Structurally Simplified Multifunctional Radical Quenchers

Sidney Hecht (Inventor)

Research output: Patent

Abstract

Mitochondrial diseases are a group of disorders associated with dysfunctional mitochondria, often caused by genetic mutations to mitochondrial DNA. Mitochondrial defects are damaging, particularly to tissues with high energy demands such as neural and muscle tissues. Energetic defects have been implicated in forms of movement disorders, cardiomyopathy, myopathy, blindness and deafness. Membrane-penetrating antioxidants are often prescribed but treatment options are limited. There have been extensive efforts to find alternative, synthetic antioxidants with superior activities and simplified synthesis routes. Researchers at the Biodesign Institute of Arizona State University have developed methods for designing and optimizing antioxidant analogs which may be useful for the treatment of mitochondrial diseases. Additionally they have identified promising coenzyme Q10 analogs as well as several novel lipophilic analogs with facile approaches to their synthesis. The coenzyme Q10 analogs act as radical quenchers while augmenting ATP production. The lipophilic analogs suppress ROS levels in cultured cells, and quench the peroxidation of mitochondrial membranes. Moreover, the lipophilic compounds function catalytically, thus increasing their potency of action. These inventions promise to help researchers more efficiently identify therapies for mitochondrial diseases as well as offers several candidates that have shown very promising therapeutic effects. Potential Applications Platform for identifying and optimizing novel antioxidant analogs Therapeutic candidates for Mitochondrial Diseases such as: Friedreich's ataxia Leber's Hereditary Optic Neuropathy Kearns-Sayre Syndrome MELAS (Mitochondrial Encephalomyopathy with Lactic Acidosis and Stroke-like Episodes) Benefits and Advantages Coenzyme Q10 Analogs: Quenching of reactive oxygen species (ROS) and carbon-centered lipid radicals Augmentation of ATP production Antioxidant Lipophilic Analogs: Multifunctional radical quenchers Simplified synthesis routes - five or fewer steps More effective suppression of autoxidation of methyl linoleate over a-tocopherol Catalytic functionality to improve potency of action Augmentation of ATP production Dowload Original PDF For more information about the inventor(s) and their research, please see Dr. Hecht's departmental webpage
Original languageEnglish (US)
StatePublished - Jan 10 2012

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coenzyme Q10
Mitochondrial Diseases
Antioxidants
MELAS Syndrome
Adenosine Triphosphate
Reactive Oxygen Species
Deaf-Blind Disorders
Kearns-Sayre Syndrome
Inventors
Research Personnel
Leber's Hereditary Optic Atrophy
Friedreich Ataxia
Tocopherols
Movement Disorders
Mitochondrial Membranes
Therapeutic Uses
Muscular Diseases
Therapeutics
Cardiomyopathies
Mitochondrial DNA

Cite this

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abstract = "Mitochondrial diseases are a group of disorders associated with dysfunctional mitochondria, often caused by genetic mutations to mitochondrial DNA. Mitochondrial defects are damaging, particularly to tissues with high energy demands such as neural and muscle tissues. Energetic defects have been implicated in forms of movement disorders, cardiomyopathy, myopathy, blindness and deafness. Membrane-penetrating antioxidants are often prescribed but treatment options are limited. There have been extensive efforts to find alternative, synthetic antioxidants with superior activities and simplified synthesis routes. Researchers at the Biodesign Institute of Arizona State University have developed methods for designing and optimizing antioxidant analogs which may be useful for the treatment of mitochondrial diseases. Additionally they have identified promising coenzyme Q10 analogs as well as several novel lipophilic analogs with facile approaches to their synthesis. The coenzyme Q10 analogs act as radical quenchers while augmenting ATP production. The lipophilic analogs suppress ROS levels in cultured cells, and quench the peroxidation of mitochondrial membranes. Moreover, the lipophilic compounds function catalytically, thus increasing their potency of action. These inventions promise to help researchers more efficiently identify therapies for mitochondrial diseases as well as offers several candidates that have shown very promising therapeutic effects. Potential Applications Platform for identifying and optimizing novel antioxidant analogs Therapeutic candidates for Mitochondrial Diseases such as: Friedreich's ataxia Leber's Hereditary Optic Neuropathy Kearns-Sayre Syndrome MELAS (Mitochondrial Encephalomyopathy with Lactic Acidosis and Stroke-like Episodes) Benefits and Advantages Coenzyme Q10 Analogs: Quenching of reactive oxygen species (ROS) and carbon-centered lipid radicals Augmentation of ATP production Antioxidant Lipophilic Analogs: Multifunctional radical quenchers Simplified synthesis routes - five or fewer steps More effective suppression of autoxidation of methyl linoleate over a-tocopherol Catalytic functionality to improve potency of action Augmentation of ATP production Dowload Original PDF For more information about the inventor(s) and their research, please see Dr. Hecht's departmental webpage",
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N2 - Mitochondrial diseases are a group of disorders associated with dysfunctional mitochondria, often caused by genetic mutations to mitochondrial DNA. Mitochondrial defects are damaging, particularly to tissues with high energy demands such as neural and muscle tissues. Energetic defects have been implicated in forms of movement disorders, cardiomyopathy, myopathy, blindness and deafness. Membrane-penetrating antioxidants are often prescribed but treatment options are limited. There have been extensive efforts to find alternative, synthetic antioxidants with superior activities and simplified synthesis routes. Researchers at the Biodesign Institute of Arizona State University have developed methods for designing and optimizing antioxidant analogs which may be useful for the treatment of mitochondrial diseases. Additionally they have identified promising coenzyme Q10 analogs as well as several novel lipophilic analogs with facile approaches to their synthesis. The coenzyme Q10 analogs act as radical quenchers while augmenting ATP production. The lipophilic analogs suppress ROS levels in cultured cells, and quench the peroxidation of mitochondrial membranes. Moreover, the lipophilic compounds function catalytically, thus increasing their potency of action. These inventions promise to help researchers more efficiently identify therapies for mitochondrial diseases as well as offers several candidates that have shown very promising therapeutic effects. Potential Applications Platform for identifying and optimizing novel antioxidant analogs Therapeutic candidates for Mitochondrial Diseases such as: Friedreich's ataxia Leber's Hereditary Optic Neuropathy Kearns-Sayre Syndrome MELAS (Mitochondrial Encephalomyopathy with Lactic Acidosis and Stroke-like Episodes) Benefits and Advantages Coenzyme Q10 Analogs: Quenching of reactive oxygen species (ROS) and carbon-centered lipid radicals Augmentation of ATP production Antioxidant Lipophilic Analogs: Multifunctional radical quenchers Simplified synthesis routes - five or fewer steps More effective suppression of autoxidation of methyl linoleate over a-tocopherol Catalytic functionality to improve potency of action Augmentation of ATP production Dowload Original PDF For more information about the inventor(s) and their research, please see Dr. Hecht's departmental webpage

AB - Mitochondrial diseases are a group of disorders associated with dysfunctional mitochondria, often caused by genetic mutations to mitochondrial DNA. Mitochondrial defects are damaging, particularly to tissues with high energy demands such as neural and muscle tissues. Energetic defects have been implicated in forms of movement disorders, cardiomyopathy, myopathy, blindness and deafness. Membrane-penetrating antioxidants are often prescribed but treatment options are limited. There have been extensive efforts to find alternative, synthetic antioxidants with superior activities and simplified synthesis routes. Researchers at the Biodesign Institute of Arizona State University have developed methods for designing and optimizing antioxidant analogs which may be useful for the treatment of mitochondrial diseases. Additionally they have identified promising coenzyme Q10 analogs as well as several novel lipophilic analogs with facile approaches to their synthesis. The coenzyme Q10 analogs act as radical quenchers while augmenting ATP production. The lipophilic analogs suppress ROS levels in cultured cells, and quench the peroxidation of mitochondrial membranes. Moreover, the lipophilic compounds function catalytically, thus increasing their potency of action. These inventions promise to help researchers more efficiently identify therapies for mitochondrial diseases as well as offers several candidates that have shown very promising therapeutic effects. Potential Applications Platform for identifying and optimizing novel antioxidant analogs Therapeutic candidates for Mitochondrial Diseases such as: Friedreich's ataxia Leber's Hereditary Optic Neuropathy Kearns-Sayre Syndrome MELAS (Mitochondrial Encephalomyopathy with Lactic Acidosis and Stroke-like Episodes) Benefits and Advantages Coenzyme Q10 Analogs: Quenching of reactive oxygen species (ROS) and carbon-centered lipid radicals Augmentation of ATP production Antioxidant Lipophilic Analogs: Multifunctional radical quenchers Simplified synthesis routes - five or fewer steps More effective suppression of autoxidation of methyl linoleate over a-tocopherol Catalytic functionality to improve potency of action Augmentation of ATP production Dowload Original PDF For more information about the inventor(s) and their research, please see Dr. Hecht's departmental webpage

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