Literature DB >> 19007200

Dihydrofuro[3,4-c]pyridinones as inhibitors of the cytolytic effects of the pore-forming glycoprotein perforin.

Gersande Lena1, Joseph A Trapani, Vivien R Sutton, Annette Ciccone, Kylie A Browne, Mark J Smyth, William A Denny, Julie A Spicer.   

Abstract

Dihydrofuro[3,4-c]pyridinones are the first class of small molecules reported to inhibit the cytolytic effects of the lymphocyte toxin perforin. A lead structure was identified from a high throughput screen, and a series of analogues were designed and prepared to explore structure-activity relationships around the core bicyclic thioxofuropyridinone and pendant furan ring. This resulted in the identification of a submicromolar inhibitor of the perforin-induced lysis of Jurkat T-lymphoma cells.

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Year:  2008        PMID： 19007200     DOI： 10.1021/jm801063n

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  8 in total

1.  The preclinical pharmacokinetic disposition of a series of perforin-inhibitors as potential immunosuppressive agents.

Authors:  M R Bull; J A Spicer; K M Huttunen; W A Denny; A Ciccone; K A Browne; J A Trapani; N A Helsby
Journal:  Eur J Drug Metab Pharmacokinet       Date:  2014-08-26       Impact factor: 2.441

2.  Preclinical Activity and Pharmacokinetic/Pharmacodynamic Relationship for a Series of Novel Benzenesulfonamide Perforin Inhibitors.

Authors:  Kate H Gartlan; Jagdish K Jaiswal; Matthew R Bull; Hedieh Akhlaghi; Vivien R Sutton; Kylie A Alexander; Karshing Chang; Geoffrey R Hill; Christian K Miller; Patrick D O'Connor; Jiney Jose; Joseph A Trapani; Susan A Charman; Julie A Spicer; Stephen M F Jamieson
Journal:  ACS Pharmacol Transl Sci       Date:  2022-05-31

3.  Substituted arylsulphonamides as inhibitors of perforin-mediated lysis.

Authors:  Julie A Spicer; Christian K Miller; Patrick D O'Connor; Jiney Jose; Kristiina M Huttunen; Jagdish K Jaiswal; William A Denny; Hedieh Akhlaghi; Kylie A Browne; Joseph A Trapani
Journal:  Eur J Med Chem       Date:  2017-05-26       Impact factor: 6.514

4.  Synthesis and anti-influenza virus activity of 4-oxo- or thioxo-4,5-dihydrofuro[3,4-c]pyridin-3(1H)-ones.

Authors:  Ye Jin Jang; Raghavendra Achary; Hye Won Lee; Hyo Jin Lee; Chong-Kyo Lee; Soo Bong Han; Young-Sik Jung; Nam Sook Kang; Pilho Kim; Meehyein Kim
Journal:  Antiviral Res       Date:  2014-04-30       Impact factor: 5.970

5.  Inefficient boosting of antitumor CD8(+) T cells by dendritic-cell vaccines is rescued by restricting T-cell cytotoxic functions.

Authors:  Joel Zhi-Iong Ma; Jianping Yang; Jim S Qin; Antonia Richter; Rachel Perret; Wafik S El-Deiry; Niklas Finnberg; Franca Ronchese
Journal:  Oncoimmunology       Date:  2012-12-01       Impact factor: 8.110

6.  Exploration of a series of 5-arylidene-2-thioxoimidazolidin-4-ones as inhibitors of the cytolytic protein perforin.

Authors:  Julie A Spicer; Gersande Lena; Dani M Lyons; Kristiina M Huttunen; Christian K Miller; Patrick D O'Connor; Matthew Bull; Nuala Helsby; Stephen M F Jamieson; William A Denny; Annette Ciccone; Kylie A Browne; Jamie A Lopez; Jesse Rudd-Schmidt; Ilia Voskoboinik; Joseph A Trapani
Journal:  J Med Chem       Date:  2013-11-19       Impact factor: 7.446

Review 7.  Inhibition of Pore-Forming Proteins.

Authors:  Neža Omersa; Marjetka Podobnik; Gregor Anderluh
Journal:  Toxins (Basel)       Date:  2019-09-19       Impact factor: 4.546

8.  Plasmodium Perforin-Like Protein Pores on the Host Cell Membrane Contribute in Its Multistage Growth and Erythrocyte Senescence.

Authors:  Swati Garg; Abhishek Shivappagowdar; Rahul S Hada; Rajagopal Ayana; Chandramohan Bathula; Subhabrata Sen; Inderjeet Kalia; Soumya Pati; Agam P Singh; Shailja Singh
Journal:  Front Cell Infect Microbiol       Date:  2020-03-24       Impact factor: 5.293
  8 in total

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