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A SARS-CoV-2 Protein Interaction Map Reveals Targets for Drug-Repurposing
A human–SARS-CoV-2 protein interaction map highlights cellular processes that are hijacked by the virus and that can be targeted by existing drugs, including inhibitors of mRNA translation and predicted regulators of the sigma receptors.
Evolving the lock to fit the key to create a family of G protein-coupled receptors potently activated by an inert ligand
- B. Armbruster, Xiang Li, M. Pausch, S. Herlitze, B. Roth
- BiologyProceedings of the National Academy of Sciences
- 20 March 2007
A facile approach for designing families of GPCRs with engineered ligand specificities will prove to be powerful tools for selectively modulating signal-transduction pathways in vitro and in vivo.
Rapid, reversible activation of AgRP neurons drives feeding behavior in mice.
Using designer receptors exclusively activated by designer drugs (DREADD) technology to provide specific and reversible regulation of neuronal activity in mice, it is demonstrated that acute activation of AgRP neurons rapidly and dramatically induces feeding, reduces energy expenditure, and ultimately increases fat stores.
Morphometric evidence for neuronal and glial prefrontal cell pathology in major depression∗ ∗ See accompanying Editorial, in this issue.
Relating protein pharmacology by ligand chemistry
- Michael J. Keiser, B. Roth, B. Armbruster, P. Ernsberger, J. Irwin, B. Shoichet
- BiologyNature Biotechnology
- 1 February 2007
This work began with 65,000 ligands annotated into sets for hundreds of drug targets, and found that methadone, emetine and loperamide (Imodium) may antagonize muscarinic M3, α2 adrenergic and neurokinin NK2 receptors, respectively.
Remote Control of Neuronal Activity in Transgenic Mice Expressing Evolved G Protein-Coupled Receptors
The expanded biology of serotonin.
New work suggests that serotonin may regulate some processes, including platelet aggregation, by receptor-independent, transglutaminase-dependent covalent linkage to cellular proteins.
Aripiprazole, A Novel Atypical Antipsychotic Drug with a Unique and Robust Pharmacology
The results support the hypothesis that the unique actions of aripiprazole in humans are likely a combination of ‘functionally selective’ activation of D2 (and possibly D3)-dopamine receptors, coupled with important interactions with selected other biogenic amine receptors—particularly 5-HT receptor subtypes (5-HT1A, 5- HT2A).
Magic shotguns versus magic bullets: selectively non-selective drugs for mood disorders and schizophrenia
It is proposed that designing selectively non-selective drugs (that is, 'magic shotguns') that interact with several molecular targets will lead to new and more effective medications for a variety of central nervous system disorders.