Award Data

DESCRIPTION (provided by applicant): Reactive oxygen species (ROS) are involved in numerous cell-signaling pathways. They have been implicated in over 150 diseases including cancer, arthritis, Parkinson's disease, diabetes, myocardial infarction and atherosclerosis. The need to understand the role of ROS in these processes is evidenced by the 80,000 publications in this field during the last ...

DESCRIPTION (provided by applicant): The perioral route for drug administration remains the most convenient way of clinical therapy and is preferred by patients, however, good bioavailability is a necessary characteristic of new candidate therapeutics. A key parameter for determining oral bioavailability is drug transport and permeability across the small intestine (SI) epithelium. Therefore, in ...

DESCRIPTION (provided by applicant): Aquilus Pharmaceuticals, Inc. proposes to evaluate the effects of a proprietary matrix metalloproteinase (MMP) inhibitor, AQU-010, for blocking neuropathic pain and morphine tolerance in a thermal injury (TI) rat model.The goals for Phase I are to scale-up the synthesis of AQU-010, determine its oral pharmacokinetics (PK) and target tissue penetration and then ...

ABSTRACT In this project we propose to exploit the recent successful isolation and reconstitution of the important ATP- dependent drug efflux transporter, ABCG2 (BCRP, Breast Cancer Resistance Protein), and combine it with a new transport assay system, the Fluorosome platform, to characterize the interaction of ABCG2 with drugs and drug candidates. The result will provide a useful, novel, highly ...

DESCRIPTION (provided by applicant): There is enormous potential of oligonucleotides (ON) as therapeutics, but the challenge remains how to effectively deliver ON into cells. Currently, there are no effective and reliable ways of delivery. Outer cell membranes resist the cellular uptake of charged ON, and charges-eliminating backbone modifications such as those in peptide nucleic acids (PNA) and m ...

DESCRIPTION (provided by applicant): Covalent drugs represent a significant portion of current pharmaceuticals, with the top 26 having sales of over 30B in the US alone. While in the past target-directed drug discovery projects rarely pursued covalent binders due to safety concerns, the industry is increasingly considering the use of targeted covalent inhibitors (TCIs) that utilize soft reactive ...

Abstract Currently, there are no molecular probes that are specifically designed for quantitative imaging of articular cartilage health. In osteoarthritis (OA), the articular cartilage becomes degraded with loss of glycosaminoglycans (GAGs) from the cartilage matrix serving as an early biomarker of the disease process. As such, there are clinical opportunities to mitigate cartilage damage in patie ...

DESCRIPTION (provided by applicant): The proposed research focuses on the development DNP-enhanced high-resolution magic-angle-spinning (HRMAS) magnetic resonance spectroscopy (MRS) to quantify cellular metabolities within intact prostate tissue. This willallow the study of micro-dissected pure pathological features, which is currently not possible due to the sensitivity limitations of the method ...

DESCRIPTION (provided by applicant): Radioluminescence microscopy is a newly developed method for imaging radionuclide uptake in live single cells. Current methods of radiotracer imaging are limited to measuring the average radiotracer uptake in large cellpopulations and, as a result, lack the ability to quantify cell-to-cell variations. With the new radio- luminescence microscopy technique, howe ...

DESCRIPTION (provided by applicant): The objective of this proposal is to introduce a product that will enable protein separations by gel electrophoresis (SDS-PAGE) to be analyzed as peptides by mass spectrometry in an efficient, high-throughput manner. Such a device will offer investigators in biology and medicine a compelling new method for analyzing complex proteomic samples (100s - 1000s of in ...