AIMC Topic: Receptors, G-Protein-Coupled

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Deep learning reveals endogenous sterols as allosteric modulators of the GPCR-Gα interface.

eLife
Endogenous intracellular allosteric modulators of GPCRs remain largely unexplored, with limited binding and phenotype data available. This gap arises from the lack of robust computational methods for unbiased cavity identification, cavity-specific li...

DeepTargetClass: a web-based platform for predicting protein target classes of small molecules.

Journal of computer-aided molecular design
The identification of protein target classes is a key step in drug discovery, as it enables prioritization of screening campaigns and supports target-based drug repurpose. In this study, we developed a deep-learning pipeline based on a multilayer per...

Cancer-associated fibroblasts enhance colorectal cancer lymphatic metastasis via CLEC11A/LGR5-mediated WNT pathway activation.

The Journal of clinical investigation
Hypoxia in the tumor microenvironment promotes lymphatic metastasis, yet the role of cancer-associated fibroblasts (CAFs) in this process remains insufficiently elucidated in colorectal cancer (CRC). In this study, we developed a large language model...

Mechanistic Basis for GPCR Phosphorylation-Dependent Allosteric Signaling Specificity of β-Arrestin 1 and 2.

Journal of chemical information and modeling
β-Arrestins (βarr1 and βarr2) are key transducers of G protein-coupled receptor (GPCR) signaling, orchestrating both shared and isoform-specific intracellular pathways. Phosphorylation of the receptor C-terminal tail by GPCR kinases encodes regulator...

Virtual screening of salty peptides from enzymatic and fermented products of wheat gluten and its molecular mechanism of interaction with TMC4 receptor.

Food chemistry
The health risks associated with excessive sodium intake have prompted an exploration of natural salt substitutes. This study was oriented to explore the salty peptides from enzymatic and fermented products of wheat gluten (WG) with different degrees...

Machine Learning Navigated Allosteric Network to Unveil Biased Allosteric Modulation of GPCRs.

Journal of chemical theory and computation
Biased allosteric modulators (BAMs) offer a promising avenue for developing safer and more selective therapeutics for G protein-coupled receptors (GPCRs). However, their molecular mechanisms remain unclear due to the complex combination of biased and...

Protein Structure-Function Relationship: A Kernel-PCA Approach for Reaction Coordinate Identification.

Journal of chemical theory and computation
In this study, we propose a Kernel-PCA model designed to capture structure-function relationships in a protein. This model also enables the ranking of reaction coordinates according to their impact on protein properties. By leveraging machine learnin...

In-silico guided identification and studies of potential FFAR4 agonists for type 2 diabetes mellitus therapy.

Expert opinion on drug discovery
BACKGROUND: The activation of free fatty acid receptor 4 (FFAR4) enhances insulin sensitivity and glucose uptake while mitigating inflammation. It is a promising therapeutic approach for managing type 2 diabetes mellitus (T2DM).

Comparing models and experimental structures of the GPR101 receptor: Artificial intelligence yields highly accurate models.

Journal of molecular graphics & modelling
Experimental structures solved through cryo-electron microscopy have recently been published for GPR101, a G protein-coupled receptor (GPCR) implicated in the genetic condition X-linked acrogigantism (X-LAG). Here, we compared these experimental stru...

Discovery of novel umami peptides and their bitterness masking effects from yellowfin tuna (Thunnus albacares) via peptidomics, multisensory evaluation, and molecular docking approaches.

Food chemistry
In this study, we identified and screened nine novel umami peptides derived from yellowfin tuna (Thunnus albacares) utilizing peptidomics combined with various machine learning based umami screening methodologies, including UMPred-FRL, TPDM, Umami-MR...