Results 201 to 210 of about 232,253 (352)

Covalent drug discovery: Progress against key targets, emerging strategies and lessons learnt

open access: yesBritish Journal of Pharmacology, EarlyView.
Abstract Covalent drug discovery is currently experiencing a boom in industrial and academic interest. To date, at least 75 covalent drugs have received regulatory approval, targeting both traditional target classes and more challenging proteins for which other approaches failed. In many cases, unique aspects of covalent targeting are essential for the
Charles P. Brown   +2 more
wiley   +1 more source

Feedback control of excitability and high K+ induced epileptiform bursts in male rat hippocampal slices with a photocaged adenosine A1 receptor agonist

open access: yesBritish Journal of Pharmacology, EarlyView.
Background and Purpose Adenosine is a potent regulator of neurotransmission and neuronal excitability, through activation of Gi coupled adenosine A1 receptors (A1Rs). Adenosine has gained interest as an anticonvulsant because of its endogenous involvement in ending seizure activity, but peripheral side effects require local application.
Erine Craey   +8 more
wiley   +1 more source

Transcriptional Reinforcement of the HER2–RAS Network in HER2‐Positive Gastric Cancer: The RUNX–SOS1 Axis in Context

open access: yesCancer Science, EarlyView.
RUNX‐dependent transcriptional control of SOS1 reinforces HER2–RAS signaling and may attenuate responses to HER2‐targeted therapies in HER2‐positive gastric cancer. ABSTRACT HER2‐positive gastric cancer represents a distinct molecular subtype characterized by chromosomal instability, variable HER2 amplification, and substantial intratumoral ...
Tatsuya Masuda   +3 more
wiley   +1 more source

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