Literature DB >> 27722650

Disrupting the PCSK9/LDLR protein-protein interaction by an imidazole-based minimalist peptidomimetic.

Mattia Stucchi1, Giovanni Grazioso2, Carmen Lammi2, Silvia Manara2, Chiara Zanoni2, Anna Arnoldi2, Giordano Lesma3, Alessandra Silvani3.   

Abstract

Herein we report on the multicomponent synthesis of a novel imidazole-based compound, able to act efficiently as a minimalist β-strand mimic. Biological evaluation proved its ability to impair the LDLR-PCSK9 protein-protein interaction, disclosing it as the first small molecule exerting a PCSK9-mediated hypocholesterolemic effect.

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Year:  2016        PMID： 27722650     DOI： 10.1039/c6ob01642a

Source DB:  PubMed          Journal:  Org Biomol Chem        ISSN： 1477-0520            Impact factor:   3.876


  8 in total

1.  Inhibition of PCSK9D374Y/LDLR Protein-Protein Interaction by Computationally Designed T9 Lupin Peptide.

Authors:  Carmen Lammi; Jacopo Sgrignani; Gabriella Roda; Anna Arnoldi; Giovanni Grazioso
Journal:  ACS Med Chem Lett       Date:  2018-12-03       Impact factor: 4.345

2.  Discovery of a cryptic peptide-binding site on PCSK9 and design of antagonists.

Authors:  Yingnan Zhang; Mark Ultsch; Nicholas J Skelton; Daniel J Burdick; Maureen H Beresini; Wei Li; Monica Kong-Beltran; Andrew Peterson; John Quinn; Cecilia Chiu; Yan Wu; Steven Shia; Paul Moran; Paola Di Lello; Charles Eigenbrot; Daniel Kirchhofer
Journal:  Nat Struct Mol Biol       Date:  2017-08-21       Impact factor: 15.369

3.  Structure-based drug design, synthesis and biological assays of P. falciparum Atg3-Atg8 protein-protein interaction inhibitors.

Authors:  Stefania Villa; Laura Legnani; Diego Colombo; Arianna Gelain; Carmen Lammi; Daniele Bongiorno; Denise P Ilboudo; Kellen E McGee; Jürgen Bosch; Giovanni Grazioso
Journal:  J Comput Aided Mol Des       Date:  2018-01-30       Impact factor: 3.686

4.  Small Molecule Inhibitors of the PCSK9·LDLR Interaction.

Authors:  Jaru Taechalertpaisarn; Bosheng Zhao; Xiaowen Liang; Kevin Burgess
Journal:  J Am Chem Soc       Date:  2018-02-26       Impact factor: 15.419

5.  Biological Characterization of Computationally Designed Analogs of peptide TVFTSWEEYLDWV (Pep2-8) with Increased PCSK9 Antagonistic Activity.

Authors:  Carmen Lammi; Jacopo Sgrignani; Anna Arnoldi; Giovanni Grazioso
Journal:  Sci Rep       Date:  2019-02-20       Impact factor: 4.379

6.  Discovery and SAR analysis of phenylbenzo[d][1,3]dioxole-based proprotein convertase subtilisin/kexin type 9 inhibitors.

Authors:  Fahui Li; Lihui Zhang; Jinhong Feng; Lei Zhang
Journal:  J Enzyme Inhib Med Chem       Date:  2022-12       Impact factor: 5.756

7.  Novel Target Study to Cure Cardiovascular Disease regarding Proprotein Converse Subtilisin/Kexin Type 9.

Authors:  Yingjing Zhao; Weihang Li; Weiye Li; Hong Tao; Yuting Li; Bo Wu; Xinhui Wang; Huasong Zhou; Bo Gao
Journal:  Biomed Res Int       Date:  2022-10-11       Impact factor: 3.246

Review 8.  Physiological and therapeutic regulation of PCSK9 activity in cardiovascular disease.

Authors:  Simon Glerup; Rainer Schulz; Ulrich Laufs; Klaus-Dieter Schlüter
Journal:  Basic Res Cardiol       Date:  2017-04-24       Impact factor: 17.165
  8 in total

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