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Updated: Sep 10, 2025

Simultaneous Measurement of HDAC1 and HDAC6 Activity in HeLa Cells Using UHPLC-MS
09:20

Simultaneous Measurement of HDAC1 and HDAC6 Activity in HeLa Cells Using UHPLC-MS

Published on: August 10, 2017

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HDAC6 阻害剤の薬理学プロファイルは,CAP グループ修正によって改善された

Olasunkanmi O Olaoye1,2, Fettah Erdogan1,2, Maria Gracia-Hernandez3

  • 1Department of Chemical and Physical Sciences, University of Toronto Mississauga, 3359 Mississauga Rd N., Mississauga, Ontario L5L 1C6, Canada.

Journal of medicinal chemistry
|August 27, 2025
PubMed
まとめ

ハイドロキサム酸 (HA) ベースのHDAC阻害剤のキャップグループを最適化することで,薬理学的なプロファイルが著しく改善されました. アナログ14は,前臨床モデルにおいて,血濃度上昇と強力な腫瘍増殖阻害を示した.

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Assays for Validating Histone Acetyltransferase Inhibitors

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Examination of Proteins Bound to Nascent DNA in Mammalian Cells Using BrdU-ChIP-Slot-Western Technique

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Nonlinear Pharmacokinetics: Dependence of Elimination Half-Life and Dose Clearance

The elimination half-life and drug clearance of drugs following nonlinear kinetics can vary with dosage. The Michaelis-Menten parameters and drug concentration influence these factors. As the dose increases, the elimination half-life tends to lengthen, resulting in a reduction in clearance and a disproportionately larger area under the curve. The total clearance can be derived from the Michaelis-Menten equation for drugs following a one-compartment model.
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Phase II reactions are essential for the detoxification and elimination of drugs from the body. These reactions involve the conjugation of parent drugs or their phase I metabolites with endogenous molecules, resulting in more hydrophilic drug conjugates. The primary conjugation reactions in this phase are sulfation and glucuronidation. Both sulfation and glucuronidation typically produce biologically inactive metabolites. However, in some cases involving prodrugs, active metabolites may be...
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