Structure and Function of Somatostatin and its Receptors in Endocrinology

B Zhang, L Xue, ZB Wu - Endocrine Reviews, 2025 - academic.oup.com
Somatostatin analogs, such as octreotide, lanreotide, and pasireotide, which function as
somatostatin receptor ligands (SRLs), are the main drugs used for the treatment of …

Designing drugs and chemical probes with the dualsteric approach

J Zha, J He, C Wu, M Zhang, X Liu… - Chemical Society Reviews, 2023 - pubs.rsc.org
Traditionally, drugs are monovalent, targeting only one site on the protein surface. This
includes orthosteric and allosteric drugs, which bind the protein at orthosteric and allosteric …

A µ-opioid receptor modulator that works cooperatively with naloxone

ES O'Brien, VA Rangari, A El Daibani, SO Eans… - Nature, 2024 - nature.com
The µ-opioid receptor (µOR) is a well-established target for analgesia, yet conventional
opioid receptor agonists cause serious adverse effects, notably addiction and respiratory …

Design and structural validation of peptide–drug conjugate ligands of the kappa-opioid receptor

E Muratspahić, K Deibler, J Han, N Tomašević… - Nature …, 2023 - nature.com
Despite the increasing number of GPCR structures and recent advances in peptide design,
the development of efficient technologies allowing rational design of high-affinity peptide …

How neuromembrane lipids modulate membrane proteins: insights from G-protein-coupled receptors (GPCRs) and receptor tyrosine kinases (RTKs)

M Girych, W Kulig, G Enkavi… - Cold Spring Harbor …, 2023 - cshperspectives.cshlp.org
Lipids play a diverse and critical role in cellular processes in all tissues. The unique lipid
composition of nerve membranes is particularly interesting because it contains, among other …

Allosteric modulation of GPCRs: From structural insights to in silico drug discovery

M Persechino, JB Hedderich, P Kolb… - Pharmacology & …, 2022 - Elsevier
G protein-coupled receptors (GPCRs) play critical roles in human physiology and are one of
the prime targets for marketed drugs. While traditional drug discovery programs have …

Molecular determinants of ligand efficacy and potency in GPCR signaling

FM Heydenreich, M Marti-Solano, M Sandhu… - Science, 2023 - science.org
Heterotrimeric guanine nucleotide–binding protein (G protein)–coupled receptors (GPCRs)
bind to extracellular ligands and drugs and modulate intracellular responses through …

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 …

Targeting in silico GPCR conformations with ultra-large library screening for hit discovery

D Sala, H Batebi, K Ledwitch, PW Hildebrand… - Trends in …, 2023 - cell.com
The use of deep machine learning (ML) in protein structure prediction has made it possible
to easily access a large number of annotated conformations that can potentially compensate …

Development of fluorescent AF64394 analogues enables real-time binding studies for the orphan class A GPCR GPR3

M Bresinsky, A Shahraki, P Kolb, S Pockes… - Journal of Medicinal …, 2023 - ACS Publications
The orphan G protein-coupled receptor (oGPCR) GPR3 represents a potential drug target
for the treatment of Alzheimer's disease and metabolic disorders. However, the limited …