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 …
(GLP1R) and parathyroid hormone 1 receptor (PTH1R), are important drug targets …
Small molecule allosteric modulation of the adenosine A1 receptor
G protein-coupled receptors (GPCRs) represent the target for approximately a third of FDA-
approved small molecule drugs. The adenosine A1 receptor (A1R), one of four adenosine …
approved small molecule drugs. The adenosine A1 receptor (A1R), one of four adenosine …
Non‐peptide agonists and positive allosteric modulators of glucagon‐like peptide‐1 receptors: Alternative approaches for treatment of type 2 diabetes
F Malik, Z Li - British Journal of Pharmacology, 2022 - Wiley Online Library
Glucagon‐like peptide‐1 (GLP‐1) receptors belong to the pharmaceutically important Class
B family of GPCRs and are involved in many biologically significant signalling pathways. Its …
B family of GPCRs and are involved in many biologically significant signalling pathways. Its …
Bayesian metamodeling of complex biological systems across varying representations
Comprehensive modeling of a whole cell requires an integration of vast amounts of
information on various aspects of the cell and its parts. To divide and conquer this task, we …
information on various aspects of the cell and its parts. To divide and conquer this task, we …
Novel and emerging therapeutic drug targets for management of type 2 diabetes mellitus
DM (Diabetes Mellitus) can be divided to type 1 and type 2, but out of both, type 2 is more
predominant form of diabetes. At present approximate more than 451 million people (1 in 11 …
predominant form of diabetes. At present approximate more than 451 million people (1 in 11 …
Discovery of non-peptide GLP-1r natural agonists for enhancing coronary safety in type 2 diabetes patients
N Shakour, S Hoseinpoor, F Rajabian… - Journal of …, 2023 - Taylor & Francis
This study explores the computational discovery of non-peptide agonists targeting the
Glucagon-Like Peptide-1 Receptor (GLP-1R) to enhance the safety of major coronary …
Glucagon-Like Peptide-1 Receptor (GLP-1R) to enhance the safety of major coronary …
Allosteric modulators enhancing GLP-1 binding to GLP-1R via a transmembrane site
J Wang, D Yang, X Cheng, L Yang, Z Wang… - ACS Chemical …, 2021 - ACS Publications
The glucagon-like peptide-1 receptor (GLP-1R) is a well-established drug target for the
treatment of type II diabetes. The development of small-molecule positive allosteric …
treatment of type II diabetes. The development of small-molecule positive allosteric …
Discovery of novel allosteric modulators targeting an extra-helical binding site of GLP-1R using structure-and ligand-based virtual screening
Allosteric modulators have emerged with many potential pharmacological advantages as
they do not compete the binding of agonist or antagonist to the orthosteric sites but ultimately …
they do not compete the binding of agonist or antagonist to the orthosteric sites but ultimately …
Drug design of GLP-1 receptor agonists: Importance of in silico methods
Drug design based on degradation-resistant, long-acting Glucagon-like peptide-1 receptor
(GLP-1R) agonists for treating type 2 diabetes is attracting a lot of attention. Here, the …
(GLP-1R) agonists for treating type 2 diabetes is attracting a lot of attention. Here, the …
Discovery of a potential positive allosteric modulator of glucagon-like peptide 1 receptor through virtual screening and experimental study
The Glucagon-like peptide 1 receptor (GLP-1R) is a well-established target for the treatment
of type 2 diabetes and GLP-1R agonist-based therapies represent an effective approach …
of type 2 diabetes and GLP-1R agonist-based therapies represent an effective approach …