthesis and is a...
PHARMACOLOGICAL AND STRUCTURE-ACTIVITY RELATIONSHIP EVALUATION OF MICROTUBULE-STABILIZING AGENTSChar...
A combined biochemical, structural, and cell biology characterization of dictyostatin is described, ...
Compounds that bind to microtubules (MTs) and alter their dynamics are highly sought as a result of ...
(-)-Dictyostatin is a sponge-derived, 22-member macrolactone natural product shown to cause cells to...
Compounds that bind to microtubules (MTs) and alter their dynamics are highly sought as a result of ...
The natural product (--)-dictyostatin is a microtubule-stabilizing agent that potently inhibits the ...
Total syntheses of (-)-dictyostatin, 6,16-bis-epi-dictyostatin, 6,14,19-tris-epi-dictyostatin and a ...
Microtubules are cellular cytoskeletal components that play an integral part in many cell functions....
Total syntheses of (-)-dictyostatin, 6,16-bis-epi-dictyostatin, 6,14,19-tris-epi-dictyostatin, and a...
The natural product ()-dictyostatin is a microtubule-stabilizing agent that potently inhibits the gr...
Dictyostatin (DCT, 1) is a complex, flexible polyketide macrolide that demonstrates potent microtubu...
Dictyostatin (DCT, 1) is a complex, flexible polyketide macrolide that demonstrates potent microtubu...
(-)-Dictyostatin, isolated from a marine sponge, shows potent cancer cell antiproliferative activity...
SummaryThe microtubule binding affinities of a series of synthetic taxanes have been measured with t...
(Chemical Equation Presented) (-)-16-Normethyldictyostatin has been made by total synthesis and is a...
PHARMACOLOGICAL AND STRUCTURE-ACTIVITY RELATIONSHIP EVALUATION OF MICROTUBULE-STABILIZING AGENTSChar...