Literature DB >> 25129616

Substrate derived peptidic α-ketoamides as inhibitors of the malarial protease PfSUB1.

Samir S Kher1, Maria Penzo2, Simone Fulle3, Paul W Finn3, Michael J Blackman2, Aigars Jirgensons1.   

Abstract

Peptidic α-ketoamides have been developed as inhibitors of the malarial protease PfSUB1. The design of inhibitors was based on the best known endogenous PfSUB1 substrate sequence, leading to compounds with low micromolar to submicromolar inhibitory activity. SAR studies were performed indicating the requirement of an aspartate mimicking the P1' substituent and optimal P1-P4 length of the non-prime part. The importance of each of the P1-P4 amino acid side chains was investigated, revealing crucial interactions and size limitations.
Copyright © 2014 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Malaria; Peptides; PfSUB1; Serine protease; α-Ketoamide

Mesh：

Substances：

Year:  2014        PMID： 25129616     DOI： 10.1016/j.bmcl.2014.07.086

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


  6 in total

1.  Peptidic boronic acids are potent cell-permeable inhibitors of the malaria parasite egress serine protease SUB1.

Authors:  Elina Lidumniece; Chrislaine Withers-Martinez; Fiona Hackett; Christine R Collins; Abigail J Perrin; Konstantinos Koussis; Claudine Bisson; Michael J Blackman; Aigars Jirgensons
Journal:  Proc Natl Acad Sci U S A       Date:  2021-05-18       Impact factor: 12.779

2.  Solution-phase automated synthesis of an α-amino aldehyde as a versatile intermediate.

Authors:  Hisashi Masui; Sae Yosugi; Shinichiro Fuse; Takashi Takahashi
Journal:  Beilstein J Org Chem       Date:  2017-01-17       Impact factor: 2.883

3.  The Plasmodium berghei serine protease PbSUB1 plays an important role in male gamete egress.

Authors:  Tomasino Pace; Felicia Grasso; Grazia Camarda; Catherine Suarez; Michael J Blackman; Marta Ponzi; Anna Olivieri
Journal:  Cell Microbiol       Date:  2019-04-29       Impact factor: 3.715

Review 4.  Merging the Versatile Functionalities of Boronic Acid with Peptides.

Authors:  Yahong Tan; Junjie Wu; Lulu Song; Mengmeng Zhang; Christopher John Hipolito; Changsheng Wu; Siyuan Wang; Youming Zhang; Yizhen Yin
Journal:  Int J Mol Sci       Date:  2021-11-30       Impact factor: 5.923

5.  Autocatalytic activation of a malarial egress protease is druggable and requires a protein cofactor.

Authors:  Michele S Y Tan; Konstantinos Koussis; Chrislaine Withers-Martinez; Steven A Howell; James A Thomas; Fiona Hackett; Ellen Knuepfer; Min Shen; Matthew D Hall; Ambrosius P Snijders; Michael J Blackman
Journal:  EMBO J       Date:  2021-05-01       Impact factor: 14.012

6.  In silico study of subtilisin-like protease 1 (SUB1) from different Plasmodium species in complex with peptidyl-difluorostatones and characterization of potent pan-SUB1 inhibitors.

Authors:  Simone Brogi; Simone Giovani; Margherita Brindisi; Sandra Gemma; Ettore Novellino; Giuseppe Campiani; Michael J Blackman; Stefania Butini
Journal:  J Mol Graph Model       Date:  2016-01-19       Impact factor: 2.518
  6 in total

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