PI3K inhibitors are finally coming of age
Abstract Overactive phosphoinositide 3-kinase (PI3K) in cancer and immune dysregulation
has spurred extensive efforts to develop therapeutic PI3K inhibitors. Although progress has …
has spurred extensive efforts to develop therapeutic PI3K inhibitors. Although progress has …
Targeting the PI3K/AKT/mTOR signaling pathway in the treatment of human diseases: Current status, trends, and solutions
J Huang, L Chen, J Wu, D Ai, JQ Zhang… - Journal of medicinal …, 2022 - ACS Publications
The phosphoinositide 3-kinase (PI3K)/protein kinase B (AKT)/mammalian target of
rapamycin (mTOR) pathway is one of the most important intracellular pathways involved in …
rapamycin (mTOR) pathway is one of the most important intracellular pathways involved in …
Covalent proximity scanning of a distal cysteine to target PI3Kα
Covalent protein kinase inhibitors exploit currently noncatalytic cysteines in the adenosine
5′-triphosphate (ATP)-binding site via electrophiles directly appended to a reversible …
5′-triphosphate (ATP)-binding site via electrophiles directly appended to a reversible …
Cryo-EM structures of cancer-specific helical and kinase domain mutations of PI3Kα
Phosphoinositide 3-kinases (PI3Ks) are a family of lipid kinases that perform multiple and
important cellular functions. The protein investigated here belongs to class IA of the PI3Ks; it …
important cellular functions. The protein investigated here belongs to class IA of the PI3Ks; it …
Cryo-EM structures of PI3Kα reveal conformational changes during inhibition and activation
Phosphoinositide 3-kinases (PI3Ks) are lipid kinases essential for growth and metabolism.
Their aberrant activation is associated with many types of cancers. Here we used single …
Their aberrant activation is associated with many types of cancers. Here we used single …
Advances in epilepsy: mechanisms, clinical trials, and drug therapies
T Hu, J Zhang, J Wang, L Sha, Y Xia… - Journal of medicinal …, 2023 - ACS Publications
Epilepsy is a common disease of the nervous system characterized by transient brain
dysfunction caused by an abnormal electrical discharge from the brain neurons. The …
dysfunction caused by an abnormal electrical discharge from the brain neurons. The …
Contemporary mTOR inhibitor scaffolds to diseases breakdown: A patent review (2015–2021)
P Oleksak, E Nepovimova, Z Chrienova… - European Journal of …, 2022 - Elsevier
Mechanistic target of rapamycin (mTOR) is a highly conserved protein kinase acting as a
central regulator of cell functions. The kinase forms two distinct mTOR complexes termed as …
central regulator of cell functions. The kinase forms two distinct mTOR complexes termed as …
The role of allylic strain for conformational control in medicinal chemistry
It is axiomatic in medicinal chemistry that optimization of the potency of a small molecule at a
macromolecular target requires complementarity between the ligand and target. In order to …
macromolecular target requires complementarity between the ligand and target. In order to …
Design, synthesis and bioevaluation of novel substituted triazines as potential dual PI3K/mTOR inhibitors
A series of novel substituted triazines bearing a benzimidazole scaffold were designed and
synthesized based on the structures of known anti-cancer agents, namely gedatolisib and …
synthesized based on the structures of known anti-cancer agents, namely gedatolisib and …
[HTML][HTML] Insights into potential targets for therapeutic intervention in epilepsy
C Zavala-Tecuapetla, M Cuellar-Herrera… - International journal of …, 2020 - mdpi.com
Epilepsy is a chronic brain disease that affects approximately 65 million people worldwide.
However, despite the continuous development of antiepileptic drugs, over 30% patients with …
However, despite the continuous development of antiepileptic drugs, over 30% patients with …