Literature DB >> 16597152

Identification of a potent botulinum neurotoxin a protease inhibitor using in situ lead identification chemistry.

Grant E Boldt1, Jack P Kennedy, Kim D Janda.   

Abstract

[reaction: see text] Botulinum neurotoxins (BoNTs), etiological agents of the deadly food poisoning disease botulism, are the most toxic proteins currently known. By using in situ lead identification chemistry, we have uncovered the first class of inhibitors that displays nanomolar potency. From a 15 microM lead compound, structure-activity relationship studies were performed granting the most potent BoNT/A inhibitor reported to date that displays an inhibition constant of 300 nM.

Entities:  

Mesh：

Substances：

Year:  2006        PMID： 16597152      PMCID： PMC2733786          DOI： 10.1021/ol0603211

Source DB:  PubMed          Journal:  Org Lett        ISSN： 1523-7052            Impact factor:   6.005


  13 in total

1.  Intimate details of the most poisonous poison.

Authors:  B R Singh
Journal:  Nat Struct Biol       Date:  2000-08

2.  Genetic and immunological comparison of anti-botulinum type A antibodies from immune and non-immune human phage libraries.

Authors:  Peter Amersdorfer; Cindy Wong; Theresa Smith; Steven Chen; Sharad Deshpande; Robert Sheridan; James D Marks
Journal:  Vaccine       Date:  2002-02-22       Impact factor: 3.641

3.  Novel small molecule inhibitors of botulinum neurotoxin A metalloprotease activity.

Authors:  James C Burnett; James J Schmidt; Robert G Stafford; Rekha G Panchal; Tam L Nguyen; Ann R Hermone; Jonathan L Vennerstrom; Connor F McGrath; Douglas J Lane; Edward A Sausville; Daniel W Zaharevitz; Rick Gussio; Sina Bavari
Journal:  Biochem Biophys Res Commun       Date:  2003-10-10       Impact factor: 3.575

Review 4.  Identification of the major steps in botulinum toxin action.

Authors:  Lance L Simpson
Journal:  Annu Rev Pharmacol Toxicol       Date:  2004       Impact factor: 13.820

5.  Serotype-selective, small-molecule inhibitors of the zinc endopeptidase of botulinum neurotoxin serotype A.

Authors:  Jewn Giew Park; Peter C Sill; Edward F Makiyi; Alfonso T Garcia-Sosa; Charles B Millard; James J Schmidt; Yuan-Ping Pang
Journal:  Bioorg Med Chem       Date:  2005-10-03       Impact factor: 3.641

6.  Improved solution- and solid-phase preparation of hydroxamic acids from esters.

Authors:  Chih Y Ho; Eric Strobel; Janet Ralbovsky; Robert A Galemmo
Journal:  J Org Chem       Date:  2005-06-10       Impact factor: 4.354

7.  Crystal structure of botulinum neurotoxin type A and implications for toxicity.

Authors:  D B Lacy; W Tepp; A C Cohen; B R DasGupta; R C Stevens
Journal:  Nat Struct Biol       Date:  1998-10

Review 8.  Botulinum toxin as a biological weapon: medical and public health management.

Authors:  S S Arnon; R Schechter; T V Inglesby; D A Henderson; J G Bartlett; M S Ascher; E Eitzen; A D Fine; J Hauer; M Layton; S Lillibridge; M T Osterholm; T O'Toole; G Parker; T M Perl; P K Russell; D L Swerdlow; K Tonat
Journal:  JAMA       Date:  2001-02-28       Impact factor: 56.272

9.  Synthesis, characterization and development of a high-throughput methodology for the discovery of botulinum neurotoxin a inhibitors.

Authors:  Grant E Boldt; Jack P Kennedy; Mark S Hixon; Laura A McAllister; Joseph T Barbieri; Saul Tzipori; Kim D Janda
Journal:  J Comb Chem       Date:  2006 Jul-Aug

10.  Solid-phase synthesis of di- and tripeptidic hydroxamic acids as inhibitors of procollagen C-proteinase.

Authors:  S M Dankwardt; R J Billedeau; L K Lawley; S C Abbot; R L Martin; C S Chan; H E Van Wart; K A Walker
Journal:  Bioorg Med Chem Lett       Date:  2000-11-20       Impact factor: 2.823
View more
  52 in total

1.  Synthesis and evaluation of library of betulin derivatives against the botulinum neurotoxin A protease.

Authors:  Peter Šilhár; Sami Alakurtti; Kateřina Čapková; Feng Xiaochuan; Charles B Shoemaker; Jari Yli-Kauhaluoma; Kim D Janda
Journal:  Bioorg Med Chem Lett       Date:  2011-03-04       Impact factor: 2.823

2.  An in vitro and in vivo disconnect uncovered through high-throughput identification of botulinum neurotoxin A antagonists.

Authors:  Lisa M Eubanks; Mark S Hixon; Wei Jin; Sukwon Hong; Colin M Clancy; William H Tepp; Michael R Baldwin; Carl J Malizio; Michael C Goodnough; Joseph T Barbieri; Eric A Johnson; Dale L Boger; Tobin J Dickerson; Kim D Janda
Journal:  Proc Natl Acad Sci U S A       Date:  2007-02-09       Impact factor: 11.205

3.  Targeting botulinum A cellular toxicity: a prodrug approach.

Authors:  Peter Silhár; Lisa M Eubanks; Hajime Seki; Sabine Pellett; Sacha Javor; William H Tepp; Eric A Johnson; Kim D Janda
Journal:  J Med Chem       Date:  2013-10-15       Impact factor: 7.446

4.  Covalent Modifiers of Botulinum Neurotoxin Counteract Toxin Persistence.

Authors:  Megan Garland; Brett M Babin; Shin-Ichiro Miyashita; Sebastian Loscher; Yi Shen; Min Dong; Matthew Bogyo
Journal:  ACS Chem Biol       Date:  2019-01-08       Impact factor: 5.100

5.  Metal Ions Effectively Ablate the Action of Botulinum Neurotoxin A.

Authors:  Paul T Bremer; Sabine Pellett; James P Carolan; William H Tepp; Lisa M Eubanks; Karen N Allen; Eric A Johnson; Kim D Janda
Journal:  J Am Chem Soc       Date:  2017-05-19       Impact factor: 15.419

Review 6.  Targeting Metalloenzymes for Therapeutic Intervention.

Authors:  Allie Y Chen; Rebecca N Adamek; Benjamin L Dick; Cy V Credille; Christine N Morrison; Seth M Cohen
Journal:  Chem Rev       Date:  2018-09-07       Impact factor: 60.622

7.  Identification of 3-hydroxy-1,2-dimethylpyridine-4(1H)-thione as a metal-binding motif for the inhibition of botulinum neurotoxin A.

Authors:  Lucy Lin; Lewis D Turner; Peter Šilhár; Sabine Pellett; Eric A Johnson; Kim D Janda
Journal:  RSC Med Chem       Date:  2020-11-12

8.  Newly Designed Quinolinol Inhibitors Mitigate the Effects of Botulinum Neurotoxin A in Enzymatic, Cell-Based, and ex Vivo Assays.

Authors:  Paul T Bremer; Michael Adler; Cecilia H Phung; Ajay K Singh; Kim D Janda
Journal:  J Med Chem       Date:  2017-01-03       Impact factor: 7.446

9.  Synthesis and structure-activity relationships of second-generation hydroxamate botulinum neurotoxin A protease inhibitors.

Authors:  Katerina Capková; Yoshiyuki Yoneda; Tobin J Dickerson; Kim D Janda
Journal:  Bioorg Med Chem Lett       Date:  2007-10-09       Impact factor: 2.823

10.  Potent new small-molecule inhibitor of botulinum neurotoxin serotype A endopeptidase developed by synthesis-based computer-aided molecular design.

Authors:  Yuan-Ping Pang; Anuradha Vummenthala; Rajesh K Mishra; Jewn Giew Park; Shaohua Wang; Jon Davis; Charles B Millard; James J Schmidt
Journal:  PLoS One       Date:  2009-11-10       Impact factor: 3.240
View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.