Molecular Pharmacology

Article	Citations
Arrestin-Dependent and -Independent Internalization of G Protein–Coupled Receptors: Methods, Mechanisms, and Implications on Cell Signaling	56
Metabotropic Glutamate Receptors As Emerging Targets for the Treatment of Schizophrenia	42
Remdesivir and EIDD-1931 Interact with Human Equilibrative Nucleoside Transporters 1 and 2: Implications for Reaching SARS-CoV-2 Viral Sanctuary Sites	33
β-Arrestin–Biased Allosteric Modulator Potentiates Carvedilol-Stimulated β Adrenergic Receptor Cardioprotection	27
Protective Effects of Flavonoids in Acute Models of Light-Induced Retinal Degeneration	24
The Tails of Protein Kinase A	23
Metformin Prevents Hyperglycemia-Associated, Oxidative Stress-Induced Vascular Endothelial Dysfunction: Essential Role for the Orphan Nuclear Receptor Human Nuclear Receptor 4A1 (Nur77)	23
Eribulin Activates the cGAS-STING Pathway via the Cytoplasmic Accumulation of Mitochondrial DNA	22
mTOR Regulation of AGC Kinases: New Twist to an Old Tail	21
Pharmacological Characterization of the Imipridone Anticancer Drug ONC201 Reveals a Negative Allosteric Mechanism of Action at the D2Dopamine Receptor	21
Unique Positive Cooperativity Between the β-Arrestin–Biased β-Blocker Carvedilol and a Small Molecule Positive Allosteric Modulator of the β2-Adrenergic Receptor	20
Characterization of Vixotrigine, a Broad-Spectrum Voltage-Gated Sodium Channel Blocker	18
Acylation of the Incretin Peptide Exendin-4 Directly Impacts Glucagon-Like Peptide-1 Receptor Signaling and Trafficking	18
Senolytic-Mediated Elimination of Head and Neck Tumor Cells Induced Into Senescence by Cisplatin	18
Ligand-Independent G Protein–Coupled Estrogen Receptor/G Protein–Coupled Receptor 30 Activity: Lack of Receptor-Dependent Effects of G-1 and 17β-Estradiol	18
Predicting Drug Interactions with Human Equilibrative Nucleoside Transporters 1 and 2 Using Functional Knockout Cell Lines and Bayesian Modeling	16
GPR83 Engages Endogenous Peptides from Two Distinct Precursors to Elicit Differential Signaling	16
The Sulfated Steroids Pregnenolone Sulfate and Dehydroepiandrosterone Sulfate Inhibit the α1β3γ2L GABAA Receptor by Stabilizing a Novel Nonconducting State	14
Mechanism-Based Inactivation of Cytochrome P450 3A4 by Benzbromarone	14
Membrane-Mediated Activity of Local Anesthetics	14
Drug-Drug Interaction between Metformin and Sorafenib Alters Antitumor Effect in Hepatocellular Carcinoma Cells	13
An Updated Review on Implications of Autophagy and Apoptosis in Tumorigenesis: Possible Alterations in Autophagy through Engineered Nanomaterials and Their Importance in Cancer Therapy	13
Structural Basis of the Negative Allosteric Modulation of 5-BDBD at Human P2X4 Receptors	13
Intrasubunit and intersubunit steroid binding sites independently and additively mediate α1β2γ2L GABAA receptor potentiation by the endogenous neurosteroid allopregnanolone	13
Structural Basis for the Allosteric Inhibition of Hypoxia-Inducible Factor 2 by Belzutifan	12

Macrophage-Inducible C-Type Lectin Signaling Exacerbates Acetaminophen-Induced Liver Injury by Promoting Kupffer Cell Activation in Mice	12
Short-Term Acyl-CoA:Cholesterol Acyltransferase Inhibition, Combined with Apoprotein A1 Overexpression, Promotes Atherosclerosis Inflammation Resolution in Mice	12
CRISPR/Cas9 Genome Editing of the Human Topoisomerase IIαIntron 19 5′ Splice Site Circumvents Etoposide Resistance in Human Leukemia K562 Cells	12
The Heartwarming Effect of Brown Adipose Tissue	11
Discovery of Novel Activators of Large-Conductance Calcium-Activated Potassium Channels for the Treatment of Cerebellar Ataxia	11
Update on Angiotensin II Subtype 2 Receptor: Focus on Peptide and Nonpeptide Agonists	11
Calcium Cycling as a Mediator of Thermogenic Metabolism in Adipose Tissue	11
Fluorizoline Blocks the Interaction between Prohibitin-2 and γ-Glutamylcyclotransferase and Induces p21Waf1/Cip1 Expression in MCF7 Breast Cancer Cells	11
Molecular Mechanisms for the Inflammation-Resolving Actions of Lenabasum	11
The Negative Allosteric Modulator EU1794-4 Reduces Single-Channel Conductance and Ca2+ Permeability of GluN1/GluN2A N-Methyl-d-Aspartate Receptors	10
Cysteine Modification by Ebselen Reduces the Stability and Cellular Levels of 14-3-3 Proteins	10
Decoding the Cardiac Actions of Protein Kinase D Isoforms	10
Multipathway In Vitro Pharmacological Characterization of Specialized Proresolving G Protein-Coupled Receptors	10
Resveratrol Binds Nuclear Receptor 4A1 (NR4A1) and Acts as an NR4A1 Antagonist in Lung Cancer Cells	10
High-Content Single-Cell Förster Resonance Energy Transfer Imaging of Cultured Striatal Neurons Reveals Novel Cross-Talk in the Regulation of Nuclear Signaling by Protein Kinase A and Extracellular Si	9
Novel Small Molecule Fibroblast Growth Factor 23 Inhibitors Increase Serum Phosphate and Improve Skeletal Abnormalities in Hyp Mice	9
Allosteric Modulator KM822 Attenuates Behavioral Actions of Amphetamine in Caenorhabditis elegans through Interactions with the Dopamine Transporter DAT-1	9
CPL207280, a Novel G Protein–Coupled Receptor 40/Free Fatty Acid Receptor 1–Specific Agonist, Shows a Favorable Safety Profile and Exerts Antidiabetic Effects in Type 2 Diabetic Animals	9
Ibrutinib Blocks YAP1 Activation and Reverses BRAF Inhibitor Resistance in Melanoma Cells	9
Identification of Celecoxib-Targeted Proteins Using Label-Free Thermal Proteome Profiling on Rat Hippocampus	9
GABAA Receptors Expressed in Oligodendrocytes Cultured from the Neonatal Rat Contain α3 and γ1 Subunits and Present Differential Functional and Pharmacological Properties	9
A Role for VCP/p97 in the Processing of Drug-Stabilized TOP2-DNA Covalent Complexes	9
Steroidal Antagonists of Progesterone- and Prostaglandin E1-Induced Activation of the Cation Channel of Sperm	9
Roles of Receptor Phosphorylation and Rab Proteins in G Protein-Coupled Receptor Function and Trafficking	9
ADP Ribosylation Factor 6 Promotes Contraction and Proliferation, Suppresses Apoptosis and Is Specifically Inhibited by NAV2729 in Prostate Stromal Cells	9
In Vitro Pharmacological Profile of KW-6356, a Novel Adenosine A2AReceptor Antagonist/Inverse Agonist	9
Inhibition of Bitter Taste from Oral Tenofovir Alafenamide	9
β2-Adrenoceptor Agonists Promote Extracellular Signal-Regulated Kinase 1/2 Dephosphorylation in Human Airway Epithelial Cells by Canonical, cAMP-Driven Signaling Independently of	9
Differential Reversible and Irreversible Interactions between Benzbromarone and Human Cytochrome P450s 3A4 and 3A5	9
Potential Use of Senolytics for Pharmacological Targeting of Precancerous Lesions	9
Thermal Unfolding of the Human Serotonin Transporter: Differential Effect by Stabilizing and Destabilizing Mutations and Cholesterol on Thermodynamic and Kinetic Stability	9
Regulation of Adrenergic, Serotonin, and Dopamine Receptors to Inhibit Diabetic Retinopathy: Monotherapies versus Combination Therapies	9
Insights into the Structure-Activity Relationship of Glycosides as Positive Allosteric Modulators Acting on P2X7 Receptors	9
Upacicalcet Is a Novel Secondary Hyperparathyroidism Drug that Targets the Amino Acid Binding Site of Calcium-Sensing Receptor	8
Nelfinavir and Its Active Metabolite M8 Are Partial Agonists and Competitive Antagonists of the Human Pregnane X Receptor	8
Biased Effect of Cardiotonic Steroids on Na/K-ATPase–Mediated Signal Transduction	8
Lubiprostone is a Non-Selective Activator of cAMP-Gated Ion Channels and Chloride Channel Protein 2 (Clc-2) Has a Minor Role in its Prosecretory Effect in Intestinal Epithelial Cells	8
Construction and Characterization of CRISPR/Cas9 Knockout Rat Model of Carboxylesterase 2a Gene	8
The Intracellular N-Terminal Domain of the Acid-Sensing Ion Channel 1a Participates in Channel Opening and Membrane Expression	8
Functional Interaction between Transient Receptor Potential V4 Channel and Neuronal Calcium Sensor 1 and the Effects of Paclitaxel	8
The Emerging Role of Neuronal Organoid Models in Drug Discovery: Potential Applications and Hurdles to Implementation	8
TP53 Null Mutations Identify Lung Cancer Cell Lines with Highest Sensitivity to the Nontaxane Microtubule Inhibitor Eribulin	8
Atypical Chemokine Receptor 3 “Senses” CXC Chemokine Receptor 4 Activation Through GPCR Kinase Phosphorylation	8
Membrane-Facilitated Receptor Access and Binding Mechanisms of Long-Acting β2-Adrenergic Receptor Agonists	7
Elevated cAMP Protects against Diclofenac-Induced Toxicity in Primary Rat Hepatocytes: A Protective Effect Mediated by the Exchange Protein Directly Activated by cAMP/cAMP-Regulated Guanine Nucleotide	7
Transforming Growth Factor β1 Increases Expression of Contractile Genes in Human Pulmonary Arterial Smooth Muscle Cells by Potentiating Sphingosine-1-Phosphate Signaling	7
Mechanisms to Repair Stalled Topoisomerase II-DNA Covalent Complexes	7
A Recombinant Dimethylarginine Dimethylaminohydrolase-1–Based Biotherapeutics to Pharmacologically Lower Asymmetric Dimethyl Arginine, thus Improving Postischemic Cardiac Function and Cardiomyocyte Mi	7
VU6036720: The First Potent and Selective In Vitro Inhibitor of Heteromeric Kir4.1/5.1 Inward Rectifier Potassium Channels	7
Identification of Chemical and Pharmacological Chaperones for Correction of Trafficking-Deficient Mutant Cyclic Nucleotide–Gated A3 Channels	7

Multiplex G Protein–Coupled Receptor Screen Reveals Reliably Acting Agonists and a Gq-Phospholipase C Coupling Mode of GPR30/GPER1	7
Novel Human-Derived RET Fusion NSCLC Cell Lines Have Heterogeneous Responses to RET Inhibitors and Differential Regulation of Downstream Signaling	7
A Novel Role of Uricosuric Agent Benzbromarone in BK Channel Activation and Reduction of Airway Smooth Muscle Contraction	7
Mice Expressing Regulators of G protein Signaling–insensitive Gαo Define Roles of μ Opioid Receptor Gαo and Gαi Subunit Coupling in Inhibition of Presynaptic GABA Release	7
Agonist-Specific Regulation of G Protein–Coupled Receptors after Chronic Opioid Treatment	7
Ferroptosis, Acyl Starvation, and Breast Cancer	7
Effects of Small Molecule Ligands on ACKR3 Receptors	7
Antidepressants Produce Persistent Gαs-Associated Signaling Changes in Lipid Rafts after Drug Withdrawal	7
Automated Intracellular Pharmacological Electrophysiology for Ligand-Gated Ionotropic Receptor and Pharmacology Screening	7
Lysine Demethylase 6B Regulates Prostate Cancer Cell Proliferation by Controlling c-MYC Expression	7
Phenylalanine 193 in Extracellular Loop 2 of the β2-Adrenergic Receptor Coordinates β-Arrestin Interaction	7
Transcriptome-Level Interactions between Budesonide and Formoterol Provide Insight into the Mechanism of Action of Inhaled Corticosteroid/Long-Acting β2-Adrenoceptor Agonist Combinat	6
Ethnic-Related Sodium Voltage-Gated Channel α Subunit 5 Polymorphisms Shape the In Vitro Pharmacological Action of Amiodarone upon Nav1.5	6
Degraders: The Ultimate Weapon Against Amplified Driver Kinases in Cancer	6
Inhibition of Human Uracil DNA Glycosylase Sensitizes a Large Fraction of Colorectal Cancer Cells to 5-Fluorodeoxyuridine and Raltitrexed but Not Fluorouracil	6
Coincident Regulation of PLCβSignaling by Gq-Coupled andμ-Opioid Receptors Opposes Opioid-Mediated Antinociception	6
New Synthetic Caffeine Analogs as Modulators of the Cholinergic System	6
High-Throughput Screening of TRPV1 Ligands in the Light of the Bioluminescence Resonance Energy Transfer Technique	6
Circular RNAs of UDP-Glycosyltransferase (UGT) Genes Expand the Complexity and Diversity of the UGT Transcriptome	6
Passive Immunotherapies Targeting Amyloid-βin Alzheimer’s Disease: A Quantitative Systems Pharmacology Perspective	6
Pharmacological Targeting of Senescence with Senolytics as a New Therapeutic Strategy for Neurodegeneration	6
Yeast β-glucan Increases Etoposide Sensitivity in Lung Cancer Cell Line A549 by Suppressing Nuclear Factor Erythroid 2-Related Factor 2 via the Noncanonical Nuclear Factor Kappa B Pathway	6
A20-Binding Inhibitor of Nuclear Factor-κB Targets β-Arrestin2 to Attenuate Opioid Tolerance	6
Positive Allosteric Modulators of Metabotropic Glutamate Receptor 5 as Tool Compounds to Study Signaling Bias	6
A Point Mutation at C151 ofKeap1of Mice Abrogates NRF2 Signaling, Cytoprotection in Vitro, and Hepatoprotection in Vivo by Bardoxolone Methyl (CDDO-Me)	6
CCT and CCT-Like Modular Protein Interaction Domains in WNK Signaling	6
Valproic Acid-Induced Upregulation of Multidrug Efflux Transporter ABCG2/BCRP via PPARα-Dependent Mechanism in Human Brain Endothelial Cells	6
Distinct regulation of cardiac fibroblast proliferation and transdifferentiation by classical and novel protein kinase C isoforms: possible implications for new antifibrotic therapies	6
Naturally Occurring Mutations to Muscle-Type Creatine Kinase Impact Its Canonical and Pharmacological Activities in a Substrate-Dependent Manner In Vitro	5
The Benzene Hematotoxic and Reactive Metabolite 1,4-Benzoquinone Impairs the Activity of the Histone Methyltransferase SET Domain Containing 2 (SETD2) and Causes Aberrant Histone H3 Lysine 36 Trimethy	5
Dynamic Expression of Transient Receptor Potential Vanilloid-3 and Integrated Signaling with Growth Factor Pathways during Lung Epithelial Wound Repair following Wood Smoke Particle and Other Forms of	5
Therapeutic Neuroprotection by an Engineered Neurotrophin that Selectively Activates Tropomyosin Receptor Kinase (Trk) Family Neurotrophin Receptors but Not the p75 Neurotrophin Receptor	5
A Potential Role for SerpinA3N in Acetaminophen-Induced Hepatotoxicity	5
Multiomics Analyses Identify Proline Endopeptidase–Like Protein As a Key Regulator of Protein Trafficking, a Pathway Underlying Alzheimer’s Disease Pathogenesis	5
Decoding Cinnabarinic Acid–Specific Stanniocalcin 2 Induction by Aryl Hydrocarbon Receptor	5
Phosphoproteomic Analysis as an Approach for Understanding Molecular Mechanisms of cAMP-Dependent Actions	5
A Benzodiazepine Ligand with Improved GABAA Receptor α5-Subunit Selectivity Driven by Interactions with Loop C	5
Cancer-Type Organic Anion Transporting Polypeptide 1B3 Is Localized in Lysosomes and Mediates Resistance against Kinase Inhibitors	5
Gossypetin Prevents the Progression of Nonalcoholic Steatohepatitis by Regulating Oxidative Stress and AMP-Activated Protein Kinase	5
Cholesterol Inhibition of Slo1 Channels Is Calcium-Dependent and Can Be Mediated by Either High-Affinity Calcium-Sensing Site in the Slo1 Cytosolic Tail	5
The Emerging Structural Pharmacology of ATP-Sensitive Potassium Channels	5
Influence of the TARP γ8-Selective Negative Allosteric Modulator JNJ-55511118 on AMPA Receptor Gating and Channel Conductance	5
How Physiological Targets Can Be Distinguished from Drug-binding Proteins	4
Influence of Tyrosine Kinase Inhibition on Organic Anion Transporting Polypeptide 1B3-Mediated Uptake	4
Thermogenic Modulation of Adipose Depots: A Perspective on Possible Therapeutic Intervention with Early Cardiorenal Complications of Metabolic Impairment	4
Current Understanding of Membrane Transporters as Regulators or Targets for Cisplatin-Induced Hearing Loss	4
Differential Enantiomer-Specific Signaling of Cannabidiol at CB1Receptors	4
Michaelis-Menten quantification of ligand signalling bias applied to the promiscuous Vasopressin V2 receptor	4
Aryl Hydrocarbon Receptor as a Therapeutical Target of Environmentally Induced Skin Conditions	4
Pharmacological Characterization and Radiolabeling of VUF15485, a High-Affinity Small-Molecule Agonist for the Atypical Chemokine Receptor ACKR3	4
Thermal Proteome Profiling Reveals Glutathione Peroxidase 4 as the Target of the Autophagy Inducer Conophylline	4
The GlycosylatedN-Terminal Domain of MUC1 Is Involved in Chemoresistance by Modulating Drug Permeation Across the Plasma Membrane	4
Analgesic α-Conotoxin Binding Site on the Human GABAB Receptor	4
Antitumor Activity of Novel Signal Transducer and Activator of Transcription 3 Inhibitors on Retinoblastoma	4
A Regional and Projection-Specific Role of RGSz1 in the Ventrolateral Periaqueductal Grey in the Modulation of Morphine Reward	4
Use-Dependent Relief of Inhibition of Nav1.8 Channels by A-887826	4
Physiologic Targets and Modes of Action for CBL0137, a Lead for Human African Trypanosomiasis Drug Development	4
Live Tissue Imaging Reveals Distinct Transcellular Pathways for Organic Cations and Anions at the Blood-Cerebrospinal Fluid Barrier	4
Selection and Characterization of FD164, a High-Affinity Signal Regulatory Protein α Variant with Balanced Safety and Effectiveness, from a Targeted Epitope Mammalian Cell-Displayed Antibody Li	4
Mutual Cooperativity of Three Allosteric Sites on the Dopamine D1 Receptor	4
The Potential Antidepressant Compound Org 34167 Modulates HCN Channels Via a Novel Mode of Action	4
Alkannin Attenuates AmyloidβAggregation and Alzheimer’s Disease Pathology	4
Phosphoproteomics-Based Characterization of Prostaglandin E2Signaling in T Cells	4
Expression of Ceramide Synthases in Mice and Their Roles in Regulating Acyl-Chain Sphingolipids: A Framework for Baseline Levels and Future Implications in Aging and Disease	4
A High-Throughput Screening Assay to Identify Drugs that Can Treat Long QT Syndrome Caused by Trafficking-Deficient KV11.1 (hERG) Variants	4
Proteomic Approaches to Investigate Regulated Trafficking and Signaling of G Protein–Coupled Receptors	4
Tacrine Induces Endoplasmic Reticulum–Stressed Apoptosis via Disrupting the Proper Assembly of Oligomeric Acetylcholinesterase in Cultured Neuronal Cells	3
A Complete Endocannabinoid Signaling System Modulates Synaptic Transmission between Human Induced Pluripotent Stem Cell–Derived Neurons	3
Molecular and Functional Characterization of GABA Receptor Subunits GRD and LCCH3 from Human Louse Pediculus Humanus Humanus	3
Identification and Characterization of a Novel Large-Conductance Calcium-Activated Potassium Channel Activator, CTIBD, and Its Relaxation Effect on Urinary Bladder Smooth Muscle	3
Molecular Determinants Underlying Delta Selective Compound 2 Activity at δ-Containing GABAA Receptors	3
Commentary on “Novel Interaction of the Dopamine D2 Receptor and the Ca2+ Binding Protein S100B: Role in D2 Receptor Function”	3
Mechanisms Underlying the Inhibition of KV1.3 Channel by Scorpion Toxin ImKTX58	3
Drug Targeting of Acyltransferases in the Triacylglyceride and 1-O-AcylCeramide Biosynthetic Pathways	3
Effects of Sarcomere Activators and Inhibitors Targeting Myosin Cross-Bridges on Ca2+-Activation of Mature and Immature Mouse Cardiac Myofilaments	3
Differential In vitro Pharmacological Profiles of Structurally Diverse Nociceptin Receptor Agonists in Activating G-protein and Beta-arrestin Signaling at the Human Nociceptin Opioid Receptor	3
Screening for Novel Type 2 Ryanodine Receptor Inhibitors by Endoplasmic Reticulum Ca2+Monitoring	3
A Comment on “Remdesivir and EIDD-1931 Interact with Human Equilibrative Nucleoside Transporters 1 and 2: Implications for Reaching SARS-CoV-2 Viral Sanctuary Sites”	3
The Common LncRNAs of Neuroinflammation-Related Diseases	3
Chronic Exposure to SCO-267, an Allosteric GPR40 Full Agonist, Is Effective in Improving Glycemic Control in Rats	3

Insights Into the Differential Desensitization ofα4β2 Nicotinic Acetylcholine Receptor Isoforms Obtained With Positive Allosteric Modulation of Mutant Receptors	3
Hexahydroquinoline Derivatives Are Selective Agonists for the Adhesion G Protein-Coupled Receptor ADGRG1/GPR56	3