A Transgenic Rat for Investigating the Anatomy and Function of Corticotrophin Releasing Factor Circuits. [PDF]
Corticotrophin-releasing factor (CRF) is a 41 amino acid neuropeptide that coordinates adaptive responses to stress. CRF projections from neurons in the central nucleus of the amygdala (CeA) to the brainstem are of particular interest for their role in ...
Blasio, Angelo +13 more
core +2 more sources
Real‐time assay of ribonucleotide reductase activity with a fluorescent RNA aptamer
Ribonucleotide reductases (RNR) synthesize DNA building blocks de novo, making them crucial in DNA replication and drug targeting. FLARE introduces the first single‐tube real‐time coupled RNR assay, which enables isothermal tracking of RNR activity at nanomolar enzyme levels and allows the reconstruction of allosteric regulatory patterns and rapid ...
Jacopo De Capitani +4 more
wiley +1 more source
Ethylphenidate: From biomarker to designer drug [PDF]
John S. Markowitz, Kennerly S. Patrick
openalex +1 more source
Catch the next designer drug: bioactivity data derived pharmacological affinity fingerprints and performance in similarity searching and unsupervised clustering [PDF]
Kedan He
openalex +1 more source
The use of a quantitative structure-activity relationship (QSAR) model to predict GABA-A receptor binding of newly emerging benzodiazepines [PDF]
The illicit market for new psychoactive substances is forever expanding. Benzodiazepines and their derivatives are one of a number of groups of these substances and thus far their number has grown year upon year.
Haegeman, Caroline +4 more
core +5 more sources
Multidrug transporters BpeB and BpeF from the Gram‐negative pathogen Burkholderia pseudomallei have a hydrophilic patch in their substrate‐binding pocket. Drug susceptibility tests and growth curve analyses using an Escherichia coli recombinant expression system revealed that the hydrophilic patches of BpeB and BpeF are involved in the substrate ...
Ui Okada, Satoshi Murakami
wiley +1 more source
Correction to: Pharmacological affinity fingerprints derived from bioactivity data for the identification of designer drugs. [PDF]
He K.
europepmc +1 more source
Bitopic binding mode of an M1 muscarinic acetylcholine receptor agonist associated with adverse clinical trial outcomes [PDF]
The realisation of the therapeutic potential of targeting the M1 muscarinic acetylcholine receptor (M1 mAChR) for the treatment of cognitive decline in Alzheimer's disease has prompted the discovery of M1 mAChR ligands showing efficacy in alleviating ...
Bradley, Sophie J. +14 more
core +1 more source
Function‐driven design of a surrogate interleukin‐2 receptor ligand
Interleukin (IL)‐2 signaling can be achieved and precisely fine‐tuned through the affinity, distance, and orientation of the heterodimeric receptors with their ligands. We designed a biased IL‐2 surrogate ligand that selectively promotes effector T and natural killer cell activation and differentiation. Interleukin (IL) receptors play a pivotal role in
Ziwei Tang +9 more
wiley +1 more source
Rapid Targeted Method of Detecting Abused Piperazine Designer Drugs. [PDF]
Welz A +3 more
europepmc +1 more source

