Macrocyclization strategies for cyclic peptides and peptidomimetics

C Bechtler, C Lamers - RSC Medicinal Chemistry, 2021 - pubs.rsc.org
Peptides are a growing therapeutic class due to their unique spatial characteristics that can
target traditionally “undruggable” protein–protein interactions and surfaces. Despite their …

Therapeutic uses of somatostatin and its analogues: current view and potential applications

U Rai, TR Thrimawithana, C Valery… - Pharmacology & …, 2015 - Elsevier
Somatostatin is an endogeneous cyclic tetradecapeptide hormone that exerts multiple
biological activities via five ubiquitously distributed receptor subtypes. Classified as a broad …

Structural insights into the activation of somatostatin receptor 2 by cyclic SST analogues

Q Bo, F Yang, Y Li, X Meng, H Zhang, Y Zhou, S Ling… - Cell Discovery, 2022 - nature.com
The endogenous cyclic tetradecapeptide SST14 was reported to stimulate all five
somatostatin receptors (SSTR1–5) for hormone release, neurotransmission, cell growth …

Structural insights into ligand recognition and selectivity of somatostatin receptors

W Zhao, S Han, N Qiu, W Feng, M Lu, W Zhang… - Cell Research, 2022 - nature.com
Somatostatin receptors (SSTRs) play versatile roles in inhibiting the secretion of multiple
hormones such as growth hormone and thyroid-stimulating hormone, and thus are …

Structure-based design of a Cortistatin analogue with immunomodulatory activity in models of inflammatory bowel disease

Á Rol, T Todorovski, P Martin-Malpartida… - Nature …, 2021 - nature.com
Ulcerative colitis and Crohn's disease are forms of inflammatory bowel disease whose
incidence and prevalence are increasing worldwide. These diseases lead to chronic …

Disulfide bond mimetics: strategies and challenges

A Gori, P Gagni, S Rinaldi - Chemistry–A European Journal, 2017 - Wiley Online Library
The activity profile of many biologically relevant proteins and peptides often relies on a
precise 3D structural organization. In this context, disulfide bonds are natural covalent …

Somatostatin and its analogs

L Sun, DH Coy - Current drug targets, 2016 - ingentaconnect.com
Somatostatin (SST) is a cyclic hormone-release inhibitory peptide that has high binding
affinity to all of its five SST receptors (SSTRs). SST negatively regulates cell proliferation and …

Ring-closing metathesis in peptides

EC Gleeson, WR Jackson, AJ Robinson - Tetrahedron Letters, 2016 - Elsevier
This review highlights developments in the field of ring-closing metathesis applied to the
synthesis of cyclic peptides. Special attention is focussed on the synthesis of dicarba …

Computational screening and selection of cyclic peptide hairpin mimetics by molecular simulation and kinetic network models

AM Razavi, WM Wuest, VA Voelz - Journal of chemical information …, 2014 - ACS Publications
Designing peptidomimetic compounds to have a preorganized structure in solution is highly
nontrivial. To show how simulation-based approaches can help speed this process, we …

Microwave-assisted syntheses of bioactive seven-membered, macro-sized heterocycles and their fused derivatives

M Driowya, A Saber, H Marzag, L Demange, K Bougrin… - Molecules, 2016 - mdpi.com
This review describes the recent advances in the microwave-assisted synthesis of 7-
membered and larger heterocyclic compounds. Several types of reaction for the cyclization …