Fragment-based drug discovery is a strategy widely used in both academia and
pharmaceutical companies to generate small-molecule protein inhibitors and drug …

The neuropharmacological community has shown a strong interest in AMPA receptors as
critical components of excitatory synaptic transmission during the last fifteen years. AMPA …

Fragment-based drug discovery (FBDD) has grown and matured to a point where it is
valuable to keep track of its extent and details of application. This Perspective summarizes …

This Perspective, the fourth in an annual series, summarizes fragment-to-lead (F2L) success
stories published during 2018. Topics such as target class, screening methods …

L-Glutamic acid is the main excitatory neurotransmitter in the central nervous system (CNS).
Its associated receptors localized on neuronal and non-neuronal cells mediate rapid …

Introduction In fragment-based drug design, fragment linking is a popular strategy where two
fragments binding to different sub-pockets of a target are linked together. This attractive …

Tetrazines (Tz) have been applied as bioorthogonal agents for various biomedical
applications, including pretargeted imaging approaches. In radioimmunoimaging …

Transition-metal-free multicomponent reactions involving aryne precursors, secondary
amines, and sulfuryl fluoride are reported herein. Zwitterionic intermediates formed from the …

Fragment‐based drug discovery (FBDD) is a method of identifying small molecule hits that
can be elaborated rationally through fragment growing, merging and linking, to afford high …

This paper summarizes the present knowledge on how positive allosteric modulators
(PAMs) interact with the ligand‐binding domain (LBD) of AMPA and kainate receptors …