FDA-approved small-molecule kinase inhibitors

P Wu, TE Nielsen, MH Clausen - Trends in pharmacological sciences, 2015 - cell.com
Kinases have emerged as one of the most intensively pursued targets in current
pharmacological research, especially for cancer, due to their critical roles in cellular …

Target identification and mechanism of action in chemical biology and drug discovery

M Schenone, V Dančík, BK Wagner… - Nature chemical …, 2013 - nature.com
Target-identification and mechanism-of-action studies have important roles in small-
molecule probe and drug discovery. Biological and technological advances have resulted in …

Rational discovery of molecular glue degraders via scalable chemical profiling

C Mayor-Ruiz, S Bauer, M Brand, Z Kozicka… - Nature chemical …, 2020 - nature.com
Targeted protein degradation is a new therapeutic modality based on drugs that destabilize
proteins by inducing their proximity to E3 ubiquitin ligases. Of particular interest are …

Tracking cancer drugs in living cells by thermal profiling of the proteome

MM Savitski, FBM Reinhard, H Franken, T Werner… - Science, 2014 - science.org
INTRODUCTION Understanding drug mechanism poses the daunting challenge of
determining the affinity of the drug for all potential targets. Drug target engagement can be …

DeepIDC: a prediction framework of injectable drug combination based on heterogeneous information and deep learning

Y Yang, D Gao, X Xie, J Qin, J Li, H Lin, D Yan… - Clinical …, 2022 - Springer
Abstract Background and Objective In clinical practice, injectable drug combination (IDC)
usually provides good therapeutic effects for patients. Numerous clinical studies have …

Dual targeting of p53 and c-MYC selectively eliminates leukaemic stem cells

SA Abraham, LEM Hopcroft, E Carrick, ME Drotar… - Nature, 2016 - nature.com
Chronic myeloid leukaemia (CML) arises after transformation of a haemopoietic stem cell
(HSC) by the protein-tyrosine kinase BCR–ABL. Direct inhibition of BCR–ABL kinase has …

Natural course and biology of CML

B Chereda, JV Melo - Annals of hematology, 2015 - Springer
Chronic myeloid leukaemia (CML) is a myeloproliferative disorder arising in the
haemopoietic stem cell (HSC) compartment. This disease is characterised by a reciprocal t …

[HTML][HTML] Modelling of compound combination effects and applications to efficacy and toxicity: state-of-the-art, challenges and perspectives

KC Bulusu, R Guha, DJ Mason, RPI Lewis… - Drug discovery today, 2016 - Elsevier
Highlights•Review of the state-of-the-art in the field of compound combination modelling.•
Significance of quality control of large-scale combination screening data.•Strategies for …

Large-scale exploration and analysis of drug combinations

P Li, C Huang, Y Fu, J Wang, Z Wu, J Ru… - …, 2015 - academic.oup.com
Motivation: Drug combinations are a promising strategy for combating complex diseases by
improving the efficacy and reducing corresponding side effects. Currently, a widely studied …

A network embedding framework based on integrating multiplex network for drug combination prediction

L Yu, M Xia, Q An - Briefings in bioinformatics, 2022 - academic.oup.com
Drug combination is a sensible strategy for disease treatment because it improves the
treatment efficacy and reduces concomitant side effects. Due to the large number of possible …