Folding and misfolding of human membrane proteins in health and disease: from single molecules to cellular proteostasis

JT Marinko, H Huang, WD Penn, JA Capra… - Chemical …, 2019 - ACS Publications
Advances over the past 25 years have revealed much about how the structural properties of
membranes and associated proteins are linked to the thermodynamics and kinetics of …

Chaperoning G protein-coupled receptors: from cell biology to therapeutics

YX Tao, PM Conn - Endocrine reviews, 2014 - academic.oup.com
G protein-coupled receptors (GPCRs) are membrane proteins that traverse the plasma
membrane seven times (hence, are also called 7TM receptors). The polytopic structure of …

Pharmacoperones as novel therapeutics for diverse protein conformational diseases

YX Tao, PM Conn - Physiological Reviews, 2018 - journals.physiology.org
After synthesis, proteins are folded into their native conformations aided by molecular
chaperones. Dysfunction in folding caused by genetic mutations in numerous genes causes …

Allosteric regulation of G-protein-coupled receptors: from diversity of molecular mechanisms to multiple allosteric sites and their ligands

AO Shpakov - International Journal of Molecular Sciences, 2023 - mdpi.com
Allosteric regulation is critical for the functioning of G protein-coupled receptors (GPCRs)
and their signaling pathways. Endogenous allosteric regulators of GPCRs are simple ions …

Gonadotropin-inhibitory hormone inhibits GnRH-induced gonadotropin subunit gene transcriptions by inhibiting AC/cAMP/PKA-dependent ERK pathway in LβT2 cells

YL Son, T Ubuka, RP Millar, H Kanasaki… - Endocrinology, 2012 - academic.oup.com
A neuropeptide that directly inhibits gonadotropin secretion from the pituitary was
discovered in quail and named gonadotropin-inhibitory hormone (GnIH). The presence and …

Discovery and development of small molecule allosteric modulators of glycoprotein hormone receptors

SG Nataraja, HN Yu, SS Palmer - Frontiers in endocrinology, 2015 - frontiersin.org
Glycoprotein hormones, follicle-stimulating hormone (FSH), luteinizing hormone (LH), and
thyroid-stimulating hormone (TSH) are heterodimeric proteins with a common α-subunit and …

Pharmacological chaperoning: a primer on mechanism and pharmacology

NJ Leidenheimer, KG Ryder - Pharmacological research, 2014 - Elsevier
Approximately forty percent of diseases are attributable to protein misfolding, including those
for which genetic mutation produces misfolding mutants. Intriguingly, many of these mutants …

Evidence for follicle-stimulating hormone receptor as a functional trimer

X Jiang, D Fischer, X Chen, SD McKenna, H Liu… - Journal of Biological …, 2014 - ASBMB
Follicle-stimulating hormone receptor (FSHR), a G-protein coupled receptor, is an important
drug target in the development of novel therapeutics for reproductive indications. The FSHR …

Gonadotropins and their analogs: current and potential clinical applications

RC Anderson, CL Newton, RA Anderson… - Endocrine …, 2018 - academic.oup.com
The gonadotropin receptors LH receptor and FSH receptor play a central role in governing
reproductive competency/fertility. Gonadotropin hormone analogs have been used clinically …

A novel small molecule chaperone of rod opsin and its potential therapy for retinal degeneration

Y Chen, Y Chen, B Jastrzebska, M Golczak… - Nature …, 2018 - nature.com
Rhodopsin homeostasis is tightly coupled to rod photoreceptor cell survival and vision.
Mutations resulting in the misfolding of rhodopsin can lead to autosomal dominant retinitis …