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Literature DB >> 32178974

Synthesis and pharmacokinetic study of a ¹¹C-labeled cholesterol 24-hydroxylase inhibitor using 'in-loop' [¹¹C]CO₂ fixation method.

Zhen Chen¹, Jiahui Chen¹, Natalia Mast², Jian Rong¹, Xiaoyun Deng¹, Tuo Shao¹, Hualong Fu¹, Qingzhen Yu¹, Jiyun Sun¹, Yihan Shao³, Lee Josephson¹, Thomas Lee Collier¹, Irina Pikuleva², Steven H Liang⁴.

Abstract

Cholesterol 24-hydroxylase, also known as CYP46A1 (EC 1.14.13.98), is a monooxygenase and a member of the cytochrome P450 family. CYP46A1 is specifically expressed in the brain where it controls cholesterol elimination by producing 24S-hydroxylcholesterol (24-HC) as the major metabolite. Modulation of CYP46A1 activity may affect Aβ deposition and p-tau accumulation by changing 24-HC formation, which thereafter serves as potential therapeutic pathway for Alzheimer's disease. In this work, we showcase the efficient synthesis and preliminary pharmacokinetic evaluation of a novel cholesterol 24-hydroxylase inhibitor 1 for use in positron emission tomography.

Entities: Chemical Disease Gene Species

Keywords: Alzheimer’s disease; CYP46A1; Cholesterol 24-hydroxylase; Positron emission tomography; [(11)C]CO(2) fixation

Mesh：

Substances：

Year: 2020 PMID： 32178974 PMCID： PMC7196435 DOI： 10.1016/j.bmcl.2020.127068

Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823

31 in total

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Review 2. (11)C[double bond, length as m-dash]O bonds made easily for positron emission tomography radiopharmaceuticals.

Authors: Benjamin H Rotstein; Steven H Liang; Michael S Placzek; Jacob M Hooker; Antony D Gee; Frédéric Dollé; Alan A Wilson; Neil Vasdev
Journal: Chem Soc Rev Date: 2016-08-22 Impact factor: 54.564

3. CYP46A1 inhibition, brain cholesterol accumulation and neurodegeneration pave the way for Alzheimer's disease.

Authors: Fathia Djelti; Jerome Braudeau; Eloise Hudry; Marc Dhenain; Jennifer Varin; Ivan Bièche; Catherine Marquer; Farah Chali; Sophie Ayciriex; Nicolas Auzeil; Sandro Alves; Dominique Langui; Marie-Claude Potier; Olivier Laprevote; Michel Vidaud; Charles Duyckaerts; Richard Miles; Patrick Aubourg; Nathalie Cartier
Journal: Brain Date: 2015-07-02 Impact factor: 13.501

Review 4. Chemistry for Positron Emission Tomography: Recent Advances in ¹¹ C-, ¹⁸ F-, ¹³ N-, and ¹⁵ O-Labeling Reactions.

Authors: Xiaoyun Deng; Jian Rong; Lu Wang; Neil Vasdev; Lei Zhang; Lee Josephson; Steven H Liang
Journal: Angew Chem Int Ed Engl Date: 2019-01-14 Impact factor: 15.336

5. Cholesterol-metabolizing enzyme cytochrome P450 46A1 as a pharmacologic target for Alzheimer's disease.

Authors: Natalia Mast; Aicha Saadane; Ana Valencia-Olvera; James Constans; Erin Maxfield; Hiroyuki Arakawa; Young Li; Gary Landreth; Irina A Pikuleva
Journal: Neuropharmacology Date: 2017-06-24 Impact factor: 5.250

Review 6. Cholesterol 24-Hydroxylation by CYP46A1: Benefits of Modulation for Brain Diseases.

Authors: Alexey M Petrov; Irina A Pikuleva
Journal: Neurotherapeutics Date: 2019-07 Impact factor: 7.620

Review 7. Determination of lipophilicity and its use as a predictor of blood-brain barrier penetration of molecular imaging agents.

Authors: Rikki N Waterhouse
Journal: Mol Imaging Biol Date: 2003 Nov-Dec Impact factor: 3.488

8. Association between a T/C polymorphism in intron 2 of cholesterol 24S-hydroxylase gene and Alzheimer's disease in Chinese.

Authors: Binbin Wang; Chuanfang Zhang; Weidong Zheng; Zeping Lu; Chenguang Zheng; Ze Yang; Li Wang; Feng Jin
Journal: Neurosci Lett Date: 2004-10-14 Impact factor: 3.046

Review 9. Cholesterol metabolism and homeostasis in the brain.

Authors: Juan Zhang; Qiang Liu
Journal: Protein Cell Date: 2015-02-15 Impact factor: 14.870

Review 10. Loss of Mevalonate/Cholesterol Homeostasis in the Brain: A Focus on Autism Spectrum Disorder and Rett Syndrome.

Authors: Marco Segatto; Claudia Tonini; Frank W Pfrieger; Viviana Trezza; Valentina Pallottini
Journal: Int J Mol Sci Date: 2019-07-05 Impact factor: 5.923

1 in total

Review 1. Cholesterol Hydroxylating Cytochrome P450 46A1: From Mechanisms of Action to Clinical Applications.

Authors: Irina A Pikuleva; Nathalie Cartier
Journal: Front Aging Neurosci Date: 2021-07-08 Impact factor: 5.750