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View article: Quantification of Binding of Small Molecules to Native Proteins Overexpressed in Living Cells
Quantification of Binding of Small Molecules to Native Proteins Overexpressed in Living Cells Open
The affinity and selectivity of small molecules for proteins drive drug discovery and development. We report a fluorescent probe cellular binding assay (FPCBA) for determination of these values for native (untagged) proteins overexpressed …
View article: Quantification of Engagement of Microtubules by Small Molecules in Living Cells by Flow Cytometry
Quantification of Engagement of Microtubules by Small Molecules in Living Cells by Flow Cytometry Open
Drugs such as paclitaxel (Taxol) that bind microtubules are widely used for the treatment of cancer. Measurements of the affinity and selectivity of these compounds for their targets are largely based on studies of purified proteins, and o…
View article: Phenylsulfamoyl Benzoic Acid Inhibitor of ERAP2 with a Novel Mode of Inhibition
Phenylsulfamoyl Benzoic Acid Inhibitor of ERAP2 with a Novel Mode of Inhibition Open
ERAP1 and ERAP2 are endoplasmic reticulum zinc-binding aminopeptidases that play crucial roles in processing peptides for loading onto class I major histocompatibility complex proteins. These enzymes are therapeutic targets in cancer and a…
View article: Visible photorelease of liquid biopsy markers following microfluidic affinity-enrichment
Visible photorelease of liquid biopsy markers following microfluidic affinity-enrichment Open
We detail a heterobifunctional, 7-aminocoumarin photocleavable (PC) linker with unique properties to covalently attach Abs to surfaces and subsequently release them with visible light (400–450 nm).
View article: Discovery of Selective Inhibitors of Endoplasmic Reticulum Aminopeptidase 1
Discovery of Selective Inhibitors of Endoplasmic Reticulum Aminopeptidase 1 Open
ERAP1 is an endoplasmic reticulum-resident zinc aminopeptidase that plays an important role in the immune system by trimming peptides for loading onto major histocompatibility complex proteins. Here, we report discovery of the first inhibi…
View article: High-Throughput Screening for Bacterial Glycosyltransferase Inhibitors
High-Throughput Screening for Bacterial Glycosyltransferase Inhibitors Open
The enteropathogenic and enterohemorrhagic Escherichia coli NleB proteins as well as the Salmonella enterica SseK proteins are type III secretion system effectors that function as glycosyltransferase enzymes to post-translationally modify …
View article: Targeting Fluorescent Sensors to Endoplasmic Reticulum Membranes Enables Detection of Peroxynitrite During Cellular Phagocytosis
Targeting Fluorescent Sensors to Endoplasmic Reticulum Membranes Enables Detection of Peroxynitrite During Cellular Phagocytosis Open
Peroxynitrite is a highly reactive oxidant derived from superoxide and nitric oxide. In normal vertebrate physiology, some phagocytes deploy this oxidant as a cytotoxin against foreign pathogens. To provide a new approach for detection of …
View article: CCDC 1486207: Experimental Crystal Structure Determination
CCDC 1486207: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 1015958: Experimental Crystal Structure Determination
CCDC 1015958: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …