| Full text | |
| Author(s): |
Scott, Fiona
[1]
;
Fala, Angela M.
[2, 3]
;
Pennicott, Lewis E.
[1]
;
Reuillon, Tristan D.
[1]
;
Massirer, Katlin B.
[2, 3]
;
Elkins, Jonathan M.
[4]
;
Ward, Simon E.
[1, 5]
Total Authors: 7
|
| Affiliation: | [1] Univ Sussex, Sussex Drug Discovery Ctr, Sussex House, Brighton BN1 9RH, E Sussex - England
[2] Univ Estadual Campinas, Dept Genet & Evolucao, Inst Biol, Struct Genom Consortium, BR-13083886 Campinas, SP - Brazil
[3] Univ Estadual Campinas, Ctr Quim Med CQMED, CBMEG, UNICAMP, BR-13083875 Campinas, SP - Brazil
[4] Univ Oxford, Nuffield Dept Med, Struct Genom Consortium, Oxford OX3 7DQ - England
[5] Cardiff Univ, Med Discovery Inst, Main Bldg, Pk Pl, Cardiff CF10 3AT - Wales
Total Affiliations: 5
|
| Document type: | Journal article |
| Source: | Bioorganic & Medicinal Chemistry Letters; v. 30, n. 8 APR 15 2020. |
| Web of Science Citations: | 0 |
| Abstract | |
Kinases are signalling proteins which have proven to be successful targets for the treatment of a variety of diseases, predominantly in cancers. However, only a small proportion of kinases ( < 20%) have been investigated for their therapeutic viability, likely due to the lack of available chemical tools across the kinome. In this work we describe initial efforts in the development of a selective chemical tool for protein kinase N2 (PKN2), a relatively unexplored kinase of interest in several types of cancer. The most successful compound, 5, has a measured IC50 of 0.064 mu M against PKN2, with ca. 17-fold selectivity over close homologue, PKN1. (AU) | |
| FAPESP's process: | 14/50897-0 - INCT 2014: Open-acess Medicinal Chemistry Centre (OpenMedChem) |
| Grantee: | Katlin Brauer Massirer |
| Support Opportunities: | Research Projects - Thematic Grants |
| FAPESP's process: | 13/50724-5 - Protein Kinase Chemical Biology Center: supporting drug development through open-access research |
| Grantee: | Paulo Arruda |
| Support Opportunities: | Research Grants - Research Partnership for Technological Innovation - PITE |