[HTML][HTML] Properties of FDA-approved small molecule protein kinase inhibitors: A 2023 update

R Roskoski Jr - Pharmacological research, 2023 - Elsevier
Owing to the dysregulation of protein kinase activity in many diseases including cancer, this
enzyme family has become one of the most important drug targets in the 21 st century. There …

PROTACs: great opportunities for academia and industry

X Sun, H Gao, Y Yang, M He, Y Wu, Y Song… - Signal transduction and …, 2019 - nature.com
Although many kinds of therapies are applied in the clinic, drug-resistance is a major and
unavoidable problem. Another disturbing statistic is the limited number of drug targets, which …

Progress towards therapies for disease modification in Parkinson's disease

N Vijiaratnam, T Simuni, O Bandmann… - The Lancet …, 2021 - thelancet.com
The development of interventions to slow or halt the progression of Parkinson's disease
remains a priority for patients and researchers alike. To date, no agents have been shown to …

Modular PROTAC design for the degradation of oncogenic BCR‐ABL

AC Lai, M Toure, D Hellerschmied… - Angewandte Chemie …, 2016 - Wiley Online Library
Abstract Proteolysis Targeting Chimera (PROTAC) technology is a rapidly emerging
alternative therapeutic strategy with the potential to address many of the challenges …

Quantitative chemical proteomics reveals mechanisms of action of clinical ABL kinase inhibitors

M Bantscheff, D Eberhard, Y Abraham, S Bastuck… - Nature …, 2007 - nature.com
We describe a chemical proteomics approach to profile the interaction of small molecules
with hundreds of endogenously expressed protein kinases and purine-binding proteins. This …

Regulation of α-synuclein by chaperones in mammalian cells

BM Burmann, JA Gerez, I Matečko-Burmann… - Nature, 2020 - nature.com
Neurodegeneration in patients with Parkinson's disease is correlated with the occurrence of
Lewy bodies—intracellular inclusions that contain aggregates of the intrinsically disordered …

Molecular biology of bcr-abl1–positive chronic myeloid leukemia

A Quintás-Cardama, J Cortes - Blood, The Journal of the …, 2009 - ashpublications.org
Chronic myeloid leukemia (CML) has been regarded as the paradigmatic example of a
malignancy defined by a unique molecular event, the BCR-ABL1 oncogene. Decades of …

Role of ABL family kinases in cancer: from leukaemia to solid tumours

EK Greuber, P Smith-Pearson, J Wang… - Nature Reviews …, 2013 - nature.com
The Abelson (ABL) family of nonreceptor tyrosine kinases, ABL1 and ABL2, transduces
diverse extracellular signals to protein networks that control proliferation, survival, migration …

Optimized hydrophobic interactions and hydrogen bonding at the target-ligand interface leads the pathways of drug-designing

R Patil, S Das, A Stanley, L Yadav, A Sudhakar… - PloS one, 2010 - journals.plos.org
Background Weak intermolecular interactions such as hydrogen bonding and hydrophobic
interactions are key players in stabilizing energetically-favored ligands, in an open …

Bruton's tyrosine kinase (BTK) inhibitors and autoimmune diseases: making sense of BTK inhibitor specificity profiles and recent clinical trial successes and failures

GE Ringheim, M Wampole, K Oberoi - Frontiers in immunology, 2021 - frontiersin.org
Clinical development of BTK kinase inhibitors for treating autoimmune diseases has lagged
behind development of these drugs for treating cancers, due in part from concerns over the …