Molecular Pharmacology

Article	Citations
A 19F-qNMR-Guided Mathematical Model for G Protein-Coupled Receptor Signaling	69
Simplified Method for Kinetic and Thermodynamic Screening of Cardiotonic Steroids through the K+-Dependent Phosphatase Activity of Na+/K+-ATPase with Chromogenic pNPP Substrate	44
In Vitro Pharmacological Profile of KW-6356, a Novel Adenosine A2A Receptor Antagonist/Inverse Agonist	37
Fat traffic control: S-acylation in axonal transport	37
Enhancing remyelination in multiple sclerosis via M1 muscarinic acetylcholine receptor	36
UCM-A86 is a selective positive allosteric modulator of GluN1/GluN3 NMDA receptors	35
Structural Basis for the Allosteric Inhibition of Hypoxia-Inducible Factor 2 by Belzutifan	32
Expression of concern: “Adelmidrol, a Palmitoylethanolamide Analogue, as a New PharmacologicalTreatment for the Management of Inflammatory Bowel Disease” [Mol. Pharmacol. 2016; 90: 549-561] by Cordaro	29
Editorial Board	28
Editorial Board	28
Table of Contents	28
Mechanism-based inactivation of human aldehyde oxidase by erlotinib: Mechanistic insights from structural analogs and molecular docking	24
Thermogenic Modulation of Adipose Depots: A Perspective on Possible Therapeutic Intervention with Early Cardiorenal Complications of Metabolic Impairment	20
Development of a Novel Assay for Direct Assessment of Selective Amylin Receptor Activation Reveals Novel Differences in Behavior of Selective and Nonselective Peptide Agonists	18
Regulation of organic anion transporting polypeptide 1B1 transport function by concurrent phosphorylation and lysine-acetylation: A novel posttranslational regulation mechanism	17
Cholesterol residence time drives regulation of the G protein-coupled cholecystokinin receptor	17
Isoprenaline shows unique kinase dependencies in stimulating β1AR–β-arrestin2 interaction compared to endogenous catecholamines	17
Targeting Cyclophilin A and CD147 to Inhibit Replication of Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) and SARS-CoV-2–Induced Inflammation	16
Editorial Board	16
Discovery of RGS2-FBXO44 interaction inhibitors using a cell-based NanoBit assay	15
The Emerging Structural Pharmacology of ATP-Sensitive Potassium Channels	15
GPR83 Engages Endogenous Peptides from Two Distinct Precursors to Elicit Differential Signaling	15
6,7-Dichloro-1H-indole-2,3-dione-3-oxime functions as a superagonist for the intermediate-conductance Ca2+-activated K+ channel KCa3.1	13
Resveratrol Binds Nuclear Receptor 4A1 (NR4A1) and Acts as an NR4A1 Antagonist in Lung Cancer Cells	13
Corrigendum to “Antitumor Effects of Dehydroxymethylepoxyquinomicin, a Novel Nuclear Factor-κB Inhibitor, in Human Liver Cancer Cells Are Mediated through a Reactive Oxygen Species-Dependent Mechanism	13

St. John’s Wort Formulations Induce Rat CYP3A23-3A1 Independent of Their Hyperforin Content	13
Research approaches for exploring the hidden conversations of G protein-coupled receptor transactivation	13
BAY58-2667 Activates Different Soluble Guanylyl Cyclase Species by Distinct Mechanisms that Indicate Its Principal Target in Cells is the Heme-Free Soluble Guanylyl Cyclase-Heat Shock Protein 90 Compl	12
Editorial Board	12
A brief history of nerve action potentials after 1600	12
Englerin A Inhibits T-Type Voltage-Gated Calcium Channels at Low Micromolar Concentrations	12
Table of Contents	12
Pore Opening, Not Voltage Sensor Movement, Underpins the Voltage-Dependence of Facilitation by a hERG Blocker	12
Table of Contents	11
Corrigendum to “A subunit-selective negative allosteric modulator of GluN1/GluN3A glycine-activated receptor” [Molecular Pharmacology 108 (2026) 100104]	11
Differential RELA and GR recruitment to the BIRC3/BIRC2 locus: Molecular insight as to combinatorial regulation by proinflammatory cytokines and glucocorticoid	11
Commentary on the fourth Transatlantic G Protein-Coupled Receptor Symposium for early-career investigators	11
Distinctive patterns of G protein coupling induced by the structurally similar 5-HT2A receptor ligands ketanserin and altanserin in human prefrontal cortex	11
Correction to “A Brief Overview of the Toxic Sphingomyelinase Ds of Brown Recluse Spider Venom and Other Organisms and Simple Methods To Detect Production of Its Signature Cyclic Ceramide Phosphate”	11
Emerging roles of ubiquitin-specific proteases in the cardiovascular system	11
Correction to “Sulforaphane Suppresses Polycomb Group Protein Level via a Proteasome-Dependent Mechanism in Skin Cancer Cells”	11
Modulation of Kv7 Channel Currents by Echinocystic Acid	11
Rational design of biased G protein-coupled receptor agonists	11
Role of HNF4A-AS1/HNRNPC-mediated HNF4A ubiquitination protection against ritonavir-induced hepatotoxicity	11
Corticosterone stimulates synthesis of 2-arachidonoylglycerol via putative membrane-bound glucocorticoid receptors and inhibits GABA release via CB1 cannabinoid receptors in the ventrolateral periaque	11
Repurposing lapatinib as a triple antagonist of chemokine receptors 3, 4, and 5	10
The β2 adrenergic receptor cross-linked interactome identifies 14-3-3 proteins as regulating the availability of signaling-competent receptors	10
Predicting compounds that interact with the 2 known agonist-induced conformations of the human β1-adrenoceptor	10
Going Rogue: Mechanisms, Regulation, and Roles of Mutationally Activated Gα in Human Cancer	10
Discovery and In Vitro Characterization of BAY 2686013, an Allosteric Small Molecule Antagonist of the Human Pituitary Adenylate Cyclase-Activating Polypeptide Receptor	10
Editorial Board	10
Expression of concern: “Caveolin-1 and Lipid Microdomains Regulate Gs Trafficking and Attenuate Gs/Adenylyl Cyclase Signaling” [Molecular Pharmacology, Volume 76, Issue 5, November 2009, Pages 1082-10	10
Editorial Board	10
EP4 Receptor Conformation Sensor Suited for Ligand Screening and Imaging of Extracellular Prostaglandins	10
Gα Protein Signaling Bias at Serotonin 1A Receptor	10
Contents	10
Corrigendum to “Novel Thiosemicarbazones Inhibit Lysine-Rich Carcinoembryonic Antigen-Related Cell Adhesion Molecule 1 (CEACAM1) Coisolated (LYRIC) and the LYRIC-Induced Epithelial- Mesenchymal Transi	10
β-Caryophyllene Inhibits Monoacylglycerol Lipase Activity and Increases 2-Arachidonoyl Glycerol Levels In Vivo: A New Mechanism of Endocannabinoid-Mediated Analgesia?	9
Editorial Board	9
Structural and Molecular Determinants of Glutamate Transporter Allosteric Modulators	9
Editorial Board	9
Heterogeneous nuclear ribonucleoprotein A/B drives gastric cancer and epithelial-mesenchymal transition via the Akt-GSK3β-Wnt pathway	9
The effects of hippocampal miR-34c-5p on the age-related discrepancies in susceptibility to traumatic stress in the post-traumatic stress disorder mice model	9
Table of Contents	8
Table of Contents	8
Corrigendum to “Targeting the Metastasis Suppressor, N-Myc Downstream Regulated Gene-1, with Novel Di-2- Pyridylketone Thiosemicarbazones: Suppression of Tumor Cell Migration and Cell-Collagen Adhesio	8
GRK2 and GRK5—The 2 critical kinases in cardiac pathophysiology	7
Upregulating vascular endothelial KCa2.3 channels alleviates pulmonary hypertension in mice	7
Induced Fit Describes Ligand Binding to Membrane-Associated Cytochrome P450 3A4	7
The M3 Muscarinic Acetylcholine Receptor Can Signal through Multiple G Protein Families	7
The Glycosylated N-Terminal Domain of MUC1 Is Involved in Chemoresistance by Modulating Drug Permeation Across the Plasma Membrane	7
Corrigendum to “The Natural Compound Withaferin A Covalently Binds to Cys239 of β-Tubulin to Promote Tubulin Degradation”	7
A Novel Role of Uricosuric Agent Benzbromarone in BK Channel Activation and Reduction of Airway Smooth Muscle Contraction	7
Editorial Board	7
Development of an LC-MS/MS Method to Measure Sphingolipids in CSF from Patients with Multiple Sclerosis	7

Circumvention of Topoisomerase IIα Intron 19 Intronic Polyadenylation in Acquired Etoposide-Resistant Human Leukemia K562 Cells	6
N-(4-Bromo-2,5-Dimethoxyphenethyl)-6-(4-Phenylbutoxy)Hexan-1-Amine (XOB): A Novel Phenylalkylamine Antagonist of Serotonin 2A Receptors and Voltage-Gated Sodium Channels	6
Aryl Hydrocarbon Receptor as a Therapeutical Target of Environmentally Induced Skin Conditions	6
Loss of α-cell GRK2 modulates glucagon response and supports cardiac function	6
Activation of TRPV3 channels in bladder cancer cells stimulates ATP release	6
Molecular determinants of 2-aminoethoxydiphenyl borate sensitivity of transient receptor potential vanilloid 2-unexpected differences between 2 rodent orthologs	6
Fanning the Flames of Endoplasmic Reticulum (ER) Stress: Can Sphingolipid Metabolism Be Targeted to Enhance ER Stress–Associated Immunogenic Cell Death in Cancer?	6
Live Tissue Imaging Reveals Distinct Transcellular Pathways for Organic Cations and Anions at the Blood-Cerebrospinal Fluid Barrier	6
Inhibition of Cardiac Kv4.3/KChIP2 Channels by Sulfonylurea Drug Gliquidone	6
Insights Into the Differential Desensitization of α4β2 Nicotinic Acetylcholine Receptor Isoforms Obtained With Positive Allosteric Modulation of Mutant Receptors	6
Elucidating the binding and metabolic interactions of sunitinib and sorafenib with Cytochrome P450s CYP2U1 and CYP2D6	6
Electrophysiological characterization of the state-dependent inhibition of Kv7.1 and IKs by UCL2077	6
Editorial Board	6
The thiazolidinedione drug troglitazone inhibits Gq signaling through direct binding to the Gq alpha subunit through inhibition of GDP release	6
Pharmacological Characterization and Radiolabeling of VUF15485, a High-Affinity Small-Molecule Agonist for the Atypical Chemokine Receptor ACKR3	6
Pharmacological Targeting of Senescence with Senolytics as a New Therapeutic Strategy for Neurodegeneration	6
Cepharanthine, a valuable sanative alternative for hepatocellular carcinoma through regulating Hippo-Yes-associated protein signal transduction	6
Elucidating molecular mechanisms governing tumor necrosis factor-alpha–mediated regulation of amyloid beta 42 uptake in blood-brain barrier endothelial cells	6
Mechanisms of Action Underlying Conductance-Modifying Positive Allosteric Modulators of the NMDA Receptor	6
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	5
Multiomics Analyses Identify Proline Endopeptidase–Like Protein As a Key Regulator of Protein Trafficking, a Pathway Underlying Alzheimer’s Disease Pathogenesis	5
Editorial Board	5
Evaluation of allosteric N-methyl-d-aspartate receptor modulation by GluN2A-selective antagonists using pharmacological equilibrium modeling	5
Table of Contents	5
Role of Mitochondrial and Cytosolic Folylpolyglutamate Synthetase in One-Carbon Metabolism and Antitumor Efficacy of Mitochondrial-Targeted Antifolates	5
Drugs Form Ternary Complexes with Human Liver Fatty Acid Binding Protein 1 (FABP1) and FABP1 Binding Alters Drug Metabolism	5
A Sentimental Segue	5
Editorial Board	5
Interaction between W41 of the hepatitis B virus preS1 surface peptide and Y146/F274 of the cellular receptor molecule Na+/taurocholate co-transporting polypeptide is essential for virus entry	5
Amyloid-Beta Peptides 40 and 42 Employ Distinct Molecular Pathways for Cell Entry and Intracellular Transit at the Blood–Brain Barrier Endothelium	5
HDAC6 inhibition ameliorates sensory hypersensitivity and reduces immune cell signatures in the dorsal root ganglia in murine chronic pain models	5
The Common LncRNAs of Neuroinflammation-Related Diseases	5
Substituted Cysteine Modification and Protection with n-Alkyl-MTS Reagents Quantifies Steric Changes Induced by a Mutation in Anesthetic Binding Sites on GABA Type A Receptors	5
Ca2+/Calmodulin-Dependent Inhibitors of Adenylyl Cyclase 1 as Novel Non-Opioid Analgesics for Chronic Inflammatory Pain	5
Extrachromosomal Circular DNAs, Amplified Oncogenes, and CRISPR-Cas9 System	4
Correction to “Neratinib Reverses ATP-Binding Cassette B1-Mediated Chemotherapeutic Drug Resistance In Vitro, In Vivo, and Ex Vivo”	4
Coassembly of Warm Temperature–Sensitive Transient Receptor Potential Vanilloid (TRPV) 3 and TRPV4 Channel Complexes with Distinct Functional Properties	4
Screening and Identification of a Novel Anti–Siglec-15 Human Antibody 3F1 and Relevant Antitumor Activity	4
Effects of two structurally diverse positive allosteric modulators on signaling bias at the μ-opioid receptor	4
Differential Activity of Orthosteric Agonists and Allosteric Modulators at Metabotropic Glutamate Receptor 7	4
Influence of the TARP γ8-Selective Negative Allosteric Modulator JNJ-55511118 on AMPA Receptor Gating and Channel Conductance	4
Upacicalcet Is a Novel Secondary Hyperparathyroidism Drug that Targets the Amino Acid Binding Site of Calcium-Sensing Receptor	4
Voltage sensor interaction site for a selective small molecule Nav1.1 sodium channel potentiator that enhances firing of fast-spiking interneurons	4
A Constitutive EGFR Kinase Dimer to Study Inhibitor Pharmacology	4
Corrigendum to “Repurposing Treprostinil for Enhancing Hematopoietic Progenitor Cell Transplantation”	4
Development of a Selective and High Affinity Radioligand, [3H]VU6013720, for the M4 Muscarinic Receptor	4
The Synthetic Cannabinoid WIN55,212-2 Can Disrupt the Golgi Apparatus Independent of Cannabinoid Receptor-1	4
Editorial Board	4
State-Dependent Inhibition of Nav1.8 Sodium Channels by VX-150 and VX-548	4
Table of Contents	4
Cannabinoid receptor 2 activating antibodies: A promising therapeutic strategy for macrophage-driven fibro-inflammatory diseases	4
Alkannin Attenuates Amyloid β Aggregation and Alzheimer’s Disease Pathology	3
Atypical Chemokine Receptor 3 “Senses” CXC Chemokine Receptor 4 Activation Through GPCR Kinase Phosphorylation	3
Corrigendum to “Functional Interaction between Transient Receptor Potential V4 Channel and Neuronal Calcium Sensor 1 and the Effects of Paclitaxel”	3
Nuclear Ceramide Is Associated with Ataxia Telangiectasia Mutated Activation in the Neocarzinostatin-Induced Apoptosis of Lymphoblastoid Cells	3
Influence of Tyrosine Kinase Inhibition on Organic Anion Transporting Polypeptide 1B3-Mediated Uptake	3
Passive Immunotherapies Targeting Amyloid-β in Alzheimer’s Disease: A Quantitative Systems Pharmacology Perspective	3
The peroxisome proliferator–activated receptor α/β/γ agonist NCPC-626 from microbial metabolites alleviates metabolic dysfunction–associated steatohepatitis in mice	3
Molecular and cellular effects of hydroxy-1,4 naphthoquinones used in dermatological and cosmetic applications on human protein tyrosine phosphatase PTP1B in human keratinocytes	3
Contents	3
Dual nuclear receptor 4A1 (NR4A1/NR4A2) ligands inhibit glioblastoma growth and target TWIST1	3
Editorial Board	3
Chemokine receptors – Exemplifying functional divergence in G protein-coupled receptors	3
Transcriptional Regulation, Signaling Pathways, and Subcellular Localization of Corticotropin-Releasing Factor Receptors in the Central Nervous System	3
Agonists of the Nuclear Receptor PPARγ Can Produce Biased Signaling	3
A machine learning–based analysis method for small molecule high content screening of three-dimensional cancer spheroid morphology	3
The Small Molecule Antagonist KCI807 Disrupts Association of the Amino-Terminal Domain of the Androgen Receptor with ELK1 by Modulating the Adjacent DNA Binding Domain	3
Table of Contents	3
Multiwalled carbon nanotubes activate the NLRP3 inflammasome-dependent pyroptosis in macrophages	3
Ketamine and Major Ketamine Metabolites Function as Allosteric Modulators of Opioid Receptors	3
New Mechanisms Underlying Oncogenesis in Dbl Family Rho Guanine Nucleotide Exchange Factors	3
Rare variant in intracellular loop-2 alters the spatial distribution and transducer coupling selectivity of the ghrelin receptor	3
G protein-coupled receptor–targeted proteolysis-targeting chimeras in cancer therapeutics	3
Cyclovirobuxine inhibits ferroptosis to mitigate Alzheimer disease in glutamate-induced SH-SY5Y cell: the role of the liquid-liquid phase separation of FTH1	3
Coexpressed δ-, μ-, and κ-Opioid Receptors Modulate Voltage-Gated Ca2+ Channels in Gastric-Projecting Vagal Afferent Neurons	2
Voltage sensors	2
Receptor Determinants for β-Arrestin Functional Specificity at C-X-C Chemokine Receptor 5	2
Deorphanization of G Protein Coupled Receptors: A Historical Perspective	2
Correction to “Gossypetin Prevents the Progression of Nonalcoholic Steatohepatitis by Regulating Oxidative Stress and AMP-Activated Protein Kinase”	2
Transient receptor potential vanilloid 3 activation accelerates keratinocyte migration in vitro but not dermal wound healing in vivo	2

Differential Effects of Remdesivir and Lumacaftor on Homomeric and Heteromeric hERG Channels	2
Signaling Specificity and Kinetics of the Human Metabotropic Glutamate Receptors	2
Special Section on Therapeutic Implications for Sphingolipids in Health and Disease—Editorial	2
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	2
Editorial Board	2
Pirin does not bind to p65 or regulate NFκB-dependent gene expression but does modulate cellular quercetin levels	2
Rescue of Familial Lecithin:Cholesterol Acyltranferase Deficiency Mutations with an Allosteric Activator	2
Biasing Gβγ Downstream Signaling with Gallein Inhibits Development of Morphine Tolerance and Potentiates Morphine-Induced Nociception in a Tolerant State	2
Emerging voices in G protein-coupled receptor biology	2
Inhibition of Tumor-Derived C-C Motif Chemokine Ligand 2 Expression Attenuates Tactile Allodynia in NCTC 2472 Fibrosarcoma-Inoculated Mice	2
Table of Contents	2
Pharmacological Characterization of the Zebrafish (Danio Rerio) Histamine H1 Receptor Reveals the Involvement of the Second Extracellular Loop in the Binding of Histamine	2
Comparative evaluation of the biological characteristics of a novel retinoid X receptor agonist and bexarotene	2
Amiodarone irrecoverably impairs the function of human ether-a-go-go-related gene potassium channels	2
Therapeutic Potential for Metabotropic Glutamate Receptor 7 Modulators in Cognitive Disorders	2
Table of Contents	2
Investigation of the binding mode of clobenprobit at CXCR4 and development of novel anti-inflammatory compounds with enhanced activity and minimal antagonist effects	2
Corrigendum to “Investigation of the binding mode of clobenprobit at CXCR4 and development of novel anti-inflammatory compounds with enhanced activity and minimal antagonist effects” [Molecular Pharma	2
Bioengineered miR-7-5p modulates non–small cell lung cancer cell metabolism to improve therapy	2
Effects of Small Molecule Ligands on ACKR3 Receptors	2
Correction to “A Novel Semisynthetic Inhibitor of the FRB Domain of Mammalian Target of Rapamycin Blocks Proliferation and Triggers Apoptosis in Chemoresistant Prostate Cancer Cells”	2
Functional Assessment of Cancer-Linked Mutations in Sensitive Regions of Regulators of G Protein Signaling Predicted by Three-Dimensional Missense Tolerance Ratio Analysis	1
Pharmacologic Characterization of LTGO-33, a Selective Small Molecule Inhibitor of the Voltage-Gated Sodium Channel NaV1.8 with a Unique Mechanism of Action	1
Prodigiosin Inhibits Transforming Growth Factor β Signaling by Interfering Receptor Recycling and Subcellular Translocation in Epithelial Cells	1
The Potential Antidepressant Compound Org 34167 Modulates HCN Channels Via a Novel Mode of Action	1
Discovery of Novel Activators of Large-Conductance Calcium-Activated Potassium Channels for the Treatment of Cerebellar Ataxia	1
Introduction of a single carboxylic acid converts the cyclic oligomeric depsipeptide ent-verticilide from a ryanodine receptor 2 (RyR2) inhibitor to RyR2 activator	1
Inhibitory Actions of Potentiating Neuroactive Steroids in the Human α1β3γ2L γ-Aminobutyric Acid Type A Receptor	1
Agonist-Specific Regulation of G Protein–Coupled Receptors after Chronic Opioid Treatment	1
Pharmacological characterization of a clinical candidate, TG-0054, a small molecule inverse agonist targeting CXCR4	1
Serotonin-Mediated Activation of Serotonin Receptor Type 1 Oppositely Modulates Voltage-Gated Calcium Channel Currents in Rat Sensory Neurons Innervating Hindlimb Muscle	1
Table of Contents	1
Extracellular ATP increases agonist potency and reduces latency at class B G protein-coupled receptors	1
Table of Contents	1
Expression of concern: “The Cyclopentenone Prostaglandin 15-Deoxy-delta12,14-Prostaglandin J2 Attenuates the Development of Acute and Chronic Inflammation” [Mol. Pharmacol. 2002; 61: 997-1007] by Cuzz	1
Discovery and Characterization of VU0542270, the First Selective Inhibitor of Vascular Kir6.1/SUR2B KATP Channels	1
Liver CYP4A autophagic lysosomal degradation: A major role for the autophagic receptor SQSTM1/p62 through an uncommon target interaction site	1
Editorial Board	1
Mechanisms for Enhancement of μ-Opioid Receptor-Mediated Antinociception in the Central Nervous System Through Gallein-Dependent Modulation of Downstream G Protein βγ Subunit Signaling	1
Determinants of Subtype-Selectivity of the Anthelmintic Paraherquamide A on Caenorhabditis elegans Nicotinic Acetylcholine Receptors	1
Intracellular Allosteric Antagonist of the Olfactory Receptor OR51E2	1
Synergy between Interleukin-1β, Interferon-γ, and Glucocorticoids to Induce TLR2 Expression Involves NF-κB, STAT1, and the Glucocorticoid Receptor	1
Perspective: Therapeutic Implications for Sphingolipids in Health and Disease	1
Ion channels and G protein-coupled receptors: Cannabidiol actions on disorders of excitability and synaptic excitatory-inhibitory ratio	1
Editorial Board	1
Screening for Novel Type 2 Ryanodine Receptor Inhibitors by Endoplasmic Reticulum Ca2+ Monitoring	1
Inhibition of the Aromatase Enzyme by Exemestane Cysteine Conjugates	1
Design and evaluation of highly selective histone deacetylase 6 inhibitors derived from the natural product tryptoline	1
Editorial Board	1
Protein Kinases and Cross-talk between Post-translational Modifications in the Regulation of Drug Transporters	1
VU6036720: The First Potent and Selective In Vitro Inhibitor of Heteromeric Kir4.1/5.1 Inward Rectifier Potassium Channels	1
Table of Contents	1
Editorial Board	1