First-in-human evaluation of the novel mitochondrial complex I inhibitor ASP4132 for treatment of cancer

2021 ◽  
Author(s):  
Filip Janku ◽  
Patricia LoRusso ◽  
Aaron S. Mansfield ◽  
Rita Nanda ◽  
Alexander Spira ◽  
...  
Keyword(s):  
Complex I ◽  
Mitochondrial Complex I ◽  
The Novel ◽  
Mitochondrial Complex ◽  
Human Evaluation ◽  
Mitochondrial Complex I Inhibitor

scholarly journals Modulation of autophagy by the novel mitochondrial complex I inhibitor Authipyrin

2019 ◽  
Vol 27 (12) ◽  
pp. 2444-2448 ◽  
Author(s):  
Nadine Kaiser ◽  
Dale Corkery ◽  
Yaowen Wu ◽  
Luca Laraia ◽  
Herbert Waldmann
Keyword(s):  
Complex I ◽  
Mitochondrial Complex I ◽  
The Novel ◽  
Mitochondrial Complex ◽  
Mitochondrial Complex I Inhibitor

scholarly journals The Putative Drp1 Inhibitor mdivi-1 Is a Reversible Mitochondrial Complex I Inhibitor that Modulates Reactive Oxygen Species

2017 ◽  
Vol 40 (6) ◽  
pp. 583-594.e6 ◽  
Author(s):  
Evan A. Bordt ◽  
Pascaline Clerc ◽  
Brian A. Roelofs ◽  
Andrew J. Saladino ◽  
László Tretter ◽  
...  
Keyword(s):  
Reactive Oxygen Species ◽  
Complex I ◽  
Reactive Oxygen ◽  
Mitochondrial Complex I ◽  
Oxygen Species ◽  
Mitochondrial Complex ◽  
Mitochondrial Complex I Inhibitor

P47 Mutations in the novel chaperone FOXRED1 cause mitochondrial complex I deficiency

2011 ◽  
Vol 21 ◽  
pp. S19
Author(s):  
E. Fassone ◽  
A.J. Duncan ◽  
J.-W. Taanman ◽  
A.T. Pagnamenta ◽  
M. Sadowski ◽  
...  
Keyword(s):  
Complex I ◽  
Mitochondrial Complex I ◽  
The Novel ◽  
Mitochondrial Complex ◽  
Complex I Deficiency

The effect of mitochondrial complex I inhibitor on longevity of short-lived and long-lived seed beetles and its mitonuclear hybrids

2014 ◽  
Vol 15 (5) ◽  
pp. 487-501 ◽  
Author(s):  
Darka Šešlija Jovanović ◽  
Mirko Đorđević ◽  
Uroš Savković ◽  
Jelica Lazarević
Keyword(s):  
Complex I ◽  
Mitochondrial Complex I ◽  
Mitochondrial Complex ◽  
Seed Beetles ◽  
Mitochondrial Complex I Inhibitor

Chemical Modification of the Mitochondrial Complex I Inhibitor 1-Trichloromethyl-1,2,3,4-tetrahydro-β-carboline: Synthesis and Evaluation of N-Alkanoyl Derivatives

2000 ◽  
Vol 55 (7-8) ◽  
pp. 620-630 ◽  
Author(s):  
Gerhard Bringmann ◽  
Doris Feineis ◽  
Ralf God ◽  
Ralph Brückner ◽  
Jens Achim-Protzen ◽  
...  
Keyword(s):  
Complex I ◽  
Mitochondrial Complex I ◽  
Mitochondrial Complex ◽  
Inhibitory Effects ◽  
Trichloromethyl Group ◽  
Hydrophobic Portion ◽  
Complex I Activity ◽  
Mitochondrial Complex I Inhibitor ◽  
Lipophilic Character

Abstract Several N-alkanoyl derivatives (4-9 and 13-16) of the potent mitochondrial complex I inhibitor TaClo (1-trichlorom ethyl-1,2,3,4-tetrahydro-β-carboline, 2) have been synthesized in order to elucidate the role of hydrophobic portion in the inhibitory action. Using rat brain homogenates or submitochondrial particles, the inhibitory effects of these compounds towards NADH-ubiquinone reductase (complex I) activity indeed appeared to correlate quite strongly with their lipophilic character. An X-ray structure analysis, exemplarily performed for N-acetyl-TaClo (4), revealed the N-substituent of such chlorinated agents to be dramatically pushed out of the β-carboline ring ‘plane’ due to the high steric demand of the huge trichloromethyl group at C-1.

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