C07K5/11

Macrocyclic broad spectrum antibiotics

Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidase (SpsB), an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.

MULTIFUNCTIONAL POLYPEPTIDE AND APPLICATION THEREOF IN FIELD OF MEDICINES
20240158442 · 2024-05-16 · ·

Provided is a multifunctional polypeptide, consisting of one or more of at least one Pro-Ala-Lys, Ala-Lys-Pro, Lys-Ala-Pro and a fragment thereof and a derived peptide, there being carnosine, anserine or ophidine at the C-terminus and/or N-terminus of the polypeptide. The polypeptide is formed by linking an oligopeptide having a thrombolysis function and carnosine composed of histidine, 1-methylhistidine and 3-methylhistidine, anserine or ophidine, etc., easily crosses the blood-brain barrier, and is administered by intravenous route for the treatment of nervous system diseases, especially brain damage and stroke.

METHODS FOR REDUCING CD36 EXPRESSION
20190248833 · 2019-08-15 ·

The invention provides a method for treating one or more complications of diabetes in a mammal. The method comprises administering to a mammal in need thereof an effective amount of an aromatic-cationic peptide having at least one net positive charge; a minimum of four amino acids; a maximum of about twenty amino acids; a relationship between the minimum number of net positive charges (p.sub.m) and the total number of amino acid residues (r) wherein 3 p.sub.m is the largest number that is less than or equal to r+1; and a relationship between the minimum number of aromatic groups (a) and the total number of net positive charges (p.sub.t) wherein 2a is the largest number that is less than or equal to p.sub.t+1, except that when a is 1, p.sub.t may also be 1.

COMPOUND, PROCESS FOR ITS PREPARATION, A PHARMACEUTICAL SOLUTION CONTAINING THE COMPOUND, A METHOD OF DETERMINING THE PRESENCE OF CANCER, A KIT FOR CANCER DETECTION, AND THE USE OF HYDROLYSIS OF THE COMPOUND FOR THE DETECTION OF CANCER

The subject of the invention is a new compound of the following chemical formula:


ABZ.sup.1-Dap(O2(Cbz)).sup.2-Dap(O1).sup.3-Dap(O2).sup.4-Arg.sup.5-ANB.sup.6-NH.sub.2 where: ABZ stands for 2-aminobenzoic acid; DAP stands for diaminopropanoic acid (Dap) derivatives, modified by the functionalised residues of mono-ethylene or diethylene glycol (PEG); ANB stands for 5-amino-2-nitrobenzoic acid

The subject of the invention is a method for producing the new compound and a pharmaceutical solution for cancer detection, which contains the above-mentioned compound.

The subject of the invention is a method for cancer detection through the in vitro analysis of a human urine sample to which a new compound is added and blended with a buffer of pH 7-9.

The subject of the invention is also a kit for detecting cancer, in particular bladder cancer, and the use of hydrolysis of the new compound in the position no. 5 by proteasome 20s for cancer detection, in particular bladder cancer.

Recombinant polypeptide production methods

Herein is reported a method for producing a fusion-polypeptide comprising the steps of a) cultivating a mammalian cell comprising a nucleic acid encoding a variant fusion-polypeptide wherein the amino acid sequence of the fusion-polypeptide has been modified by replacing in a pro-fusion-polypeptide the endogenous protease cleavage site between the pro-peptide and the fusion-polypeptide with an exogenous (with respect to the origins of the parts of the fusion-polypeptide) or artificial protease cleavage site, and b) recovering the fusion-polypeptide or fusion-pro-polypeptide from the cell or the cultivation medium and thereby producing the (recombinant) fusion-polypeptide.

CRYSTALLINE BIS- AND TRIS-HYDROCHLORIDE SALT OF ELAMIPRETIDE
20190233474 · 2019-08-01 ·

Disclosed are crystalline forms of the bis- and tris-(hydrochloride) salts of D-Arg-Tyr(2,6-DiMe)-Lys-Phe-NH.sub.2, which is also known as MTP-131.

PROTEIN INTERFACES
20190216879 · 2019-07-18 ·

The present disclosure provides methods to treat conditions, including cancer, using compounds that can target resistant cancer cells. The compounds can be used to sensitize resistant cancer cells or decrease the proliferation of cells. The compounds can target proteins in the DNA damage repair pathway leading to a decrease in DNA damage repair in target cells.

Process for preparing compounds having triple activities of thrombolysis, antithrombosis, and radical scavenging

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.

N-CARBOXYANHYDRIDE-BASED-SCALE SYNTHESIS OF ELAMIPRETIDE
20190202861 · 2019-07-04 ·

Disclosed are methods of making elamipretide (MTP-131), a peptide compound with therapeutic potential for treating various mitochondrial myopathies. The synthesis of the peptide can be achieved via the use of N-carboxyanhydride-modified amino acid residues, which increases the efficiency of the synthetic process and the purity of the peptide product generated.

Peptidomimetics with antiangiogenic activity

We disclose novel peptidomimetics with antiangiogenic activity and their uses, particularly in the treatment of neoplasms and chronic inflammation (in particular of: rheumatoid arthritis, colitis), in eczema, diabetes, age-related macular degeneration (ARMD), nephropathy and neuropathy, in particular for use in the form of intravenous infusions or injections, or implants releasing the active ingredient.