Unnatural helical peptidic foldamers as protein segment mimics

P Sang, J Cai - Chemical Society Reviews, 2023 - pubs.rsc.org
Unnatural helical peptidic foldamers have attracted considerable attention owing to their
unique folding behaviours, diverse artificial protein binding mechanisms, and promising …

PTH/PTHrP receptor signaling, allostery, and structures

I Sutkeviciute, LJ Clark, AD White, TJ Gardella… - Trends in Endocrinology …, 2019 - cell.com
The parathyroid hormone (PTH) type 1 receptor (PTHR) is the canonical G protein-coupled
receptor (GPCR) for PTH and PTH-related protein (PTHrP) and the key regulator of calcium …

[HTML][HTML] Advancing oral delivery of biologics: Machine learning predicts peptide stability in the gastrointestinal tract

F Wang, N Sangfuang, LE McCoubrey, V Yadav… - International Journal of …, 2023 - Elsevier
The oral delivery of peptide therapeutics could facilitate precision treatment of numerous
gastrointestinal (GI) and systemic diseases with simple administration for patients. However …

Improved GPCR ligands from nanobody tethering

RW Cheloha, FA Fischer, AW Woodham… - Nature …, 2020 - nature.com
Antibodies conjugated to bioactive compounds allow targeted delivery of therapeutics to cell
types of choice based on that antibody's specificity. Here we develop a new type of …

Hormone Analogues with Unique Signaling Profiles from Replacement of α-Residue Triads with β/γ Diads

R Gibadullin, TW Kim, LML Tran… - Journal of the American …, 2023 - ACS Publications
We have applied an underexplored backbone modification strategy to generate new
analogues of peptides that activate two clinically important class B1 G protein-coupled …

Use of backbone modification to enlarge the spatiotemporal diversity of parathyroid hormone receptor-1 signaling via biased agonism

S Liu, FG Jean-Alphonse, AD White… - Journal of the …, 2019 - ACS Publications
The type-1 parathyroid hormone receptor (PTHR1), which regulates calcium homeostasis
and tissue development, has two native agonists, parathyroid hormone (PTH) and PTH …

Receptor selectivity from minimal backbone modification of a polypeptide agonist

S Liu, RW Cheloha, T Watanabe… - Proceedings of the …, 2018 - National Acad Sciences
Human parathyroid hormone (PTH) and N-terminal fragments thereof activate two receptors,
hPTHR1 and hPTHR2, which share∼ 51% sequence similarity. A peptide comprising the …

Altered signaling at the PTH receptor via modified agonist contacts with the extracellular domain provides a path to prolonged agonism in vivo

S Liu, Z Yu, EJ Daley, CA Bingman… - Proceedings of the …, 2022 - National Acad Sciences
The parathyroid hormone type 1 receptor (PTHR1), a Class B GPCR, is activated by long
polypeptides, including drugs for osteoporosis and hypoparathyroidism. The PTHR1 …

Ureidopeptide GLP-1 analogues with prolonged activity in vivo via signal bias and altered receptor trafficking

J Fremaux, C Venin, L Mauran, R Zimmer… - Chemical …, 2019 - pubs.rsc.org
The high demand of the pharmaceutical industry for new modalities to address the
diversification of biological targets with large surfaces of interaction led us to investigate the …

Backbone Modification Provides a Long-Acting Inverse Agonist of Pathogenic, Constitutively Active PTH1R Variants

S Liu, EJ Daley, LML Tran, Z Yu, M Reyes… - Journal of the …, 2024 - ACS Publications
Parathyroid hormone 1 receptor (PTH1R) plays a key role in mediating calcium homeostasis
and bone development, and aberrant PTH1R activity underlies several human diseases …