scholarly journals Dual inhibitors of LSD1 and spermine oxidase

MedChemComm ◽  
2019 ◽  
Vol 10 (5) ◽  
pp. 778-790 ◽  
Author(s):  
Steven Holshouser ◽  
Matthew Dunworth ◽  
Tracy Murray-Stewart ◽  
Yuri K. Peterson ◽  
Pieter Burger ◽  
...  
Keyword(s):  
Spermine Oxidase ◽  
Dual Inhibitors ◽  
Acetylpolyamine Oxidase

Dual inhibitors of LSD1 and SMOX, with no activity against N1-acetylpolyamine oxidase (PAOX).

scholarly journals Polyamine catabolism and disease

2009 ◽  
Vol 421 (3) ◽  
pp. 323-338 ◽  
Author(s):  
Robert A. Casero ◽  
Anthony E. Pegg
Keyword(s):  
Dominant Role ◽  
Therapeutic Benefit ◽  
Spermine Oxidase ◽  
Polyamine Catabolism ◽  
Disease States ◽  
Disease Aetiology ◽  
Multiple Cell ◽  
Druggable Targets ◽  
Acetylpolyamine Oxidase ◽  
Insight Into

In addition to polyamine homoeostasis, it has become increasingly clear that polyamine catabolism can play a dominant role in drug response, apoptosis and the response to stressful stimuli, and contribute to the aetiology of several pathological states, including cancer. The highly inducible enzymes SSAT (spermidine/spermine N1-acetyltransferase) and SMO (spermine oxidase) and the generally constitutively expressed APAO (N1-acetylpolyamine oxidase) appear to play critical roles in many normal and disease processes. The dysregulation of polyamine catabolism frequently accompanies several disease states and suggests that such dysregulation may both provide useful insight into disease mechanism and provide unique druggable targets that can be exploited for therapeutic benefit. Each of these enzymes has the potential to alter polyamine homoeostasis in response to multiple cell signals and the two oxidases produce the reactive oxygen species H2O2 and aldehydes, each with the potential to produce pathological states. The activity of SSAT provides substrates for APAO or substrates for the polyamine exporter, thus reducing the intracellular polyamine concentration, the net effect of which depends on the magnitude and rate of any increase in SSAT. SSAT may also influence cellular metabolism via interaction with other proteins and by perturbing the content of acetyl-CoA and ATP. The goal of the present review is to cover those aspects of polyamine catabolism that have an impact on disease aetiology or treatment and to provide a solid background in this ever more exciting aspect of polyamine biology.

scholarly journals Development of Irreversible Inactivators of Spermine Oxidase and N1-Acetylpolyamine Oxidase

2014 ◽  
Vol 37 (3) ◽  
pp. 475-480 ◽  
Author(s):  
Shun-suke Moriya ◽  
Toshiyuki Miura ◽  
Koichi Takao ◽  
Yoshiaki Sugita ◽  
Keijiro Samejima ◽  
...  
Keyword(s):  
Spermine Oxidase ◽  
Acetylpolyamine Oxidase

The Glu216/Ser218 pocket is a major determinant of spermine oxidase substrate specificity

2014 ◽  
Vol 461 (3) ◽  
pp. 453-459 ◽  
Author(s):  
Manuela Cervelli ◽  
Emanuela Angelucci ◽  
Pasquale Stano ◽  
Loris Leboffe ◽  
Rodolfo Federico ◽  
...  
Keyword(s):  
Substrate Specificity ◽  
Oxidase Activity ◽  
Major Determinant ◽  
Spermine Oxidase ◽  
Acetylpolyamine Oxidase ◽  
Specific Inhibitors

Mutation of spermine oxidase Glu216/Ser218 into the paralogue acetylpolyamine oxidase residues endows spermine oxidase with acetylpolyamine oxidase activity. Glu216 and Ser218 are major determinants of spermine oxidase substrate specificity. This finding will allow for the design of specific inhibitors for these enzymes.

Discovery of COX-1 and 5-LOX dual inhibitors by UHPLC-HRFTMS-metabolomics

Planta Medica ◽  
2016 ◽  
Vol 81 (S 01) ◽  
pp. S1-S381
Author(s):  
DPV Faleiro ◽  
FB Da Costa
Keyword(s):  
Dual Inhibitors ◽  
Cox 1

Virtual Screening for the Development of Dual-Inhibitors Targeting Topoisomerase IB and Tyrosyl-DNA Phosphodiesterase 1

2017 ◽  
Vol 18 (5) ◽  
pp. 544-555 ◽  
Author(s):  
Francesca Cardamone ◽  
Simone Pizzi ◽  
Federico Iacovelli ◽  
Mattia Falconi ◽  
Alessandro Desideri
Keyword(s):  
Virtual Screening ◽  
Topoisomerase Ib ◽  
Dual Inhibitors

Novel Dual Inhibitors of Secretory Phospholipase A2 and Sphingomyelin Synthase: Design, Synthesis and Evaluation

2016 ◽  
Vol 13 (10) ◽  
pp. 1025-1032 ◽  
Author(s):  
Haojun Gong ◽  
Lu Zhou ◽  
Deyong Ye ◽  
Xing Gao ◽  
Yali Li ◽  
...  
Keyword(s):  
Phospholipase A2 ◽  
Secretory Phospholipase A2 ◽  
Design Synthesis ◽  
Secretory Phospholipase ◽  
Sphingomyelin Synthase ◽  
Dual Inhibitors
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