Protein epitope mimetic macrocycles as biopharmaceuticals.
نویسندگان
چکیده
Fully synthetic medium-sized macrocyclic peptides mimicking the key β-hairpin and α-helical protein epitopes relevant in many protein-protein interactions have emerged as a novel class of drugs with the potential to fill an important gap between small molecules and proteins. Conformationally stabilized macrocyclic scaffolds represent ideal templates for medicinal chemists to incorporate bioactive peptide and protein pharmacophores in order to generate novel drugs to treat diseases with high unmet medical need. This review describes recent approaches to design and generate large libraries of such macrocycles, for hit identification, and for their efficient optimization. Finally, this review describes some of the most advanced protein epitope mimetic (PEM) macrocycles in clinical development.
منابع مشابه
A Novel Multi-Epitope Vaccine For Cross Protection Against Hepatitis C Virus (HCV): An Immunoinformatics Approach
Background: Hepatitis C virus (HCV) causes acute and chronic human hepatitis infections. Due to the high genetic diversity and high rates of mutations in the genetic material so far there is no approved vaccine against HCV. Materials and Methods: The aim of this study was to determination B and T cell conserved epitopes of E1 and E2 proteins from HCV and construction of a chimeric pepti...
متن کاملطراحی، ساخت و بیان اپیتوپهای پروتئین VP1 ویروس تب برفکی سروتیپO ایران
Foot-and-mouth disease (FMD) is an extremely infectious and occasionally fatal viral disease with a rapid onset and a short course that affects cloven-hoofed animals and results in considerable financial losses. For this reason, availability of more reliable and efficient vaccines against Foot-and-mouth disease virus (FMDV) is felt as a necessity. The purpose of this study is to develop a ...
متن کاملProtective effect of a Protein Epitope Mimetic CCR10 antagonist, POL7085, in a model of allergic eosinophilic airway inflammation
BACKGROUND Potential involvement of the CCR10/CCL28 axis was recently reported in murine models of allergic asthma. If confirmed, blockade of the CCR10 receptor would represent an alternative to current asthma therapies. We evaluated the effect of a novel Protein Epitope Mimetic CCR10 antagonist, POL7085, in a murine model of allergic eosinophilic airway inflammation. METHODS Mice were sensit...
متن کاملExpression of G1- epitope of bovine ephemeral fever virus in E. coli : A novel candidate to develop ELISA kit
Bovine ephemeral fever is an acute and arthropod-borne viral disease of cattle and water buffalo which occurs seasonally in most of the world tropical and subtropical regions. The epizootic feature of the disease has been reported in Iran with serious economic consequences. The surface glycoprotein G of bovine ephemeral fever virus (BEFV) is composed of 4 antigenic sites (G1-G4) and plays the m...
متن کاملReceptor Epitope Usage by Interleukin 5 Mimetic Peptide
Tetsuya Ishino, Cecilia Urbina, Madhushree Bhattacharya, Dominick Panarello, and Irwin Chaiken From the Department of Biochemistry and Molecular Biology, and A. J. Drexel Institute of Basic and Applied Protein Science, Drexel University College of Medicine, Philadelphia, PA, 19102 Running Title: Receptor Epitope Usage by Interleukin 5 Mimetic Peptide Address correspondence to: Irwin Chaiken, De...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید
ثبت ناماگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید
ورودعنوان ژورنال:
- Current opinion in chemical biology
دوره 38 شماره
صفحات -
تاریخ انتشار 2017