[HTML][HTML] Automated solid-phase peptide synthesis to obtain therapeutic peptides

V Mäde, S Els-Heindl… - Beilstein journal of …, 2014 - beilstein-journals.org
The great versatility and the inherent high affinities of peptides for their respective targets
have led to tremendous progress for therapeutic applications in the last years. In order to …

[HTML][HTML] Pancreatic polypeptide revisited: Potential therapeutic effects in obesity-diabetes

W Zhu, N Tanday, PR Flatt, N Irwin - Peptides, 2023 - Elsevier
Pancreatic polypeptide (PP), a member of the neuropeptide Y (NPY) family of peptides, is a
hormone secreted from the endocrine pancreas with established actions on appetite …

Structural basis of ligand binding modes at the neuropeptide YY1 receptor

Z Yang, S Han, M Keller, A Kaiser, BJ Bender, M Bosse… - Nature, 2018 - nature.com
Neuropeptide Y (NPY) receptors belong to the G-protein-coupled receptor superfamily and
have important roles in food intake, anxiety and cancer biology,. The NPY–Y receptor …

Receptor-specific recognition of NPY peptides revealed by structures of NPY receptors

T Tang, Q Tan, S Han, A Diemar, K Löbner, H Wang… - Science …, 2022 - science.org
In response to three highly conserved neuropeptides, neuropeptide Y (NPY), peptide YY,
and pancreatic polypeptide (PP), four G protein–coupled receptors mediate multiple …

N-Terminus to Arginine Side-Chain Cyclization of Linear Peptidic Neuropeptide YY4 Receptor Ligands Results in Picomolar Binding Constants

A Konieczny, M Conrad, FJ Ertl, J Gleixner… - Journal of Medicinal …, 2021 - ACS Publications
The family of neuropeptide Y (NPY) receptors comprises four subtypes (Y1R, Y2R, Y4R,
Y5R), which are addressed by at least three endogenous peptides, ie, NPY, peptide YY, and …

Structure–Activity Relationship Study of the High-Affinity Neuropeptide Y4 Receptor Positive Allosteric Modulator VU0506013

C Schüß, O Vu, NM Mishra, IR Tough… - Journal of Medicinal …, 2023 - ACS Publications
Positive allosteric modulators targeting the Y4 receptor (Y4R), a G protein-coupled receptor
(GPCR) involved in the regulation of satiety, offer great potential in anti-obesity research. In …

Highly Selective Y4 Receptor Antagonist Binds in an Allosteric Binding Pocket

C Schüß, O Vu, M Schubert, Y Du… - Journal of Medicinal …, 2021 - ACS Publications
Human neuropeptide Y receptors (Y1R, Y2R, Y4R, and Y5R) belong to the superfamily of G
protein-coupled receptors and play an important role in the regulation of food intake and …

Neuropeptide receptors as potential pharmacological targets for obesity

BT Meneguetti, MH Cardoso, CFA Ribeiro… - Pharmacology & …, 2019 - Elsevier
Obesity is a chronic multifactorial disease, characterized by an excessive accumulation of
adipose tissue. It is usually the result of excessive food intake and/or low energy …

Discovery and characterization of VU0529331, a synthetic small-molecule activator of homomeric G protein-gated, inwardly rectifying, potassium (GIRK) channels

KA Kozek, Y Du, S Sharma, FJ Prael III… - ACS chemical …, 2018 - ACS Publications
G protein-gated, inwardly rectifying, potassium (GIRK) channels are important regulators of
cellular excitability throughout the body. GIRK channels are heterotetrameric and …

Oligopeptides as Neuropeptide YY4 Receptor Ligands: Identification of a High-Affinity Tetrapeptide Agonist and a Hexapeptide Antagonist

A Konieczny, D Braun, D Wifling… - Journal of Medicinal …, 2020 - ACS Publications
Within the family of neuropeptide Y (NPY) receptors, the Y4 receptor (Y4R) is unique as it
prefers pancreatic polypeptide over NPY and peptide YY. Today, low-molecular-weight Y4R …