Protein and Peptide Letters - Volume 25, Issue 12, 2018

Peptide-derived drugs constitute a significant fraction of therapeutic agents. In 2013, The global market of peptide therapeutics was ca. $19 billion; this value does not include revenue from insulin derivatives of $28 million. The combined sales of insulin and non-insulin peptide drugs is estimated to exceed $70 billion by 2019. A significant fraction of peptide-derived drugs is composed of an amino acid sequence and additional che Read More

Background: Interactions between proteins play a key role in nearly all cellular process, and therefore, its dysregulation may lead to many different types of cellular dysfunctions. Hence, pathologic Protein-Protein Interactions (PPIs) constitute highly attractive drug targets and hold great potential for developing novel therapeutic agents for the treatment of incurable human diseases. Unfortunately, the identification of PPI inhibitors Read More

Background: Inducible Nitric Oxide Synthase (iNOS or NOS2) produces Nitric Oxide (NO) and related reactive nitrogen species, which are critical effectors of the host innate response and play key roles in the intracellular killing of bacterial and parasitic pathogens. The SPRY domain- containing SOCS box proteins SPSB1 and SPSB2 are key physiological regulators of this important enzyme. Disrupting the endogenous SPSB-iNOS i Read More

Background: Mitochondria are the primary source of energy in most tissues. Mitochondrial dysfunction results in cellular energy deficiency, triggers the production of reactive oxygen species, and initiates various cell death and inflammatory pathways. Several cell-permeable peptides (SS peptides) have been described that selectively target cardiolipin on the inner mitochondrial membrane and promote efficiency of the el Read More

Background: Tyrosine sulfation is an important post-translational modification of secreted and membrane proteins in multi-cellular organisms. This modification is catalyzed by tyrosylprotein sulfotransferases that often modify tyrosine residues in their target substrates in a heterogeneous manner. Chemokine receptors such as CCR5, which play roles in inflammation, immunity and viral infection, are sulfated on tyrosine resi Read More

Background: Venom peptides are a proven resource for identifying novel drugs, however the process of identifying bioactive venom peptides is currently labor intensive, costly, and rarely results in pharmaceutical success. As venom peptides are modulators of ion channels and receptors their potential for manipulating cell signals in diseased states are unique and offer an untapped resource for finding new medicines. Rec Read More

Background: Research has been directed at the optimization of insulin for medicinal purposes. An insulin analog that could be reversibly activated might provide more precise pharmacokinetic control and broaden the inherent therapeutic index of the hormone. The prospect of using intramolecular structural constraint to reversibly inactive insulin might constitute the first step to achieving such an optimized analog. Ch Read More