13 results about "Peptide mimetic" patented technology

The present invention provides synthetic peptide compounds and uses thereof for therapy and diagnostics of complement-mediated diseases, such as inflammatory diseases, autoimmune diseases, and microbial and bacterial infections; and non-complement-mediated diseases, such cystic fibrosis and various acute diseases. The invention is directed to modifications of a synthetic peptide of 15 amino acids from the Polar Assortant (PA) peptide, which is a scrambled peptide derived from human Astrovirus protein. In some embodiments, the invention is directed to peptide compounds that are peptide mimetics, peptide analogs and / or synthetic derivatives of PA (e.g., sarcosine derivatives) having, for example, internal peptide substitutions, and modifications, including PEGylation at the N-terminus and C-terminus. The invention further provides methods of selecting at least one synthetic peptide for treating various conditions.

The present invention provides peptide compounds that regulate the complement system and methods of using these compounds. The invention is an isolated, purified peptide of 30 amino acids derived from human astrovirus protein, called CP1. The invention is directed to peptide compounds that are peptide mimetics, peptide analogs and / or synthetic derivatives of CP1 having, for example, internal peptide deletions and substitutions, deletions and substitutions at the N-terminus and C-terminus, and that are able to regulate complement activation. The invention further provides pharmaceutical compositions of therapeutically effective amounts of the peptide compounds and a pharmaceutically acceptable carrier, diluent, or excipient for treating a disease or condition associated with complement-mediated tissue damage.

The present invention relates to Mitochondrial Fission Factor (MFF)-derived peptides or peptide mimetics and to methods of making MFF-derived peptides or peptide mimetics. Also provided are methods of treating a disease in a subject in need thereof, comprising administering to the subject an effective amount of a MFF-derived peptide or peptide mimetic.

EphA2 targeting agents developed herein are potent peptide-mimetics with high affinity (Kds 8-20 nanomolar) for the ligand binding domain, called targefrin. Monomeric versions of targefrin act as antagonists while dimeric versions (targefrin-dimer) of the agent cause receptor internalization and degradation via a lysosomal pathway. Hence, targefrin-dimer agents are effective in reducing pro-oncogenic EphA2 levels in cancer cells when used as single agents or in combination with standards of care. Targefrin-dimers can also sensitive cancer cells that developed resistance to EGER or BRAE inhibitors, and potentially other anti-cancer agents. In addition, the dimeric agents can be conjugated with chemotherapy such as paclitaxel to deliver selectively cytotoxic agent to EphA2 expressing cancer cells. Monomeric agents can be linked to chemotherapy via a stable cleavable linker, accumulate the cytotoxic at the tumor, that then would enter the tumor. Novel composition and examples of these applications are reported.

The invention discloses a polypeptide ligand targeting fibroblast activating protein and application of the polypeptide ligand. Part of the structure in the cyclopeptide skeleton of the ligand is a peptide mimetic skeleton structure aiming at an FAP target, the specific binding force with the FAP is stronger, the ligand has stronger FAP targeting, higher tumor specificity and faster kidney clearance rate, and the retention time at a tumor part is longer, so that the ligand has an obvious inhibiting effect on the FAP and can be used as or used for preparing an FAP inhibitor; the compound can be connected with one of a fluorophore, a radionuclide for diagnosis, a chelating group containing the radionuclide for diagnosis and the like to serve as or be used for preparing a developing agent for developing tumors, inflammatory sites, infected sites and the like. The polypeptide can be connected with one of therapeutic radionuclide, a chelating group containing the therapeutic radionuclide, a cytotoxin group, other functional groups and the like to serve as or be used for preparing targeted polypeptide coupling drugs for treating diseases such as tumors, inflammations, infection and the like; the effect is good, the safety is high and the application is wide.

The application discloses a kind of fat cationic amphiphilic peptide mimics and its preparation method and application.The application first develops a kind of cysteine-based amphiphilic cationic peptide mimic system, then, by forming peptide bond at carboxyl terminal, introduce ethylenediamine as cationic group, while introducing aromatic ring-containing hydrophobic group in thiol side chain;Among them, cationic group provides positive charge and hydrophilicity, helps to carry out electrostatic interaction with the bacterial membrane with negative charge, while hydrophobic group helps membrane insertion phospholipid bilayer;In addition, the application tunes the amphiphilic balance of cysteine-based cationic peptide mimic by modifying N-terminal with different chain length fatty acids, and finally synthesizes fat cationic amphiphilic peptide mimic.The peptide mimic has good antibacterial activity, and is not easy to induce bacteria to produce drug resistance, and can be used for preparing drugs for treating, improving and / or preventing drug-resistant bacteria and / or drug-resistant fungal infection.

Described herein are synthetic cyclic peptide mimetics comprising alternating D-amino acids and L-amino acids and amino acid derivatives, such as aza-amino acids and azasulfuryl-amino acids. Optionally, the cyclic peptide mimetics may be conjugated to another agent via a linker to form cyclic peptide mimetic conjugates. The cyclic peptide mimetics described herein may be used as diagnostic or therapeutic agents for diagnosis or treatment of amyloidogenic diseases.

The invention discloses a peptide simulant and a preparation method thereof, 3-oxetanone and 3-methyl-1-nitrobutane are used as raw materials, and all reactions are carried out to obtain a target product. The peptide simulant is novel in structure and has potential biological activity, adopted protecting groups and functional groups are good in compatibility, and follow-up structural modification is facilitated; the designed synthesis route is simple, the reaction condition is mild, and amplification is easy; the yield of each step is high, and the product is easy to purify.

The invention relates to chemical compounds useful as structural mimetics of peptides comprising polyproline helix structures, preferably polyproline-type II (PPII) helix structures. The invention further relates to the medical use of the chemical compounds in the treatment of a medical condition associated with a modified intracellular signal transduction process mediated by a poly-proline helix structure and a protein having a binding domain binding to said polyproline helix structure such as an infectious disease, immune disease, neurological disease, cardiometabolic disease and a cancerous disease. The invention further relates to pharmaceutical compositions comprising a compound of the present invention or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier. The invention further relates to an in vitro method for modifying an intracellular signal transduction process mediated by a poly-proline helix structure, comprising contacting a compound of the invention with a biological cell.

The present invention relates to an injectable delivery system for long-acting administration of drugs. The present invention includes compounds formed at least in part from peptidomimetic molecules. The compound is configured to link one or more drug molecules, and is further configured to release the one or more drug molecules under physiological conditions. A solution of the compound forms a hydrogel in response to an endogenous enzyme of a human or animal. A solution of the compound can be applied to the skin where it forms a hydrogel upon application, and any drug attached to the compound will then be gradually released.

This disclosure provides engineered polypeptides with Atg8 binding activity. The polypeptides comprise a LC-3 interacting motif comprising one or more mutations relative to a wild type LC3 -interacting motif. Also provided are heterobifunctional compounds, compositions comprising the compounds or engineered polypeptides, and methods of using the compounds or engineered polypeptides.

The invention provides an indole antibacterial peptide simulant with antibacterial activity and a preparation method and application thereof, and relates to the technical field of medicinal chemistry, the chemical structural formula of the indole antibacterial peptide simulant is shown as the following (I), and n and R in the formula are defined as the specification; in-vitro antibacterial activity experiments prove that the indole antibacterial peptide simulant disclosed by the invention has relatively good antibacterial activity on gram-positive bacteria such as staphylococcus aureus, bacillus subtilis and enterococcus faecalis, and has the characteristics of low cytotoxicity, low hemolysis and difficulty in generating drug resistance; the compound can be applied to preparation of drugs for resisting bacteria or treating bacterial infection. (I)

The invention belongs to the technical field of antibacterial peptides, and provides an antibacterial peptide simulant based on a cinnamic acid skeleton as well as a preparation method and application of the antibacterial peptide simulant. The antibacterial peptide simulant based on the cinnamic acid skeleton comprises an ammonium salt antibacterial peptide simulant and / or a guanidine salt antibacterial peptide simulant, and is prepared by the following steps: taking 4-bromomethyl biphenyl as a raw material, and performing bromination reaction to obtain an intermediate 1; then the intermediate 1 and (2E)-3-phenyl-2-acrylic acid are subjected to an amide condensation reaction and a Boc removal protection reaction to obtain an ammonium salt antibacterial peptide simulant, and then the guanidinium antibacterial peptide simulant is obtained through a guanidinylation reaction and a Boc removal protection reaction. The antibacterial peptide simulant based on the cinnamic acid skeleton has excellent antibacterial activity, and also has the characteristics of strong stability, low toxicity, simple structure, rapid sterilization and difficult generation of drug resistance, and the clinical application of the antibacterial peptide simulant is greatly promoted.