Antimony is considered a priority environmental pollutant by the EPA. The ant operon of the antimony-mining bacterium, C. testosterone, confers resistance to Sb(III). The operon is regulated by the product of the first gene in the operon, antR. This is the first report of the structure and binding properties of antR, with high selectivity for environmental antimony. Read more »
ALS Work Using Protein Crystallography
Protein crystallography is used for determining the molecular structure of proteins. Crystallized protein molecules cause a beam of incident x-rays to scatter in many directions, with constructive and destructive interference generating a diffraction pattern. By analyzing these patterns, a crystallographer can produce a three-dimensional picture of the density of electrons within the crystal and thus determine the protein's structure.
Sifting through Fragments for COVID-19 Treatments
COVID-19 vaccines are essential for preventing serious disease, but the identification of new drugs is still necessary for the treatment of patients who become sick as a result of SARS-CoV-2 infection. Here, scientists used computational docking and crystallography to screen large numbers of small molecules for potential use in drug compounds. Read more »
Scientist at Berkeley Lab Played a Hand in “Inescapable” COVID-19 Antibody Discovery
An antibody therapy that appears to neutralize all known SARS-CoV-2 strains—including newly emerged mutants that can now “escape” from previous antibody therapies—was developed with a little help from structural biologist Jay Nix. His work helped generate detailed structural maps of how antibodies bind to the spike protein, enabling the selection of promising contenders. Read more »
Researchers Set Sights on Another COVID-19 Target
Early in the COVID-19 pandemic, it was quickly established that the receptor binding domain (RBD) of the SARS-CoV-2 spike protein is a prime target for neutralizing antibodies. Now, scientists have found a second region of the spike protein that is targeted by dozens of antibodies, some of which exhibit ultrapotent neutralizing activity. Read more »
Structure of blood coagulation factor VIII in complex with an anti–C1 domain pathogenic antibody inhibitor
van der Waals sphere representation of the factor VIII C1 domain, highlighting surface‐exposed hemophilia A–associated mutations that cause impaired von Willebrand factor binding and overlap with a pathogenic anti‐C1 domain inhibitor epitope. Read more »
Guiding Target Selection for COVID-19 Antibody Therapeutics
Protein-structure studies helped demonstrate that the primary target of antibody-based COVID-19 immunity is the part of the virus’s spike protein that can most easily mutate. The work anticipated the rise of SARS-CoV-2 variants and guides the selection of antibody therapeutics that are likely to be more resistant to immune escape. Read more »
Structure-Based Design of Selective LONP1 Inhibitors for Probing In Vitro Biology
LONP1 is an AAA+ protease that maintains mitochondrial homeostasis by removing damaged or misfolded proteins. Elevated activity and expression promotes cancer cell proliferation and resistance to apoptosis-inducing reagents. Herein, we report the development of selective boronic acid-based LONP1 inhibitors using structure-based drug design as well as the first structures of human LONP1 bound to various inhibitors. Read more »
Targeting KRAS Mutant Cancers via Combination Treatment: Discovery of a 5-Fluoro-4-(3H)-quinazolinone Aryl Urea pan-RAF Kinase Inhibitor
The cover feature shows a chessboard (representative of KRAS mutant cells) and how the concerted action of the MEK inhibitor cobimetinib (rook) and the new selective pan-RAF inhibitor GNE-0749 (queen) force the opposing king (phospho-ERK, the downstream signaling node of RAF and MEK) into checkmate. Read more »
Mystery Protein Helps COVID–19 Avoid Immunity
Using the Advanced Light Source (ALS), researchers solved the structure of ORF8, a protein specific to SARS-CoV-2. Understanding the structure of ORF8 opens the door to therapy studies targeting SARS-CoV-2, the virus responsible for causing COVID-19. Read more »
Construction, characterization and crystal structure of a fluorescent single-chain Fv chimera
In vitro display technologies based on phage and yeast have a successful history of selecting single-chain variable fragment (scFv) antibodies against various targets. However, single-chain antibodies are often unstable and poorly expressed. We explore the feasibility of converting scFv antibodies to an intrinsically fluorescent format by inserting a monomeric, stable fluorescent protein between the light- and heavy-chain variable regions. Read more »
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