[HTML][HTML] Therapeutic peptides: Historical perspectives, current development trends, and future directions

JL Lau, MK Dunn - Bioorganic & medicinal chemistry, 2018 - Elsevier
Peptide therapeutics have played a notable role in medical practice since the advent of
insulin therapy in the 1920s. Over 60 peptide drugs are approved in the United States and …

The corticotropin-releasing factor family: physiology of the stress response

JM Deussing, A Chen - Physiological reviews, 2018 - journals.physiology.org
The physiological stress response is responsible for the maintenance of homeostasis in the
presence of real or perceived challenges. In this function, the brain activates adaptive …

Structural insights into multiplexed pharmacological actions of tirzepatide and peptide 20 at the GIP, GLP-1 or glucagon receptors

F Zhao, Q Zhou, Z Cong, K Hang, X Zou… - Nature …, 2022 - nature.com
Glucose homeostasis, regulated by glucose-dependent insulinotropic polypeptide (GIP),
glucagon-like peptide-1 (GLP-1) and glucagon (GCG) is critical to human health. Several …

Conserved class B GPCR activation by a biased intracellular agonist

LH Zhao, Q He, Q Yuan, Y Gu, X He, H Shan, J Li… - Nature, 2023 - nature.com
Class B G-protein-coupled receptors (GPCRs), including glucagon-like peptide 1 receptor
(GLP1R) and parathyroid hormone 1 receptor (PTH1R), are important drug targets …

Structural insights into differences in G protein activation by family A and family B GPCRs

D Hilger, KK Kumar, H Hu, MF Pedersen, ES O'Brien… - Science, 2020 - science.org
INTRODUCTION Transmembrane signaling of heterotrimeric guanine nucleotide–binding
protein (G protein)–coupled receptors (GPCRs) is mediated by ligand-dependent …

Glucagon-like peptide-1 and its class BG protein–coupled receptors: a long march to therapeutic successes

C De Graaf, D Donnelly, D Wootten, J Lau… - Pharmacological …, 2016 - ASPET
The glucagon-like peptide (GLP)-1 receptor (GLP-1R) is a class BG protein–coupled
receptor (GPCR) that mediates the action of GLP-1, a peptide hormone secreted from three …

Generic GPCR residue numbers–aligning topology maps while minding the gaps

V Isberg, C De Graaf, A Bortolato, V Cherezov… - Trends in …, 2015 - cell.com
Generic residue numbers facilitate comparisons of, for example, mutational effects, ligand
interactions, and structural motifs. The numbering scheme by Ballesteros and Weinstein for …

History and review of anti‐calcitonin gene‐related peptide (CGRP) therapies: From translational research to treatment

SJ Tepper - Headache: The Journal of Head and Face Pain, 2018 - Wiley Online Library
Objective–To briefly describe the history of and available data on anti‐calcitonin gene‐
related peptide (CGRP) therapies for headache. Background–CGRP was proposed as a …

Human GLP-1 receptor transmembrane domain structure in complex with allosteric modulators

G Song, D Yang, Y Wang, C De Graaf, Q Zhou, S Jiang… - Nature, 2017 - nature.com
The glucagon-like peptide-1 receptor (GLP-1R) and the glucagon receptor (GCGR) are
members of the secretin-like class B family of G-protein-coupled receptors (GPCRs) and …

GPCR signaling and trafficking: the long and short of it

NJ Pavlos, PA Friedman - Trends in Endocrinology & Metabolism, 2017 - cell.com
Emerging findings disclose unexpected components of G protein-coupled receptor (GPCR)
signaling and cell biology. Select GPCRs exhibit classical signaling, that is restricted to cell …