A number of clinically validated drugs have been developed by repurposing the CUL4-DDB1-CRBN-RBX1 (CRL4CRBN) E3 ubiquitin ligase complex with molecular glue degraders to eliminate disease-driving proteins. Here, we present the identification of a first-in-class GSPT1-selective cereblon E3 ligase modulator, CC-90009, that targets acute myeloid leukemia blasts and leukemia stem cells. Read more »
The Odd Structure of ORF8: Scientists Map the Coronavirus Protein Linked to Immune Evasion and Disease Severity
Researchers determined the atomic structure of a coronavirus protein thought to help the pathogen evade and dampen response from human immune cells. Researchers determined the atomic structure of a coronavirus protein thought to help the pathogen evade and dampen response from human immune cells. Read more »
Experimental Drug Targets HIV in a Novel Way
Researchers from Gilead Sciences Inc. solved the structure of an experimental HIV drug bound to a novel target: the capsid protein that forms a shield around the viral RNA. The work could lead to a long-lasting HIV treatment that overcomes the problem of drug resistance and avoids the need for burdensome daily pill-taking. Read more »
Jennifer Doudna and the Nobel Prize: The Advanced Light Source Perspective
The 2020 Nobel Prize in Chemistry was awarded to Jennifer Doudna and Emmanuelle Charpentier for the development of a world-changing gene-editing technology. At the ALS, Doudna’s work on CRISPR-Cas9 was enabled by many visionary people with innovative ideas, implemented in support of a world-class structural biology program. Read more »
Study Finds ‘Missing Link’ in the Evolutionary History of Carbon-Fixing Protein Rubisco
Scientists discovered an ancient form of rubisco, the most abundant enzyme on Earth and critical to life as we know it. Found in previously unknown environmental microbes, the newly identified rubisco provides insight into the evolution of the photosynthetic organisms that underlie the planet’s food chains. Read more »
Targeting the trypanosome kinetochore with CLK1 protein kinase inhibitors
Saldivia et al. identify CLK1 as the target for the amidobenzimidazoles series of compounds. Inhibition of this protein kinase impairs inner kinetochore recruitment, causing cell-cycle arrest and cell death in trypanosomal pathogens such as Trypanosoma brucei. Read more »
Providing New Technologies for Vaccine Development
Antigens can sometimes be attached to a protein scaffold to mimic the shape of a virus and elicit a stronger immune response. Scientists developed a method to design such proteins, and ALS data helped to visualize the atomic structure and determine the dynamics of the designed scaffolds. Read more »
Missing Lysine Link Could Improve Plant-Based Nutrition
To engineer crops with higher levels of the important amino acid, lysine, researchers solved the structure of an enzyme that helps break down lysine in plants. A fuller understanding of the factors affecting lysine levels should aid in the successful development of stable high-lysine crops to combat malnutrition globally. Read more »
Rotavirus VP3 Is a Multifunctional Capping Machine
Rotavirus, a major cause of infantile gastroenteritis, is responsible for the deaths of about 200,000 children per year. Although vaccines are available, the virus still circulates, and a fuller understanding of the viral structures is needed. Here, scientists investigate the structure and function of the last unsolved rotavirus structural protein. Read more »
Evaluation of Free Energy Calculations for the Prioritization of Macrocycle Synthesis
Free energy perturbation methods represent a paradigm shift in drug discovery, where computational methods inform benchtop activities. Macrocycles are highly constrained molecules, often resulting in nonintuitive structure–activity relationships requiring lengthy synthetic routes. Free energy perturbation methods can be used to predict potency, guiding synthetic chemistry efforts to de-risk complex synthesis. Read more »
- « Previous Page
- 1
- 2
- 3
- 4
- 5
- …
- 9
- Next Page »