Andrew C. Kruse
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View article: Conformational regulation of two essential activators of bacterial cell elongation
Conformational regulation of two essential activators of bacterial cell elongation Open
The peptidoglycan (PG) cell wall is critical for bacterial growth and survival and is a primary antibiotic target. MreD is an essential accessory factor of the Rod complex, which carries out PG synthesis during elongation, yet little is kn…
View article: Structural insights into G protein-coupled receptor signaling
Structural insights into G protein-coupled receptor signaling Open
G protein-coupled receptors (GPCRs) are the largest single family of transmembrane proteins encoded in the human genome, and they are among the most successful classes of therapeutic drug targets of all time. Signaling by GPCRs relies on a…
View article: GPCR Antagonism via Antibody-Mediated Rewiring of Receptor Trafficking and Degradation
GPCR Antagonism via Antibody-Mediated Rewiring of Receptor Trafficking and Degradation Open
G-protein coupled receptors (GPCRs) represent one of the most important yet incompletely targeted classes of therapeutic proteins. Here, we report a novel strategy for functional GPCR antagonism through antibody-mediated endocytosis and ly…
View article: β-arrestin recruitment facilitates a direct association with G proteins
β-arrestin recruitment facilitates a direct association with G proteins Open
G protein-coupled receptors (GPCRs) are targets for almost a third of all FDA-approved drugs. GPCRs are known to signal through both heterotrimeric G proteins and β-arrestins. Traditionally these pathways were viewed as largely separable, …
View article: Decoding protein-peptide interactions using a large, target-agnostic yeast surface display library
Decoding protein-peptide interactions using a large, target-agnostic yeast surface display library Open
Protein-peptide interactions underlie key biological processes and are commonly utilized in biomedical research and therapeutic discovery. It is often desirable to identify peptide sequence properties that confer high-affinity binding to a…
View article: G Protein Selectivity in Dopamine Receptors is Determined before GDP Release
G Protein Selectivity in Dopamine Receptors is Determined before GDP Release Open
Dopaminergic signaling in neurophysiological processes utilizes multiple G proteins. The dopamine receptor subtypes D1R/D5R selectively couple to Gs/olf proteins, while D2R/D3R/D4R is selective for Gi/o proteins. The molecular mechanisms u…
View article: Epitope-directed selection of GPCR nanobody ligands with evolvable function
Epitope-directed selection of GPCR nanobody ligands with evolvable function Open
Antibodies have the potential to target G protein–coupled receptors (GPCRs) with high receptor, cellular, and tissue selectivity; however, few antibody ligands for GPCRs exist. Here, we describe a generalizable selection method to enrich f…
View article: <i>In silico</i> discovery of nanobody binders to a G-protein coupled receptor using AlphaFold-Multimer
<i>In silico</i> discovery of nanobody binders to a G-protein coupled receptor using AlphaFold-Multimer Open
Antibodies are central mediators of the adaptive immune response, and they are powerful research tools and therapeutics. Antibody discovery requires substantial experimental effort, such as immunization campaigns or in vitro library screen…
View article: Isolation of PCSK9-specific nanobodies from synthetic libraries using a combined protein selection strategy
Isolation of PCSK9-specific nanobodies from synthetic libraries using a combined protein selection strategy Open
Nanobodies (Nbs) hold great potential to replace conventional antibodies in various biomedical applications. However, conventional methods for their discovery can be time-consuming and expensive. We have developed a reliable protein select…
View article: The hit-and-run of cell wall synthesis: LpoB transiently binds and activates PBP1b through a conserved allosteric switch
The hit-and-run of cell wall synthesis: LpoB transiently binds and activates PBP1b through a conserved allosteric switch Open
The peptidoglycan (PG) cell wall is the primary protective layer of bacteria, making the process of PG synthesis a key antibiotic target. Class A penicillin-binding proteins (aPBPs) are a family of conserved and ubiquitous PG synthases tha…
View article: MreC-MreD structure reveals a multifaceted interface that controls MreC conformation
MreC-MreD structure reveals a multifaceted interface that controls MreC conformation Open
The peptidoglycan (PG) cell wall is critical for bacterial growth and survival and is a primary antibiotic target. MreD is an essential accessory factor of the Rod complex, which carries out PG synthesis during elongation, yet little is kn…
View article: Engineering and Characterization of a Long-Half-Life Relaxin Receptor RXFP1 Agonist
Engineering and Characterization of a Long-Half-Life Relaxin Receptor RXFP1 Agonist Open
Relaxin-2 is a peptide hormone with important roles in human cardiovascular and reproductive biology. Its ability to activate cellular responses such as vasodilation, angiogenesis, and anti-inflammatory and antifibrotic effects has led to …
View article: Structures of the σ2 receptor enable docking for bioactive ligand discovery
Structures of the σ2 receptor enable docking for bioactive ligand discovery Open
The σ2 receptor has attracted intense interest in cancer imaging1, psychiatric disease2, neuropathic pain3–5 and other areas of biology6,7. Here we determined the crystal structure of this receptor in complex with the clinical candidate ro…
View article: A spatiotemporal map of co-receptor signaling networks underlying B cell activation
A spatiotemporal map of co-receptor signaling networks underlying B cell activation Open
The B cell receptor (BCR) signals together with a multi-component co-receptor complex to initiate B cell activation in response to antigen binding. Here, we take advantage of peroxidase-catalyzed proximity labeling combined with quantitati…
View article: COVID-19: Famotidine, Histamine, Mast Cells, and Mechanisms
COVID-19: Famotidine, Histamine, Mast Cells, and Mechanisms Open
SARS-CoV-2 infection is required for COVID-19, but many signs and symptoms of COVID-19 differ from common acute viral diseases. SARS-CoV-2 infection is necessary but not sufficient for development of clinical COVID-19 disease. Currently, t…
View article: AlphaFold2 structures guide prospective ligand discovery
AlphaFold2 structures guide prospective ligand discovery Open
AlphaFold2 (AF2) models have had wide impact but mixed success in retrospective ligand recognition. We prospectively docked large libraries against unrefined AF2 models of the σ 2 and serotonin 2A (5-HT2A) receptors, testing hundreds of ne…
View article: SpoVAF and FigP assemble into oligomeric ion channels that enhance spore germination
SpoVAF and FigP assemble into oligomeric ion channels that enhance spore germination Open
Bacterial spores can remain dormant for decades yet rapidly germinate and resume growth in response to nutrients. GerA family receptors that sense and respond to these signals have recently been shown to oligomerize into nutrient-gated ion…
View article: AlphaFold2 structures template ligand discovery
AlphaFold2 structures template ligand discovery Open
AlphaFold2 (AF2) and RosettaFold have greatly expanded the number of structures available for structure-based ligand discovery, even though retrospective studies have cast doubt on their direct usefulness for that goal. Here, we tested unr…