C07K5/11

Novel Peptides and Analogs for Use in the Treatment of Oral Mucositis

Preclinical data obtained in models of chemotherapy-induced mucositis, radiation-induced mucositis, neutropenic infection and colitis indicate oral mucositis is a promising indication for Innate Defense Regulator (IDR) peptides. Preclinical efficacy results obtained with IDRs in mouse and hamster models of mucositis indicate that dosing every third day should be able to cover the mucositis window with seven to fourteen doses, depending on the duration of chemotherapy or radiation exposure. IDRs have also shown efficacy in mouse models of chemotherapy-induced oral and gastrointestinal mucositis, consistent with the response of the innate immune response to chemotherapy and/or radiation damage. IDRs are also effective at reducing bacterial burden and improve survival in the presence or absence of antibiotic treatment in various murine infection models.

Fluorescent imaging agents

Provided is a family of intramolecularly quenched imaging agents for use in both in vivo and in vitro imaging that contain at least one enzymatically cleavable oligopeptide and two fluorophores or a fluorophore and a quencher. When subjected to proteolytic cleavage, at least one fluorophore is unquenched and becomes capable of producing a fluorescent signal upon excitation with light of an appropriate wavelength. Also provided are in vivo and in vitro imaging methods using such imaging agents.

Tetrapeptide compound and method for producing same

The present invention is to provide a method for the efficient production on an industrial scale of SS-31 (D-Arg-Dmt-Lys-Phe-NH.sub.2), which is an SS peptide. According to the present invention, the desired SS-31 is produced by efficiently synthesizing a tetrapeptide compound as a precursor of SS-31 and improving the tetrapeptide purity by crystallization.

Thienopyranones as kinase inhibitors

The invention relates to compounds of formula I (or pharmaceutically acceptable salts thereof) as defined herein, pharmaceutical compositions thereof, and their use in manufactures and methods for modulating biological processes including inhibition of kinase activity such as PI-3 kinase.

Compositions and Methods for the Intracellular Disruption of VEGF and VEGFR-2 by Intraceptors

The present invention provides an intraceptor that interacts with and decreases activity of with VEGF and/or a VEGFR for the treatment of angiogenesis-related conditions. The present invention further provides pharmaceutical compositions, and methods of use thereof for the treatment and prevention of an angiogenesis-related condition using said intraceptors. The invention further provides for nucleic acids encoding said intraceptors.

PROCESS FOR PREPARING COMPOUNDS HAVING TRIPLE ACTIVITIES OF THROMBOLYSIS, ANTITHROMBOTIC AND RADICAL SCAVENGING
20180134748 · 2018-05-17 ·

The present invention relates to a compound simultaneously having triple activities of thrombolysis, antithrombosis and free radical scavenging, as well as the preparation method, composition, and applications thereof. The compound is represented by the formula I shown below:

##STR00001##

wherein the definitions of T, Q, R.sub.1 and R.sub.2 are described herein. The compound of the present invention simultaneously has triple functions of thrombolysis, free radical scavenging and thrombus-targeting/antithrombosis. The present invention also relates to a pharmaceutical composition comprising the compound, and a preparation method and a nanostructure of the compound.

Tetrapeptide having effect of inhibiting VEGF-induced angiogenesis and use thereof

Provided are a tetrapeptide for inhibiting VEGF-induced angiogenesis and a use thereof, and particularly, provided is a peptide having the amino acid sequence of R-X1-X2-E (wherein X1 is leucine (L), isoleucine (I) or valine (V), and X2 is tyrosine (Y) or phenylalanine (F)) for inhibiting angiogenesis, or preventing, improving or treating cancer. This research was supported by grants from the National Research Foundation of Korea (NRF) funded by the Ministry of Science, ICT and Future Planning (MSIP), Republic of Korea, in 2011 and 2013 [NRF-2011-0028790 and 2013M3A9B6046563]. The tetrapeptide may effectively inhibit VEGF-induced angiogenesis or growth of cancer cells without a risk of side effects, and therefore may be expected to exhibit an excellent anticancer effect.

PSMA-targeted NIR dyes and their uses

The present disclosure relates to prostate specific membrane antigen (PSMA) targeted compounds conjugated to near-infra red (NIR) dyes and methods for their therapeutic and diagnostic use. More specifically, this disclosure provides compounds and methods for diagnosing and treating diseases associated with cells and/or vasculature expressing prostate specific membrane antigen (PSMA), such as prostate cancer and related diseases. The disclosure further describes methods and compositions for making and using the compounds, methods incorporating the compounds, and kits incorporating the compounds.

Peptide Treatment for Inflammation and Fibrosis
20180125919 · 2018-05-10 ·

The invention is directed to peptides which inhibit phosphorylation of an amino phosphoacceptor domain of C/EBP? and their use for treating inflammation and fibrosis.

COMPOSITIONS AND METHODS FOR IDENTIFYING ZIKA ENZYME INHIBITORS
20180127800 · 2018-05-10 ·

In alternative embodiments, provided are compositions, e.g., multiplexed platforms or systems, to screen for small molecule drugs that inhibit enzymes such as proteases, e.g., viral proteases, including Zika Virus (ZIKV). In one embodiment, provided are cell-based or multiplexed platforms for monitoring the activity of enzymes, e.g., proteases such as Zika Virus (ZIKV) viral proteases. In alternative embodiments, provided are assays that monitor the activity of the viral ZIKV NS3 protease, as observed by the cleavage of its boundaries with its cofactor NS2B and its downstream nonstructural protein NS4A.