Literature DB >> 36105330

mRNA Display Reaches for the Clinic with New PCSK9 Inhibitor.

Sabrina E Iskandar1, Albert A Bowers1,2,3.   

Abstract

Merck & Co. recently reported one of the first mRNA display-derived clinical candidates in a bioavailable inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9). Herein, we discuss the chemical and pharmacological challenges surmounted in bringing this compound to trials and the current outlook for mRNA display-based therapeutic development.
© 2022 American Chemical Society.

Entities:  

Year:  2022        PMID： 36105330      PMCID： PMC9465826          DOI： 10.1021/acsmedchemlett.2c00319

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.632


  28 in total

1.  Series of Novel and Highly Potent Cyclic Peptide PCSK9 Inhibitors Derived from an mRNA Display Screen and Optimized via Structure-Based Design.

Authors:  Candice Alleyne; Rupesh P Amin; Bhavana Bhatt; Elisabetta Bianchi; J Craig Blain; Nicolas Boyer; Danila Branca; Mark W Embrey; Sookhee N Ha; Kelli Jette; Douglas G Johns; Angela D Kerekes; Kenneth A Koeplinger; Derek LaPlaca; Nianyu Li; Beth Murphy; Peter Orth; Alonso Ricardo; Scott Salowe; Kathleen Seyb; Aurash Shahripour; Joseph R Stringer; Yili Sun; Rodger Tracy; Chengwei Wu; Yusheng Xiong; Hyewon Youm; Hratch J Zokian; Thomas J Tucker
Journal:  J Med Chem       Date:  2020-11-10       Impact factor: 7.446

Review 2.  Small molecules as inhibitors of PCSK9: Current status and future challenges.

Authors:  Shengtao Xu; Shanshan Luo; Zheying Zhu; Jinyi Xu
Journal:  Eur J Med Chem       Date:  2018-11-11       Impact factor: 6.514

3.  Evolocumab and Clinical Outcomes in Patients with Cardiovascular Disease.

Authors:  Marc S Sabatine; Robert P Giugliano; Anthony C Keech; Narimon Honarpour; Stephen D Wiviott; Sabina A Murphy; Julia F Kuder; Huei Wang; Thomas Liu; Scott M Wasserman; Peter S Sever; Terje R Pedersen
Journal:  N Engl J Med       Date:  2017-03-17       Impact factor: 91.245

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.  Phage-encoded combinatorial chemical libraries based on bicyclic peptides.

Authors:  Christian Heinis; Trevor Rutherford; Stephan Freund; Greg Winter
Journal:  Nat Chem Biol       Date:  2009-07       Impact factor: 15.040

6.  In vitro selection of highly modified cyclic peptides that act as tight binding inhibitors.

Authors:  Yollete V Guillen Schlippe; Matthew C T Hartman; Kristopher Josephson; Jack W Szostak
Journal:  J Am Chem Soc       Date:  2012-03-29       Impact factor: 15.419

7.  Expanding the Chemical Diversity of Genetically Encoded Libraries.

Authors:  Sabrina E Iskandar; Victoria A Haberman; Albert A Bowers
Journal:  ACS Comb Sci       Date:  2020-11-09       Impact factor: 3.903

Review 8.  PCSK9 and LDLR degradation: regulatory mechanisms in circulation and in cells.

Authors:  Thomas A Lagace
Journal:  Curr Opin Lipidol       Date:  2014-10       Impact factor: 4.776

9.  Identification of a mast-cell-specific receptor crucial for pseudo-allergic drug reactions.

Authors:  Benjamin D McNeil; Priyanka Pundir; Sonya Meeker; Liang Han; Bradley J Undem; Marianna Kulka; Xinzhong Dong
Journal:  Nature       Date:  2014-12-17       Impact factor: 49.962

10.  Macrocycle peptides delineate locked-open inhibition mechanism for microorganism phosphoglycerate mutases.

Authors:  Hao Yu; Patricia Dranchak; Zhiru Li; Ryan MacArthur; Matthew S Munson; Nurjahan Mehzabeen; Nathan J Baird; Kevin P Battalie; David Ross; Scott Lovell; Clotilde K S Carlow; Hiroaki Suga; James Inglese
Journal:  Nat Commun       Date:  2017-04-03       Impact factor: 14.919
View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.