A61K49/0056

INTRA-OPERATIVE IMAGING

The present invention relates to the use of a NIR fluorescent probe comprising an aza-bicycloalkane based cyclic peptide labelled with a Cy5.5 dye moiety in the fluorescence- guided surgery of pathologic regions and to an optical imaging method that comprises using this fluorescent probe for the identification and demarcation of tumor margins during the surgical resection.

PSMA binding ligand-linker conjugates and methods for using

Described herein are prostate specific membrane antigen (PSMA) binding conjugates that are useful for delivering therapeutic, diagnostic and imaging agents. Also described herein are pharmaceutical composition containing them and methods of using the conjugates and compositions. Also described are processes for manufacture of the conjugates and the compositions containing them.

PEPTIDE NUCLEIC ACID CONJUGATES
20230174585 · 2023-06-08 ·

The present disclosure is directed to conjugates of a specific binding entity and an oligomer, i.e. [Specific Binding Entity]-[Oligomer].sub.n, wherein n is an integer ranging from 1 to 12, and where the Oligomer includes, in some embodiments, a PNA sequence having at least one substituent at a gamma carbon position. In some embodiments, the substituent at the gamma carbon position, e.g. an amino acid, a peptide, a miniPEG, or a polymer, includes at least one reporter moiety.

MELANOCORTIN 1 RECEPTOR LIGANDS AND METHODS OF USE

The subject invention pertains to a modified MC1R peptide ligand comprising a peptide that is a melanocortin 1 receptor (MC1R) ligand and a functionality or linker, such as a click functionality, for conjugation to a surface or agent. The modified MC1R peptide ligand can be coupled, e.g., via a click reaction with a complementary click functionality attached, to a moiety to form an MC1R-targeted agent. Drugs, contrast agents, polymers, particles, micelles, surfaces of larger structures, or other moieties can be targeted to the MC1R. The subject invention also pertains to a MC1R peptide ligand-micelle complex comprising a peptide that is a melanocortin 1 receptor ligand connected via a click reaction product to a micelle. The micelle is stable in vivo and can target melanoma tumor cells by association of the peptide ligand with the MC1R or the tumor and selectively provide a detectable and/or therapeutic agent (such as an imageable contrast agent and/or anti-cancer agent) selectively to the tumor cell.

PEPTIDES FOR TARGETING COLORECTAL CANCER, AND MEDICAL USE THEREOF

Provided is a peptide for targeting colorectal cancer, a composition for diagnosing radioresponsiveness-dependent prognosis of colorectal cancer using the peptide, and a drug delivery use of the peptide, wherein a functional peptide capable of targeting cancer has been discovered so as to implement personalized diagnosis and treatment for individual patients having cancer, in consideration of problems occurring during treatment in which treatment cases of respective patients differ due to different therapeutic responses resulting from genetic differences in the individual patients.

Synthetic somatostatin receptor ligands

Disclosed are Somatostatin receptor ligands comprising a peptide moiety, pharmaceutical compositions and uses thereof. Disclosed are also synthetic Somatostatin receptor ligands comprising a cyclic peptide moiety and an active agent moiety covalently bonded to the cyclic peptide moiety through a nitrogen atom of a side chain functional group of an internal residue of the cyclic peptide moiety, pharmaceutical compositions and uses thereof. Disclosed are also synthetic Somatostatin receptor ligands comprising a cyclic peptide moiety and a nanoparticle active agent moiety covalently bonded to the cyclic peptide moiety, pharmaceutical compositions and uses thereof.

Transdermal peptide with nuclear localization ability and use thereof

A transdermal peptide with a nuclear localization ability and having an amino acid sequence as shown in SEQ ID NO: 1 is disclosed. A fusion protein including a macromolecular protein with one end being linked to the transdermal peptide is also disclosed. The transdermal peptide can be used in the preparation of a medicament or a transdermal preparation for treating skin diseases. A medicament for treating a skin disease includes the transdermal peptide and a pharmaceutically acceptable excipient. The transdermal peptide enters the cells autonomously to locate in the nuclei, and can penetrate through the stratum corneum of the skin into cells in the dermis. The peptide is conveniently synthesized artificially and suitable for transdermal administration, and has a therapeutic potential via transdermal administration by carrying a drug for treating skin diseases.

PSMA-targeted NIR dyes and their uses
11484607 · 2022-11-01 · ·

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.

ANGIOPEP AND DERIVATIVES THEREOF FOR IMAGING AMYLOIDS

The present application relates to the molecular labeling and in vivo imaging of amyloids. Specifically, the present application relates to a polypeptide-based method/vector for targeting amyloids. Such a method/vector enables the transportation of compounds or drugs across blood-brain-barrier of an individual and then binding to amyloids in brain. Particularly, the vector of the present application can transport an imaging group linked to the vector across the blood-brain-barrier, and can binds to amyloids in brain, and thus enables the labeling and imaging of amyloid deposits. When used as an imaging agent for detecting amyloid deposits in body or tissues, the vector may be labeled with suitable optical imaging groups, radioactive isotopes or imaging groups suitable for MRI or CT detection. The method/vector can especially used for the in vivo non-invasive diagnosis of amyloid-related diseases including Alzheimer's disease, and for the observation of the therapeutic effect of drugs targeting amyloid deposits.

UPAR TARGETING PEPTIDE FOR USE IN PEROPERATIVE OPTICAL IMAGING OF INVASIVE CANCER
20170304468 · 2017-10-26 ·

There is provided a novel conjugate that binds to the cell surface receptor uPA (uPAR). The conjugate is based on a fluorescence-labeled peptide useful as a diagnostic probe to the surfaces of cells expressing uPAR. The conjugate is capable of carrying a suitable detectable and imageable label that will allow qualitative detection and also quantitation of uPAR levels in vitro and in vivo. This renders the surgical resection of tumors more optimal.