Design, Synthesis, and SAR of Potent and Selective Dipeptide-Derived Inhibitors for Dipeptidyl Peptidases
摘要:
In this paper we report the systematic search for new, potent, and selective DPP II inhibitors. A study of the structure-activity relationship was conducted starting from aminoacyl pyrrolidides as lead compounds. Rational exploration of the P-1 and P-2 building blocks led to the discovery of some very potent DPP II inhibitors which can be characterized by their high selectivity for DPP II with regard to DPP IV. Dab-Pip and Dab-Pip-2-CN were selected as the most promising inhibitors (IC50 nM range) and will enable us to study the physiological role of DPP II and to differentiate between DPP 11 and DPP IV in biological systems.
TETRAZINES/TRANS-CYCLOOCTENES IN SOLID PHASE SYNTHESIS OF LABELED PEPTIDES
申请人:MEMORIAL SLOAN-KETTERING CANCER CENTER
公开号:US20150359913A1
公开(公告)日:2015-12-17
This invention is in the field of labeled peptide construction for medical treatment and analysis. The invention relates to synthetic labeled peptide compositions, methods of synthesis, and methods of use for the synthetic labeled peptide compositions for medical treatment, imaging, and research purposes.
Vicinal Disulfide Constrained Cyclic Peptidomimetics: a Turn Mimetic Scaffold Targeting the Norepinephrine Transporter
作者:Andreas Brust、Ching-I. A. Wang、Norelle L. Daly、Joe Kennerly、Mahsa Sadeghi、Macdonald J. Christie、Richard J. Lewis、Mehdi Mobli、Paul F. Alewood
DOI:10.1002/anie.201304660
日期:2013.11.11
Loopy peptides: Peptide turnmimetics of a clinically relevant norepinephrine reuptake inhibitor were developed employing a high‐throughput synthesis approach to generate peptide thioesters, with subsequent cyclization through native chemical ligation. The vicinaldisulfideconstrainedcyclicpeptidomimetics (see scheme) show high structural and functional similarity to the parent peptide, though with
[EN] DIPEPTIDYL PEPTIDASE INHIBITORS<br/>[FR] INHIBITEURS DE DIPEPTIDYLE PEPTIDASE
申请人:AIC
公开号:WO2004076433A1
公开(公告)日:2004-09-10
The present invention relates to novel inhibitors of serine type peptidases in general and of serine type dipeptidyl peptidases in particular. The present invention further relates to the use of the dipeptidyl peptidase inhibitors for selective inhibition of dipeptidyl peptidases. The present invention also relates to pharmaceutical compositions comprising these novel dipeptidyl peptidase inhibitors. The present invention further relates to the use of the novel inhibitors in therapy, diagnosis and research.
The present invention relates to polypeptide compound optimized for subcutaneous administration, exemplified by growth hormone conjugates having a linker providing non-covalent binding to albumin.