Search Results - "Treiber, Daniel K."
-
1
Comprehensive analysis of kinase inhibitor selectivity
Published in Nature biotechnology (01-11-2011)“…Davis et al . extend their previous efforts to use inhibitor-kinase interactions to understand kinase inhibitor selectivity by profiling the binding of 72…”
Get full text
Journal Article -
2
Progress towards a public chemogenomic set for protein kinases and a call for contributions
Published in PloS one (02-08-2017)“…Protein kinases are highly tractable targets for drug discovery. However, the biological function and therapeutic potential of the majority of the 500+ human…”
Get full text
Journal Article -
3
Dual kinase-bromodomain inhibitors for rationally designed polypharmacology
Published in Nature chemical biology (01-04-2014)“…Kinases are a widely targeted enzyme class in cancer chemotherapy. Several clinically used kinase inhibitors also inhibit bromodomains, epigenetic ‘readers’ of…”
Get full text
Journal Article -
4
A quantitative analysis of kinase inhibitor selectivity
Published in Nature biotechnology (01-01-2008)“…Kinase inhibitors are a new class of therapeutics with a propensity to inhibit multiple targets 1 , 2 . The biological consequences of multi-kinase activity…”
Get full text
Journal Article -
5
Utilizing comprehensive and mini-kinome panels to optimize the selectivity of quinoline inhibitors for cyclin G associated kinase (GAK)
Published in Bioorganic & medicinal chemistry letters (15-07-2019)“…[Display omitted] We demonstrate an innovative approach for optimization of kinase inhibitor potency and selectivity utilising kinase mini-panels and…”
Get full text
Journal Article -
6
Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit
Published in Journal of medicinal chemistry (26-05-2016)“…The acetyl post-translational modification of chromatin at selected histone lysine residues is interpreted by an acetyl-lysine specific interaction with…”
Get full text
Journal Article -
7
Inhibition of Drug-Resistant Mutants of ABL, KIT, and EGF Receptor Kinases
Published in Proceedings of the National Academy of Sciences - PNAS (02-08-2005)“…To realize the full potential of targeted protein kinase inhibitors for the treatment of cancer, it is important to address the emergence of drug resistance in…”
Get full text
Journal Article -
8
Kinetic Intermediates Trapped by Native Interactions in RNA Folding
Published in Science (American Association for the Advancement of Science) (20-03-1998)“…In the magnesium ion-dependent folding of the Tetrahymena ribozyme, a kinetic intermediate accumulates in which the P4-P6 domain is formed, but the P3-P7…”
Get full text
Journal Article -
9
Ins and Outs of Kinase DFG Motifs
Published in Chemistry & biology (20-06-2013)“…In this issue of Chemistry & Biology, Hari and colleagues show that two positions in kinase active sites, including the well-known “gatekeeper” residue,…”
Get full text
Journal Article -
10
Donated chemical probes for open science
Published in eLife (20-04-2018)“…Potent, selective and broadly characterized small molecule modulators of protein function (chemical probes) are powerful research reagents. The pharmaceutical…”
Get full text
Journal Article -
11
An Optimal Mg2+ Concentration for Kinetic Folding of the Tetrahymena Ribozyme
Published in Proceedings of the National Academy of Sciences - PNAS (26-10-1999)“…Divalent metal ions, such as Mg2+, are generally required for tertiary structure formation in RNA. Although the role of Mg2+ binding in RNA-folding equilibria…”
Get full text
Journal Article -
12
A small molecule-kinase interaction map for clinical kinase inhibitors
Published in Nature biotechnology (01-03-2005)“…Kinase inhibitors show great promise as a new class of therapeutics. Here we describe an efficient way to determine kinase inhibitor specificity by measuring…”
Get full text
Journal Article -
13
Structure of the kinase domain of an imatinib-resistant abl mutant in complex with the aurora kinase inhibitor VX-680
Published in Cancer research (Chicago, Ill.) (15-01-2006)“…We present a high-resolution (2.0 A) crystal structure of the catalytic domain of a mutant form of the Abl tyrosine kinase (H396P; Abl-1a numbering) that is…”
Get full text
Journal Article -
14
Beyond kinetic traps in RNA folding
Published in Current Opinion in Structural Biology (01-06-2001)“…Large RNAs often have rugged folding energy landscapes that result in severe misfolding and slow folding kinetics. Several interdependent parameters that…”
Get full text
Book Review Journal Article -
15
Exposing the kinetic traps in RNA folding
Published in Current opinion in structural biology (01-06-1999)“…Large ribozymes fold on a ‘glacials timescale compared to the folding of their protein counterparts. The sluggish folding exhibited by large RNAs results from…”
Get full text
Journal Article -
16
Activation State-Dependent Binding of Small Molecule Kinase Inhibitors: Structural Insights from Biochemistry
Published in Chemistry & biology (24-11-2010)“…Interactions between kinases and small molecule inhibitors can be activation state dependent. A detailed understanding of inhibitor binding therefore requires…”
Get full text
Journal Article -
17
Novel series of pyrrolotriazine analogs as highly potent pan-Aurora kinase inhibitors
Published in Bioorganic & medicinal chemistry letters (15-09-2011)“…The synthesis and SAR for a novel series of pyrrolotriazines as pan-Aurora kinase inhibitors are described. The synthesis and SAR for a novel series of…”
Get full text
Journal Article -
18
Discovery of Highly Potent and Selective Pan-Aurora Kinase Inhibitors with Enhanced in Vivo Antitumor Therapeutic Index
Published in Journal of medicinal chemistry (12-04-2012)“…Serine/threonine protein kinases Aurora A, B, and C play essential roles in cell mitosis and cytokinesis. Currently a number of Aurora kinase inhibitors with…”
Get full text
Journal Article -
19
Arylcarboxyamino-substituted diaryl ureas as potent and selective FLT3 inhibitors
Published in Bioorganic & medicinal chemistry letters (01-09-2009)“…A series of diaryl ureas with an amide substitution at the 4-position was prepared and found to be potent and selective FLT3 inhibitors with good oral…”
Get full text
Journal Article -
20
Discovery of AC710, a Globally Selective Inhibitor of Platelet-Derived Growth Factor Receptor-Family Kinases
Published in ACS medicinal chemistry letters (13-12-2012)“…A series of potent, selective platelet-derived growth factor receptor-family kinase inhibitors was optimized starting from a globally selective lead molecule 4…”
Get full text
Journal Article