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.
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).
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.
This invention consists of a novel compound and method for treating Polycystic Kidney Disease utilizing a novel liver kinase B1 (LKB1) activator to stimulate AMP-activated protein kinase (AMPK), leading to inhibition of mTOR-mediated cellular proliferation and chloride-dependent fluid secretion, key components of cyst growth.
A novel class of small molecule Alpha, Beta-ABAD interaction inhibitors for the treatment of Alzheimer's Disease.