Richters, Andre, Basu, Debjit, Engel, Julian, Ercanoglu, Meryem S., Balke-Want, Hyatt, Tesch, Roberta, Thomas, Roman K. and Rauh, Daniel ORCID: 0000-0002-1970-7642 (2015). Identification and Further Development of Potent TBK1 Inhibitors. ACS Chem. Biol., 10 (1). S. 289 - 299. WASHINGTON: AMER CHEMICAL SOC. ISSN 1554-8937

Full text not available from this repository.

Abstract

The cytosolic Ser/Thr kinase TBK1 was discovered to be an essential element in the mediation of signals that lead to tumor migration and progression. These findings meet the need for the identification of novel tool compounds and potential therapeutics to gain deeper insights into TBK1 related signaling and its relevance in tumor progression. Herein, we undertake the activity-based screening for unique inhibitors of TBK1 and their subsequent optimization. Initial screening approaches identified a selection of TBK1 inhibitors that were optimized using methods of medicinal chemistry. Variations of the structural characteristics of a representative 2,4,6-substituted pyrimidine scaffold resulted in improved potency. Prospective use as tool compounds or basic contributions to drug design approaches are anticipated for our improved small molecules.

Item Type: Journal Article
Creators:
CreatorsEmailORCIDORCID Put Code
Richters, AndreUNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Basu, DebjitUNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Engel, JulianUNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Ercanoglu, Meryem S.UNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Balke-Want, HyattUNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Tesch, RobertaUNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Thomas, Roman K.UNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Rauh, DanielUNSPECIFIEDorcid.org/0000-0002-1970-7642UNSPECIFIED
URN: urn:nbn:de:hbz:38-417529
DOI: 10.1021/cb500908d
Journal or Publication Title: ACS Chem. Biol.
Volume: 10
Number: 1
Page Range: S. 289 - 299
Date: 2015
Publisher: AMER CHEMICAL SOC
Place of Publication: WASHINGTON
ISSN: 1554-8937
Language: English
Faculty: Unspecified
Divisions: Unspecified
Subjects: no entry
Uncontrolled Keywords:
KeywordsLanguage
BINDING KINASE 1; TBK1/IKK-EPSILON KINASES; NONCANONICAL IKKS; BREAST-CANCER; LUNG-CANCER; KAPPA-B; ACTIVATION; SELECTIVITY; DISCOVERY; EPSILONMultiple languages
Biochemistry & Molecular BiologyMultiple languages
URI: http://kups.ub.uni-koeln.de/id/eprint/41752

Downloads

Downloads per month over past year

Altmetric

Export

Actions (login required)

View Item View Item