The invention relates to peptide dimer compounds and peptide monomer compounds that potently inhibit binding of α4β7 to the mucosal addressin cell adhesion molecule (MAdCAM) in vivo, possess high selectivity against α4β1 binding, and have high stability under gastrointestinal conditions.
Oral peptide inhibitors of interleukin-23 receptor and their use to treat inflammatory bowel diseases
申请人:Protagonist Therapeutics, Inc.
公开号:US10023614B2
公开(公告)日:2018-07-17
Peptide inhibitors of the interleukin-23 receptor, and related compositions and methods of using these peptide inhibitors to treat or prevent a variety of diseases and disorders, including inflammatory bowel disease, are disclosed.
The invention relates to thioether monomer and dimer peptide molecules which inhibit binding of α4β7 to the mucosal addressing cell adhesion molecule (MAdCAM) in vivo.
Cyclic monomer and dimer peptides having integrin antagonist activity
申请人:Protagonist Therapeutics, Inc.
公开号:US10301371B2
公开(公告)日:2019-05-28
The invention relates to C to N cyclized (C-N cyclic) monomer and dimer peptide molecules, as well as peptide dimers which are connected by linker moieties at the N terminus and the C terminus of each peptide subunit, which inhibit binding of α4β7 to the mucosal addressin cell adhesion molecule (MAdCAM) in vivo, and show high selectivity against α4β1 binding.
本发明涉及 C-N 环化(C-N cyclic)单体和二聚体肽分子,以及在每个肽亚基的 N 端和 C 端通过连接分子连接的肽二聚体,它们在体内可抑制 α4β7 与粘膜地址素细胞粘附分子(MAdCAM)的结合,并对α4β1 的结合具有高度选择性。
Methods for synthesizing α4β7 peptide antagonists
申请人:Protagonist Therapeutics, Inc.
公开号:US10407468B2
公开(公告)日:2019-09-10
The present invention provides methods of making α4β7 peptide monomer and dimer antagonists. Methods of the present invention include solid phase and solution phase methods, as well as synthesis via condensation of smaller peptide fragments. Methods of the present invention further include methods directed to the synthesis of peptides comprising one or more penicillamine residues.