The technology presents a novel structural modification of an existing first generation Grp94 selective inhibitor to generate a second generation Grp94-specific scaffold which has greater affinity and selectivity compared to existing inhibitors and prevents unfavorable binding of other Hsp90 isoforms.
The invention consists of compounds for the treatment of parasitic diseases such as Trypanosomiasis and Leishmaniasis. Compounds are first-in-class, and selectively targeted towards pathogenic cells with nanomolar potency.
This invention provides an improved method for producing a novel interfacing capillary device that is less costly and more durable than existing sheathless devices. This simplified production method does not require sample dilution, etching, or precision hand tools, and is automated and reproducible.
This invention describes the first selective inhibitor of heat shock protein 90 kDa beta (Hsp90β). The invented inhibitor selectively binds to the N-terminus of Hsp90β and may be developed for the treatment of cancers. The inhibitor was developed based on the sequence alignment of the N-terminal ATP-binding domains of Hsp90α and Hsp90β complexed with a non-selective Hsp90 inhibitor, which revealed Hsp90β-specific residues that were key to exploit the selectivity of the new inhibitor.
Structural modification of a non-selective aminocyclohexanol-based heat shock protein 90 KDa (Hsp90) inhibitor led to a highly selective inhibitor of glucose regulated protein 94 kDa (Grp94). The new Grp94-selective inhibitor can be used to develop an effective therapy for the treatment of metastatic cancer and/or primary open angle glaucoma (POAG).
Use of a genetic dereplication strategy eliminates major known SM biosynthetic pathways in Aspergillus nidulans, reducing the complexity of SM profiles and activating an abundance of silent SM gene clusters to enable identification of a new pool of fungal products for drug discovery.
Selective heat shock protein 90 (Hsp90) and glucose regulated protein 94 (Grp94) inhibitors that can be used to develop an effective therapy for treating primary open angle glaucoma (POAG).
The small molecules in this work represent a novel composition of matter that can be used as either Kappa Opioid Receptor (KOR) agonists or antagonists. Further some of the compounds have been shown to weak agonists making them ideal to explore for the use of addiction.
Broad based label-free systems identify protein stabilizers at physiological or near physiological conditions that specifically inhibit Bacterial Toxin or Viral entry into cells.
PEPCK is an enzyme critical in the process of gluconeogenesis whose inhibition could be used to treat hyperglycemia and diabetes.