Cryo-electron microscopy (cryo-EM) of non-crystalline single particles is a biophysical
technique that can be used to determine the structure of biological macromolecules and …

The carbamate group is a key structural motif in many approved drugs and prodrugs. There
is an increasing use of carbamates in medicinal chemistry and many derivatives are …

HIV-1 protease inhibitors continue to play an important role in the treatment of HIV/AIDS,
transforming this deadly ailment into a more manageable chronic infection. Over the years …

Three-dimensional molecular structures can provide detailed information on biological
mechanisms and, for cases in which the molecular function affects human health, can …

Proteases form one of the largest and more important groups of enzymes. They selectively
catalyze the hydrolysis of peptide bonds and can be divided into four major classes …

Most drugs have been discovered in random screens or by exploiting information about
macromolecular receptors. One source of this information is in the structures of critical …

▪ Abstract Retroviral protease (PR) from the human immunodeficiency virus type 1 (HIV-1)
was identified over a decade ago as a potential target for structure-based drug design. This …

It has now been two decades since acquired immunodeficiency syndrome (AIDS) was first
reported by the US Center for Diseases Control (CDC). A few years later, it was found that a …

Mechanistic information and structure-based design methods have been used to design a
series of nonpeptide cyclic ureas that are potent inhibitors of human immunodeficiency virus …

Proline residues confer unique structural constraints on peptide chains and markedly
influence the susceptibility of proximal peptide bonds to protease activity. This review …