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 …
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 …
includes orthosteric and allosteric drugs, which bind the protein at orthosteric and allosteric …
A µ-opioid receptor modulator that works cooperatively with naloxone
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 …
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
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 …
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)
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 …
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 …
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 …
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 …
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
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 …
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
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 …
for the treatment of Alzheimer's disease and metabolic disorders. However, the limited …