Inhibition of human constitutive 20S proteasome and 20S immunoproteasome with novel N ‐terminally modified peptide aldehydes and their antitumor activity

2018 ◽  
Vol 111 (4) ◽  
Author(s):  
Marta Lubos ◽  
Dawid Dębowski ◽  
Ewelina Barcińska ◽  
Annika Meid ◽  
Iwona Inkielewicz‐Stepniak ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
20S Proteasome ◽  
Peptide Aldehydes

scholarly journals Synthesis and Evaluation of Macrocyclic Peptide Aldehydes as Potent and Selective Inhibitors of the 20S Proteasome

2016 ◽  
Vol 7 (3) ◽  
pp. 250-255 ◽  
Author(s):  
David L. Wilson ◽  
Isabel Meininger ◽  
Zack Strater ◽  
Stephanie Steiner ◽  
Frederick Tomlin ◽  
...  
Keyword(s):  
20S Proteasome ◽  
Selective Inhibitors ◽  
Peptide Aldehydes ◽  
Macrocyclic Peptide

scholarly journals Nostocyclopeptides as New Inhibitors of 20S Proteasome

Biomolecules ◽  
2021 ◽  
Vol 11 (10) ◽  
pp. 1483
Author(s):  
Anna Fidor ◽  
Katarzyna Cekała ◽  
Ewa Wieczerzak ◽  
Marta Cegłowska ◽  
Franciszek Kasprzykowski ◽  
...  
Keyword(s):  
Aldehyde Group ◽  
20S Proteasome ◽  
Nonribosomal Peptides ◽  
Inhibitory Effects ◽  
Linear Peptide ◽  
Cellular Processes ◽  
Peptide Aldehydes ◽  
Enzymatic Complex ◽  
Selective Activity

Nostocyclopeptides (Ncps) are a small class of bioactive nonribosomal peptides produced solely by cyanobacteria of the genus Nostoc. In the current work, six Ncps were isolated from Nostoc edaphicum strain CCNP1411. The bioactivity of these compounds was tested in vitro against 20S proteasome, a proteolytic complex that plays an important role in maintaining cellular proteostasis. Dysfunction of the complex leads to many pathological disorders. The assays indicated selective activity of specific Ncp variants. For two linear peptide aldehydes, Ncp-A2-L and Ncp-E2-L, the inhibitory effects on chymotrypsin-like activity were revealed, while the cyclic variant, Ncp-A2, inactivated the trypsin-like site of this enzymatic complex. The aldehyde group was confirmed to be an important element of the chymotrypsin-like activity inhibitors. The nostocyclopeptides, as novel inhibitors of 20S proteasome, increased the number of natural products that can be considered potential regulators of cellular processes.

scholarly journals Synthesis and SAR Study of Novel Peptide Aldehydes as Inhibitors of 20S Proteasome

Molecules ◽  
2011 ◽  
Vol 16 (9) ◽  
pp. 7551-7564 ◽  
Author(s):  
Yuheng Ma ◽  
Bo Xu ◽  
Yuan Fang ◽  
Zhenjun Yang ◽  
Jingrong Cui ◽  
...  
Keyword(s):  
20S Proteasome ◽  
Peptide Aldehydes ◽  
Sar Study

710: TNF-Related Apoptosis Inducing Ligand (TRAIL/APO-2L): A Novel Mechanism for BCG-Induced Antitumor Activity

2004 ◽  
Vol 171 (4S) ◽  
pp. 188-189
Author(s):  
Aaron T. Ludwig ◽  
Jill M. Moore ◽  
Yi Luo ◽  
Xiaohong Chen ◽  
Michael A. O’Donnell ◽  
...  
Keyword(s):  
Antitumor Activity

Antitumor activity of tricin, a flavone isolated from leaves of Casearia arborea (Salicaceae)

2017 ◽  
Author(s):  
P Sartorelli ◽  
A Santos ◽  
C Figueiredo ◽  
J Lago ◽  
M Soares
Keyword(s):  
Antitumor Activity

Adaptive NK cells with decreased antitumor activity are expanded in HBV-associated HCC

2018 ◽  
Vol 56 (01) ◽  
pp. E2-E89
Author(s):  
C Rennert ◽  
C Tauber ◽  
B Zecher ◽  
A Schuch ◽  
M Hofmann ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Nk Cells

Synthesis of Some New Tetracyclic Pyrimidine Derivatives Using Exocyclic α,β-Unsaturated Ketone and Evaluation of Their Antitumor Activities

2016 ◽  
Vol 12 (8) ◽  
pp. 311-317
Author(s):  
Kamelia El-Mahdy
Keyword(s):  
Antitumor Activity ◽  
Spectroscopic Data ◽  
Acid Hydrazide ◽  
Chloroacetic Acid ◽  
Equimolar Amount ◽  
Unsaturated Ketone ◽  
Cyanoacetic Acid ◽  
Antitumor Activities ◽  
Pyrimidine Derivatives ◽  
Cyanoacetic Acid Hydrazide

Thiazolopyrimidine 2 was obtained from the reaction of dihydropyrimidinone with chloroacetic acid and benzaldehyde. Thiazolopyrimidine 2 containing an α,β-unsaturated ketonic function [-CH=CH-CO-] has been used as a component of Michael addition with an equimolar amount of dinucleophiles to give a series of novel tetracyclic pyrimidine derivatives. Treatment of thiazolopyrimidine 2 with uracil, aminotriazole, cyanoacetic acid hydrazide, o-phenylenediamine or diaminopyridine afforded the corresponding pyridopyrimidine, triazolopyrimidine, pyrazolone, benzodiazepine and triazepine derivative, respectively. The detailed synthesis, spectroscopic data, and antitumor activity for synthesized compounds were reported.

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