Versitech, Inc.

The University of Hong Kong

Other

Sunshine Lake Pharma Co., Ltd.

The University of Hong Kong Shenzhen Institute of Research and Innovation

Xuechen Li

Yi Tsun Richard Kao

Ming Liu

Peng Gao

Yingjun Zhang

Qingyun Ren

Huichao Luo

Zhimin Xiong

Hiu Yung Lam

Chi-Lung Lee

Jiaochao Xu

Chun Ling Tung

Clarence Tsun Ting Wong

Hoi Yee Chow

Ali Huang

Xianwu Fu

Jianchao Xu

Chi Lung Lee

Pharmaceuticals, and specifically a Teixobactin analogue and use thereof. A pharmaceutical composition having the compound and use of the compound and the pharmaceutical composition thereof inhibits the growth and/or reproduction of Gram-positive bacteria or. A compound has Formula (Ia) or a stereoisomer, a tautomer, an N-oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof,

Teixobactin analogue and use thereof

Cyclic lipopeptides having one or more modifications relative to daptomycin, and methods of making them are provided. The cyclic lipopeptides can be used as antibacterial agents. The daptomycin analogues are generated by chemical synthesis, which makes introduction of an unnatural amino acid and any modification into daptomycin possible. Pharmaceutical compositions and method of use thereof for the disclosed daptomycin analogues are also provided.

Antibacterial cyclic lipopeptides

Provided herein are compounds, derivatives thereof, and compositions including one or more of the compounds and derivatives, and methods for prevention and/or treatment of microbial infections and/or related diseases or conditions. The present compounds and/or derivatives thereof can be represented by Formula (I): The present methods include administering to a subject an effective amount of one or more compounds of Formula (I). In one embodiment, the microbial infections are bacterial infections. More specifically, the bacterial infections are staphylococcal infections.

Compounds and methods for the treatment of microbial infections

Provided herein are compounds, derivatives thereof, composition comprising one or more of said compounds and derivatives, and methods for prevention and/or treatment of microbial infections and/or related diseases or conditions. The present compounds and/or derivatives thereof can be represented by Formula (II): The present methods include administering to a subject an effective amount of one or more compounds of Formula (II). In one embodiment, said microbial infections are bacterial infections. More specifically, said bacterial infections are staphylococcal infections.

Compounds affecting pigment production and methods for treatment of bacterial diseases

Described are design and generation of a set of novel cyclic lipopeptides as potential antibacterial agents. New daptomycin analogues are generated by chemical synthesis, which makes introduction of an unnatural amino acid and any modification into daptomycin possible.

Provided herein are compounds, derivatives thereof, composition comprising one or more of said compounds and derivatives, and methods for prevention and/or treatment of microbial infections and/or related diseases or conditions. The present compounds and/or derivatives thereof can be represented by Formula (I): The present methods include administering to a subject an effective amount of one or more compounds of Formula (I). In one embodiment, said microbial infections are bacterial infections. More specifically, said bacterial infections are staphylococcal infections.

A method for the synthesis of daptomycin or a daptomycin analog is carried out on a resin to form a linear precursor followed by a serine ligation macrocyclization in solution. Daptomycin analogs can differ from daptomycin by substitution of amino acids residues and/or deletion or addition of amino acid residues. Daptomycin analogs can include a different fatty acid in the side arm of the daptomycin analog.

Daptomycin analogues and a method for the preparation of daptomycin or a daptomycin analogue

The present disclosure relates to the design and generation of stapled helical peptides that perturb protein-protein interactions (PPIs). The methods disclosed herein for preparing stapled peptides involve providing a peptide having a first amino acid that is functionalized with a salicylaldehyde ester side group and a second amino acid functionalized with a 1,2-hydroxyl amine side group; reacting the first and second amino acids to generate an N,O-benzylidene acetal moiety; and performing acidolysis of the resultant N,O-benzylidene acetal moiety to generate the stapled peptide. In many forms, the stapled helical peptides described herein are not hydrophobic.

Stapled helical peptides and methods of synthesis

Compounds, compositions and methods for the preparation of peptide/protein conjugates, said method comprising a step of reacting a compound (2) represented by the formula (2) with a compound (3) represented by the formula (3) to obtain compound (1) represented by the formula (1), wherein R' represents substituent, and R represents H or at least one substituents. Also disclosed is a kit comprising the compound. 

Compounds, compositions and methods for the preparation of peptide/protein conjugates

A chemoselective chemical ligation method is disclosed. The method joins two peptide segments efficiently to produce a larger peptide or protein, by generating a natural peptide bond (Xaa-Ser and Xaa-Thr) at the ligation site (Xaa represents any 5 amino acid). The method requires two steps (FIG.()): a) reacting the starting peptide(s) to form an acetal intermediate with an acetal group at the ligation site; b) converting said acetal intermediate to a desired peptide or protein with said natural peptide bond.

Growing community of inventors

Hong Kong, China

Xuechen Li