[HTML][HTML] Small molecules in targeted cancer therapy: advances, challenges, and future perspectives

L Zhong, Y Li, L Xiong, W Wang, M Wu… - Signal transduction and …, 2021 - nature.com
Due to the advantages in efficacy and safety compared with traditional chemotherapy drugs,
targeted therapeutic drugs have become mainstream cancer treatments. Since the first …

Challenges and opportunities in cancer drug resistance

RA Ward, S Fawell, N Floc'h, V Flemington… - Chemical …, 2020 - ACS Publications
There has been huge progress in the discovery of targeted cancer therapies in recent years.
However, even for the most successful and impactful cancer drugs which have been …

Illuminating the dark phosphoproteome

EJ Needham, BL Parker, T Burykin, DE James… - Science …, 2019 - science.org
Protein phosphorylation is a major regulator of protein function and biological outcomes.
This was first recognized through functional biochemical experiments, and in the past …

Dual-specificity, tyrosine phosphorylation-regulated kinases (DYRKs) and cdc2-like kinases (CLKs) in human disease, an overview

MF Lindberg, L Meijer - International Journal of Molecular Sciences, 2021 - mdpi.com
Dual-specificity tyrosine phosphorylation-regulated kinases (DYRK1A, 1B, 2-4) and cdc2-
like kinases (CLK1-4) belong to the CMGC group of serine/threonine kinases. These protein …

Prospects for pharmacological targeting of pseudokinases

JE Kung, N Jura - Nature Reviews Drug Discovery, 2019 - nature.com
Pseudokinases are members of the protein kinase superfamily but signal primarily through
noncatalytic mechanisms. Many pseudokinases contribute to the pathologies of human …

Alzheimer's disease beyond amyloid: Can the repetitive failures of amyloid-targeted therapeutics inform future approaches to dementia drug discovery?

K Mullane, M Williams - Biochemical pharmacology, 2020 - Elsevier
Alzheimer's Disease (AD) therapeutics based on the amyloid hypothesis have repeatedly
failed in clinical trials. Together with numerous reports that amyloid is present in brains from …

A hybrid structure-based machine learning approach for predicting kinase inhibition by small molecules

C Liu, P Kutchukian, ND Nguyen… - Journal of Chemical …, 2023 - ACS Publications
Kinases have been the focus of drug discovery programs for three decades leading to over
70 therapeutic kinase inhibitors and biophysical affinity measurements for over 130,000 …

The omnipresence of DYRK1A in human diseases

E Deboever, A Fistrovich, C Hulme… - International journal of …, 2022 - mdpi.com
The increasing population will challenge healthcare, particularly because the worldwide
population has never been older. Therapeutic solutions to age-related disease will be …

Compounds from natural sources as protein kinase inhibitors

A Baier, R Szyszka - Biomolecules, 2020 - mdpi.com
The advantage of natural compounds is their lower number of side-effects when compared
to most synthetic substances. Therefore, over the past several decades, the interest in …

Tracing the origin and evolution of pseudokinases across the tree of life

A Kwon, S Scott, R Taujale, W Yeung, KJ Kochut… - Science …, 2019 - science.org
Protein phosphorylation by eukaryotic protein kinases (ePKs) is a fundamental mechanism
of cell signaling in all organisms. In model vertebrates,~ 10% of ePKs are classified as …