Targeting p53–MDM2 interaction by small-molecule inhibitors: Learning from MDM2 inhibitors in clinical trials
H Zhu, H Gao, Y Ji, Q Zhou, Z Du, L Tian… - Journal of hematology & …, 2022 - Springer
Abstract p53, encoded by the tumor suppressor gene TP53, is one of the most important
tumor suppressor factors in vivo and can be negatively regulated by MDM2 through p53 …
tumor suppressor factors in vivo and can be negatively regulated by MDM2 through p53 …
Reaching for high-hanging fruit in drug discovery at protein–protein interfaces
Targeting the interfaces between proteins has huge therapeutic potential, but discovering
small-molecule drugs that disrupt protein–protein interactions is an enormous challenge …
small-molecule drugs that disrupt protein–protein interactions is an enormous challenge …
Intrinsically Disordered Proteins in Human Diseases: Introducing the D2 Concept
Intrinsically disordered proteins (IDPs) lack stable tertiary and/or secondary structures under
physiological conditions in vitro. They are highly abundant in nature and their functional …
physiological conditions in vitro. They are highly abundant in nature and their functional …
Understanding protein non-folding
This review describes the family of intrinsically disordered proteins, members of which fail to
form rigid 3-D structures under physiological conditions, either along their entire lengths or …
form rigid 3-D structures under physiological conditions, either along their entire lengths or …
A decade and a half of protein intrinsic disorder: biology still waits for physics
VN Uversky - Protein Science, 2013 - Wiley Online Library
The abundant existence of proteins and regions that possess specific functions without
being uniquely folded into unique 3D structures has become accepted by a significant …
being uniquely folded into unique 3D structures has become accepted by a significant …
Fluorescence polarization assays in small molecule screening
WA Lea, A Simeonov - Expert opinion on drug discovery, 2011 - Taylor & Francis
Importance of the field: Fluorescence polarization (FP) is a homogeneous method that
allows rapid and quantitative analysis of diverse molecular interactions and enzyme …
allows rapid and quantitative analysis of diverse molecular interactions and enzyme …
The unfoldomics decade: an update on intrinsically disordered proteins
Background Our first predictor of protein disorder was published just over a decade ago in
the Proceedings of the IEEE International Conference on Neural Networks (Romero P …
the Proceedings of the IEEE International Conference on Neural Networks (Romero P …
Oncogenic protein interfaces: small molecules, big challenges
Historically, targeting protein–protein interactions with small molecules was not thought
possible because the corresponding interfaces were considered mostly flat and featureless …
possible because the corresponding interfaces were considered mostly flat and featureless …
The δ isoform of CaM kinase II is required for pathological cardiac hypertrophy and remodeling after pressure overload
J Backs, T Backs, S Neef… - Proceedings of the …, 2009 - National Acad Sciences
Acute and chronic injuries to the heart result in perturbation of intracellular calcium
signaling, which leads to pathological cardiac hypertrophy and remodeling …
signaling, which leads to pathological cardiac hypertrophy and remodeling …
Features of protein–protein interactions that translate into potent inhibitors: topology, surface area and affinity
Protein–protein interactions (PPIs) control the assembly of multi-protein complexes and,
thus, these contacts have enormous potential as drug targets. However, the field has …
thus, these contacts have enormous potential as drug targets. However, the field has …