[HTML][HTML] MLKL: Functions beyond serving as the Executioner of Necroptosis

C Zhan, M Huang, X Yang, J Hou - Theranostics, 2021 - ncbi.nlm.nih.gov
Recently, necroptosis, as a programmed cell death pathway, has drawn much attention as it
has been implicated in multiple pathologies, especially in the field of inflammatory diseases …

Molecular insights into the mechanism of necroptosis: the necrosome as a potential therapeutic target

J Chen, R Kos, J Garssen, F Redegeld - Cells, 2019 - mdpi.com
Necroptosis, or regulated necrosis, is an important type of programmed cell death in addition
to apoptosis. Necroptosis induction leads to cell membrane disruption, inflammation and …

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 …

From (tool) bench to bedside: the potential of necroptosis inhibitors

CR Gardner, KA Davies, Y Zhang… - Journal of Medicinal …, 2023 - ACS Publications
Necroptosis is a regulated caspase-independent form of necrotic cell death that results in an
inflammatory phenotype. This process contributes profoundly to the pathophysiology of …

PROTACs targeting MLKL protect cells from necroptosis

OH Rathje, L Perryman, RJ Payne… - Journal of Medicinal …, 2023 - ACS Publications
Mixed Lineage Kinase domain-Like pseudokinase (MLKL) is implicated in a broad range of
diseases due to its role as the ultimate effector of necroptosis and has therefore emerged as …

Small-molecule inhibitors of necroptosis: current status and perspectives

C Zhuang, F Chen - Journal of Medicinal Chemistry, 2019 - ACS Publications
Necroptosis, an important form of programmed cell death (PCD), is a highly regulated
caspase-independent type of cell death that plays a critical role in the pathophysiology of …

Phosphorylation-dependent pseudokinase domain dimerization drives full-length MLKL oligomerization

Y Meng, SE Garnish, KA Davies, KA Black… - Nature …, 2023 - nature.com
The necroptosis pathway is a lytic, pro-inflammatory mode of cell death that is widely
implicated in human disease, including renal, pulmonary, gut and skin inflammatory …

Pseudokinases: update on their functions and evaluation as new drug targets

DP Byrne, DM Foulkes, PA Eyers - Future medicinal chemistry, 2017 - Taylor & Francis
The pseudokinase complement of the human kinase superfamily consists of approximately
60 signaling proteins, which lacks one or more of the amino acids typically required to …

Modulating undruggable targets to overcome cancer therapy resistance

C Passirani, A Vessières, G La Regina, W Link… - Drug Resistance …, 2022 - Elsevier
Many cancer patients frequently fail to respond to anti-cancer treatment due to therapy
resistance which is the major obstacle towards curative cancer treatment. Therefore …

Locking mixed-lineage kinase domain-like protein in its auto-inhibited state prevents necroptosis

M Rübbelke, D Fiegen, M Bauer… - Proceedings of the …, 2020 - National Acad Sciences
As an alternative pathway of controlled cell death, necroptosis can be triggered by tumor
necrosis factor via the kinases RIPK1/RIPK3 and the effector protein mixed-lineage kinase …