scholarly journals Jakinibs: a new class of kinase inhibitors in cancer and autoimmune disease

2012 ◽  
Vol 12 (4) ◽  
pp. 464-470 ◽  
Author(s):  
Apostolos Kontzias ◽  
Alexander Kotlyar ◽  
Arian Laurence ◽  
Paul Changelian ◽  
John J O'Shea
Keyword(s):  
Autoimmune Disease ◽  
Kinase Inhibitors ◽  
New Class

ChemInform Abstract: Entry into a New Class of Protein Kinase Inhibitors by Pseudo Ring Design.

ChemInform ◽  
2008 ◽  
Vol 39 (27) ◽  
Author(s):  
Pascal Furet ◽  
Giorgio Caravatti ◽  
Vito Guagnano ◽  
Marc Lang ◽  
Thomas Meyer ◽  
...  
Keyword(s):  
Protein Kinase ◽  
Kinase Inhibitors ◽  
Protein Kinase Inhibitors ◽  
New Class

Tyrosine kinase inhibitors: New class of antimalarials on the horizon?

2015 ◽  
Vol 55 (2) ◽  
pp. 119-126 ◽  
Author(s):  
Vrushali Pathak ◽  
Roshan Colah ◽  
Kanjaksha Ghosh
Keyword(s):  
Tyrosine Kinase ◽  
Tyrosine Kinase Inhibitors ◽  
Kinase Inhibitors ◽  
New Class

ChemInform Abstract: Synthesis and Initial SAR Studies of 3,6-Disubstituted Pyrazolo[1,5-a]pyrimidines: A New Class of KDR Kinase Inhibitors.

ChemInform ◽  
2010 ◽  
Vol 33 (51) ◽  
pp. no-no
Author(s):  
Mark E. Fraley ◽  
et al. et al.
Keyword(s):  
Kinase Inhibitors ◽  
New Class ◽  
Sar Studies

Discovery of heterocyclic ureas as a new class of raf kinase inhibitors: identification of a second generation lead by a combinatorial chemistry approach

2001 ◽  
Vol 11 (20) ◽  
pp. 2775-2778 ◽  
Author(s):  
Roger A Smith ◽  
James Barbosa ◽  
Cheri L Blum ◽  
Mark A Bobko ◽  
Yolanda V Caringal ◽  
...  
Keyword(s):  
Combinatorial Chemistry ◽  
Second Generation ◽  
Kinase Inhibitors ◽  
Raf Kinase ◽  
New Class

scholarly journals Kinase inhibitors as an approach to autoimmune disease treatment

2013 ◽  
Vol 142 (2) ◽  
pp. 63-67
Author(s):  
Masamichi Inami
Keyword(s):  
Autoimmune Disease ◽  
Kinase Inhibitors ◽  
Disease Treatment

New class of kinase inhibitors poised to join the anticancer arsenal

2012 ◽  
Vol 11 (11) ◽  
pp. 819-820 ◽  
Author(s):  
Alisa Opar
Keyword(s):  
Kinase Inhibitors ◽  
New Class

Meriolins, a New Class of Cell Death–Inducing Kinase Inhibitors with Enhanced Selectivity for Cyclin-Dependent Kinases

2007 ◽  
Vol 67 (17) ◽  
pp. 8325-8334 ◽  
Author(s):  
Karima Bettayeb ◽  
Oscar M. Tirado ◽  
Séverine Marionneau-Lambot ◽  
Yoan Ferandin ◽  
Olivier Lozach ◽  
...  
Keyword(s):  
Cell Death ◽  
Kinase Inhibitors ◽  
Cyclin Dependent Kinases ◽  
New Class ◽  
Enhanced Selectivity

scholarly journals Antineoplastic kinase inhibitors: A new class of potent anti-amoebic compounds

2021 ◽  
Vol 15 (2) ◽  
pp. e0008425
Author(s):  
Conall Sauvey ◽  
Gretchen Ehrenkaufer ◽  
Da Shi ◽  
Anjan Debnath ◽  
Ruben Abagyan
Keyword(s):  
Kinase Inhibitors ◽  
Model Organism ◽  
Protozoan Parasite ◽  
Drug Candidates ◽  
New Class ◽  
Alternative Approach ◽  
The 1960S ◽  
Approved Drugs ◽  
Micromolar Range

Entamoeba histolytica is a protozoan parasite which infects approximately 50 million people worldwide, resulting in an estimated 70,000 deaths every year. Since the 1960s E. histolytica infection has been successfully treated with metronidazole. However, drawbacks to metronidazole therapy exist, including adverse effects, a long treatment course, and the need for an additional drug to prevent cyst-mediated transmission. E. histolytica possesses a kinome with approximately 300–400 members, some of which have been previously studied as potential targets for the development of amoebicidal drug candidates. However, while these efforts have uncovered novel potent inhibitors of E. histolytica kinases, none have resulted in approved drugs. In this study we took the alternative approach of testing a set of twelve previously FDA-approved antineoplastic kinase inhibitors against E. histolytica trophozoites in vitro. This resulted in the identification of dasatinib, bosutinib, and ibrutinib as amoebicidal agents at low-micromolar concentrations. Next, we utilized a recently developed computational tool to identify twelve additional drugs with human protein target profiles similar to the three initial hits. Testing of these additional twelve drugs led to the identification of ponatinib, neratinib, and olmutinib were identified as highly potent, with EC50 values in the sub-micromolar range. All of these six drugs were found to kill E. histolytica trophozoites as rapidly as metronidazole. Furthermore, ibrutinib was found to kill the transmissible cyst stage of the model organism E. invadens. Ibrutinib thus possesses both amoebicidal and cysticidal properties, in contrast to all drugs used in the current therapeutic strategy. These findings together reveal antineoplastic kinase inhibitors as a highly promising class of potent drugs against this widespread and devastating disease.

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