Molecular Pharmacology

Article	Citations
Does COVID19 Infect the Brain? If So, Smokers Might Be at a Higher Risk	93
Five Decades of Research on Opioid Peptides: Current Knowledge and Unanswered Questions	84
Notch1 in Cancer Therapy: Possible Clinical Implications and Challenges	57
Intrinsic Efficacy of Opioid Ligands and Its Importance for Apparent Bias, Operational Analysis, and Therapeutic Window	49
Arrestin-Dependent and -Independent Internalization of G Protein–Coupled Receptors: Methods, Mechanisms, and Implications on Cell Signaling	42
Inhibition of Brain Epidermal Growth Factor Receptor Activation: A Novel Target in Neurodegenerative Diseases and Brain Injuries	39
Metabotropic Glutamate Receptors As Emerging Targets for the Treatment of Schizophrenia	36
Heparin-binding Peptides as Novel Therapies to Stop SARS-CoV-2 Cellular Entry and Infection	31
Remdesivir and EIDD-1931 Interact with Human Equilibrative Nucleoside Transporters 1 and 2: Implications for Reaching SARS-CoV-2 Viral Sanctuary Sites	31
β-Arrestin–Biased Allosteric Modulator Potentiates Carvedilol-Stimulated β Adrenergic Receptor Cardioprotection	24
Molecular Pharmacology of NRH:Quinone Oxidoreductase 2: A Detoxifying Enzyme Acting as an Undercover Toxifying Enzyme	23
Protective Effects of Flavonoids in Acute Models of Light-Induced Retinal Degeneration	21
MicroRNA-1291-5p Sensitizes Pancreatic Carcinoma Cells to Arginine Deprivation and Chemotherapy through the Regulation of Arginolysis and Glycolysis	21
5-Hydroxymethyl-Furfural and Structurally Related Compounds Block the Ion Conductance in Human Aquaporin-1 Channels and Slow Cancer Cell Migration and Invasion	21
Functions of the CXCL12 Receptor ACKR3/CXCR7—What Has Been Perceived and What Has Been Overlooked	19
Characterization of Meta-Iodobenzylguanidine (mIBG) Transport by Polyspecific Organic Cation Transporters: Implication for mIBG Therapy	18
Unique Positive Cooperativity Between the β-Arrestin–Biased β-Blocker Carvedilol and a Small Molecule Positive Allosteric Modulator of the β2-Adrenergic Receptor	18
Eribulin Activates the cGAS-STING Pathway via the Cytoplasmic Accumulation of Mitochondrial DNA	17
Metformin Prevents Hyperglycemia-Associated, Oxidative Stress-Induced Vascular Endothelial Dysfunction: Essential Role for the Orphan Nuclear Receptor Human Nuclear Receptor 4A1 (Nur77)	17
The Structure-Function Relationship of Angular Estrogens and Estrogen Receptor Alpha to Initiate Estrogen-Induced Apoptosis in Breast Cancer Cells	17
Regulators of G Protein Signaling in Analgesia and Addiction	17
GZD824 Inhibits GCN2 and Sensitizes Cancer Cells to Amino Acid Starvation Stress	17
GS-967 and Eleclazine Block Sodium Channels in Human Induced Pluripotent Stem Cell–Derived Cardiomyocytes	17
Targeting Angiotensin-Converting Enzyme-2/Angiotensin-(1-7)/Mas Receptor Axis in the Vascular Progenitor Cells for Cardiovascular Diseases	17
mTOR Regulation of AGC Kinases: New Twist to an Old Tail	16

Chronic Treatment with Morphine Disrupts Acute Kinase-Dependent Desensitization of GPCRs	16
Pharmacology and Molecular Mechanisms of Clinically Relevant Estrogen Estetrol and Estrogen Mimic BMI-135 for the Treatment of Endocrine-Resistant Breast Cancer	16
The Tails of Protein Kinase A	16
Atomic-Level Characterization of the Methadone-Stabilized Active Conformation of µ-Opioid Receptor	15
Berberine Represses β-Catenin Translation Involving 4E-BPs in Hepatocellular Carcinoma Cells	15
Pharmacological Characterization of the Imipridone Anticancer Drug ONC201 Reveals a Negative Allosteric Mechanism of Action at the D2Dopamine Receptor	15
Characterization of Vixotrigine, a Broad-Spectrum Voltage-Gated Sodium Channel Blocker	15
Phosphoproteomic Identification of Vasopressin/cAMP/Protein Kinase A–Dependent Signaling in Kidney	15
Mechanism-Based Inactivation of Cytochrome P450 3A4 by Benzbromarone	14
Predicting Drug Interactions with Human Equilibrative Nucleoside Transporters 1 and 2 Using Functional Knockout Cell Lines and Bayesian Modeling	14
Targeting VGLUT Machinery: Implications on mGluR5 Signaling and Behavior	14
A Truncated Six Transmembrane Splice Variant MOR-1G Enhances Expression of the Full-Length Seven Transmembrane μ-Opioid Receptor through Heterodimerization	14
TMEM16A Ca2+-Activated Cl- Channel Regulates the Proliferation and Migration of Brain Capillary Endothelial Cells	14
Senolytic-Mediated Elimination of Head and Neck Tumor Cells Induced Into Senescence by Cisplatin	13
GPR83 Engages Endogenous Peptides from Two Distinct Precursors to Elicit Differential Signaling	13
Kinetic Analysis of the Early Signaling Steps of the Human Chemokine Receptor CXCR4	13
Ligand-Independent G Protein–Coupled Estrogen Receptor/G Protein–Coupled Receptor 30 Activity: Lack of Receptor-Dependent Effects of G-1 and 17β-Estradiol	13
Organic Anion Transporting Polypeptide–Mediated Hepatic Uptake of Glucuronide Metabolites of Androgens	13
Acylation of the Incretin Peptide Exendin-4 Directly Impacts Glucagon-Like Peptide-1 Receptor Signaling and Trafficking	13
MicroRNA hsa-miR-1301-3p Regulates Human ADH6, ALDH5A1 and ALDH8A1 in the Ethanol-Acetaldehyde-Acetate Metabolic Pathway	13
Structural Basis of the Negative Allosteric Modulation of 5-BDBD at Human P2X4 Receptors	12
Emerging Roles for Regulator of G Protein Signaling 2 in (Patho)physiology	12
Differing Activity Profiles of the Stereoisomers of 2,3,5,6TMP-TQS, a Putative Silent Allosteric Modulator of α7 nAChR	12
Hydroxynorketamine Blocks N-Methyl-d-Aspartate Receptor Currents by Binding to Closed Receptors	11
Functional impact of the G279S substitution in the adenosine A1-receptor (A1R-G279S), a mutation associated with Parkinson's disease	11
Dysregulation of Angiotensin Converting Enzyme 2 Expression and Function in Comorbid Disease Conditions Possibly Contributes to Coronavirus Infectious Disease 2019 Complication Severity	11
Detailed In Vitro Pharmacological Characterization of Clinically Tested Negative Allosteric Modulators of the Metabotropic Glutamate Receptor 5	11
Regulation of Kappa Opioid Receptor Inactivation Depends on Sex and Cellular Site of Antagonist Action	11
Structure of Cytochrome P450 2C9*2 in Complex with Losartan: Insights into the Effect of Genetic Polymorphism	11
Membrane-Mediated Activity of Local Anesthetics	11
An Updated Review on Implications of Autophagy and Apoptosis in Tumorigenesis: Possible Alterations in Autophagy through Engineered Nanomaterials and Their Importance in Cancer Therapy	11
Arginine-259 of UGT2B7 Confers UDP-Sugar Selectivity	11
Transient Receptor Potential Ankyrin-1 and Vanilloid-3 Differentially Regulate Endoplasmic Reticulum Stress and Cytotoxicity in Human Lung Epithelial Cells After Pneumotoxic Wood Smoke Particle Exposu	10
Macrophage-Inducible C-Type Lectin Signaling Exacerbates Acetaminophen-Induced Liver Injury by Promoting Kupffer Cell Activation in Mice	10
Neprilysin Controls the Synaptic Activity of Neuropeptides in the Intercalated Cells of the Amygdala	10
Short-Term Acyl-CoA:Cholesterol Acyltransferase Inhibition, Combined with Apoprotein A1 Overexpression, Promotes Atherosclerosis Inflammation Resolution in Mice	10
LUF7244 plus Dofetilide Rescues Aberrant Kv11.1 Trafficking and Produces Functional IKv11.1	10
Nicotinic Acetylcholine Receptor Accessory Subunits Determine the Activity Profile of Epibatidine Derivatives	10
Allosterically Potentiated α7 Nicotinic Acetylcholine Receptors: Reduced Calcium Permeability and Current-Independent Control of Intracellular Calcium	10
Novel c-Myc–Targeting Compound N, N-Bis (5-Ethyl-2-Hydroxybenzyl) Methylamine for Mediated c-Myc Ubiquitin-Proteasomal Degradation in Lung Cancer Cells	10
Spinal Opioid Tolerance Depends upon Platelet-Derived Growth Factor Receptor-β Signaling, Not μ-Opioid Receptor Internalization	9
The Sulfated Steroids Pregnenolone Sulfate and Dehydroepiandrosterone Sulfate Inhibit the α1β3γ2L GABAA Receptor by Stabilizing a Novel Nonconducting State	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
CRISPR/Cas9 Genome Editing of the Human Topoisomerase IIαIntron 19 5′ Splice Site Circumvents Etoposide Resistance in Human Leukemia K562 Cells	9
Pain, Motivation, Migraine, and the Microbiome: New Frontiers for Opioid Systems and Disease	9
Intrasubunit and intersubunit steroid binding sites independently and additively mediate α1β2γ2L GABAA receptor potentiation by the endogenous neurosteroid allopregnanolone	9
Fluorizoline Blocks the Interaction between Prohibitin-2 and γ-Glutamylcyclotransferase and Induces p21Waf1/Cip1 Expression in MCF7 Breast Cancer Cells	9
Tubulin-Binding 3,5-Bis(styryl)pyrazoles as Lead Compounds for the Treatment of Castration-Resistant Prostate Cancer	9
Discovery of Novel Activators of Large-Conductance Calcium-Activated Potassium Channels for the Treatment of Cerebellar Ataxia	9
Drug-Drug Interaction between Metformin and Sorafenib Alters Antitumor Effect in Hepatocellular Carcinoma Cells	9

Identification of Celecoxib-Targeted Proteins Using Label-Free Thermal Proteome Profiling on Rat Hippocampus	9
The Negative Allosteric Modulator EU1794-4 Reduces Single-Channel Conductance and Ca2+ Permeability of GluN1/GluN2A N-Methyl-d-Aspartate Receptors	9
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
Molecular Mechanisms for the Inflammation-Resolving Actions of Lenabasum	9
Cysteine Modification by Ebselen Reduces the Stability and Cellular Levels of 14-3-3 Proteins	9
Insights into the Structure-Activity Relationship of Glycosides as Positive Allosteric Modulators Acting on P2X7 Receptors	8
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	8
CXL146, a Novel 4H-Chromene Derivative, Targets GRP78 to Selectively Eliminate Multidrug-Resistant Cancer Cells	8
The Emerging Role of Neuronal Organoid Models in Drug Discovery: Potential Applications and Hurdles to Implementation	8
Differential Reversible and Irreversible Interactions between Benzbromarone and Human Cytochrome P450s 3A4 and 3A5	8
Small Molecule Inhibitors Confirm Ubiquitin-Dependent Removal of TOP2-DNA Covalent Complexes	8
In Vitro Pharmacological Profile of KW-6356, a Novel Adenosine A2AReceptor Antagonist/Inverse Agonist	8
Functional Interaction between Transient Receptor Potential V4 Channel and Neuronal Calcium Sensor 1 and the Effects of Paclitaxel	8
Thermal Unfolding of the Human Serotonin Transporter: Differential Effect by Stabilizing and Destabilizing Mutations and Cholesterol on Thermodynamic and Kinetic Stability	8
Structural Basis for the Allosteric Inhibition of Hypoxia-Inducible Factor 2 by Belzutifan	8
The Heartwarming Effect of Brown Adipose Tissue	8
Decoding the Cardiac Actions of Protein Kinase D Isoforms	7
Transforming Growth Factor β1 Increases Expression of Contractile Genes in Human Pulmonary Arterial Smooth Muscle Cells by Potentiating Sphingosine-1-Phosphate Signaling	7
Calcium Cycling as a Mediator of Thermogenic Metabolism in Adipose Tissue	7
Lysine Demethylase 6B Regulates Prostate Cancer Cell Proliferation by Controlling c-MYC Expression	7
Antiepileptic Drug–Activated Constitutive Androstane Receptor Inhibits Peroxisome Proliferator–Activated Receptorαand Peroxisome Proliferator–Activated ReceptorγCoactivator 1α–Dep	7
Agonist-Specific Regulation of G Protein–Coupled Receptors after Chronic Opioid Treatment	7
Identification of Chemical and Pharmacological Chaperones for Correction of Trafficking-Deficient Mutant Cyclic Nucleotide–Gated A3 Channels	7
Multipathway In Vitro Pharmacological Characterization of Specialized Proresolving G Protein-Coupled Receptors	7
Structure of the Complex of an Iminopyridinedione Protein Tyrosine Phosphatase 4A3 Phosphatase Inhibitor with Human Serum Albumin	7
Antidepressants Produce Persistent Gαs-Associated Signaling Changes in Lipid Rafts after Drug Withdrawal	7
Arrestin Recruitment to C-C Chemokine Receptor 5: Potent C-C Chemokine Ligand 5 Analogs Reveal Differences in Dependence on Receptor Phosphorylation and Isoform-Specific Recruitment Bias	7
Biased Effect of Cardiotonic Steroids on Na/K-ATPase–Mediated Signal Transduction	7
ADP Ribosylation Factor 6 Promotes Contraction and Proliferation, Suppresses Apoptosis and Is Specifically Inhibited by NAV2729 in Prostate Stromal Cells	7
Identification of the Functional Binding Site for the Convulsant Tetramethylenedisulfotetramine in the Pore of the α2β3γ2 GABAA Recepto	7
Inhibition of Bitter Taste from Oral Tenofovir Alafenamide	7
Tyrosine nitration contributes to nitric oxide-stimulated degradation of CYP2B6	7
A Role for VCP/p97 in the Processing of Drug-Stabilized TOP2-DNA Covalent Complexes	7
Steroidal Antagonists of Progesterone- and Prostaglandin E1-Induced Activation of the Cation Channel of Sperm	7
Heteromeric Assembly of Truncated Neuronal Kv7 Channels: Implications for Neurologic Disease and Pharmacotherapy	7
VU6036720: The First Potent and Selective In Vitro Inhibitor of Heteromeric Kir4.1/5.1 Inward Rectifier Potassium Channels	7
Enhancement of muscimol binding and gating by allosteric modulators of the GABAA receptor: relating occupancy to state functions	7
Upacicalcet Is a Novel Secondary Hyperparathyroidism Drug that Targets the Amino Acid Binding Site of Calcium-Sensing Receptor	6
High-Throughput Screening of TRPV1 Ligands in the Light of the Bioluminescence Resonance Energy Transfer Technique	6
Multiplex G Protein–Coupled Receptor Screen Reveals Reliably Acting Agonists and a Gq-Phospholipase C Coupling Mode of GPR30/GPER1	6
Mechanisms to Repair Stalled Topoisomerase II-DNA Covalent Complexes	6
TP53 Null Mutations Identify Lung Cancer Cell Lines with Highest Sensitivity to the Nontaxane Microtubule Inhibitor Eribulin	6
Novel Small Molecule Fibroblast Growth Factor 23 Inhibitors Increase Serum Phosphate and Improve Skeletal Abnormalities in Hyp Mice	6
Roles of Receptor Phosphorylation and Rab Proteins in G Protein-Coupled Receptor Function and Trafficking	6
Regulation of Adrenergic, Serotonin, and Dopamine Receptors to Inhibit Diabetic Retinopathy: Monotherapies versus Combination Therapies	6
Unique Pharmacological Properties of the Kappa Opioid Receptor Signaling Through Gαz as Shown with Bioluminescence Resonance Energy Tranfer	6
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	6
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	6
Nelfinavir and Its Active Metabolite M8 Are Partial Agonists and Competitive Antagonists of the Human Pregnane X Receptor	6
Construction and Characterization of CRISPR/Cas9 Knockout Rat Model of Carboxylesterase 2a Gene	6
Novel Human-Derived RET Fusion NSCLC Cell Lines Have Heterogeneous Responses to RET Inhibitors and Differential Regulation of Downstream Signaling	6
A Recombinant Dimethylarginine Dimethylaminohydrolase-1–Based Biotherapeutics to Pharmacologically Lower Asymmetric Dimethyl Arginine, thus Improving Postischemic Cardiac Function and Cardiomyocyte Mi	6
Phenylalanine 193 in Extracellular Loop 2 of the β2-Adrenergic Receptor Coordinates β-Arrestin Interaction	6
Fentanyl-Induced Block of hERG Channels Is Exacerbated by Hypoxia, Hypokalemia, Alkalosis, and the Presence of hERG1b	6
Transcriptome-Level Interactions between Budesonide and Formoterol Provide Insight into the Mechanism of Action of Inhaled Corticosteroid/Long-Acting β2-Adrenoceptor Agonist Combinat	6
Small-Molecule Ligands that Bind the RET Receptor Activate Neuroprotective Signals Independent of but Modulated by Coreceptor GFRα1	6
Update on Angiotensin II Subtype 2 Receptor: Focus on Peptide and Nonpeptide Agonists	6
GABAA Receptors Expressed in Oligodendrocytes Cultured from the Neonatal Rat Contain α3 and γ1 Subunits and Present Differential Functional and Pharmacological Properties	6
Resveratrol Binds Nuclear Receptor 4A1 (NR4A1) and Acts as an NR4A1 Antagonist in Lung Cancer 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
Potential Use of Senolytics for Pharmacological Targeting of Precancerous Lesions	6
New Synthetic Caffeine Analogs as Modulators of the Cholinergic System	6
Weak Microbial Metabolites: a Treasure Trove for Using Biomimicry to Discover and Optimize Drugs	6
Ibrutinib Blocks YAP1 Activation and Reverses BRAF Inhibitor Resistance in Melanoma Cells	5
A20-Binding Inhibitor of Nuclear Factor-κB Targets β-Arrestin2 to Attenuate Opioid Tolerance	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
N-Terminal Targeting of Regulator of G Protein Signaling Protein 2 for F-Box Only Protein 44–Mediated Proteasomal Degradation	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
Phosphoproteomic Analysis as an Approach for Understanding Molecular Mechanisms of cAMP-Dependent Actions	5
A Novel Role of Uricosuric Agent Benzbromarone in BK Channel Activation and Reduction of Airway Smooth Muscle Contraction	5
Influence of the TARP γ8-Selective Negative Allosteric Modulator JNJ-55511118 on AMPA Receptor Gating and Channel Conductance	5
Naturally Occurring Mutations to Muscle-Type Creatine Kinase Impact Its Canonical and Pharmacological Activities in a Substrate-Dependent Manner In Vitro	5
Effects of Small Molecule Ligands on ACKR3 Receptors	5
Circular RNAs of UDP-Glycosyltransferase (UGT) Genes Expand the Complexity and Diversity of the UGT Transcriptome	5
The Emerging Structural Pharmacology of ATP-Sensitive Potassium Channels	5
Inhibition of Ligand-Gated TRPA1 by General Anesthetics	5
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	5
The Intracellular N-Terminal Domain of the Acid-Sensing Ion Channel 1a Participates in Channel Opening and Membrane Expression	5
Membrane-Facilitated Receptor Access and Binding Mechanisms of Long-Acting β2-Adrenergic Receptor Agonists	5
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	5

Positive Allosteric Modulators of Metabotropic Glutamate Receptor 5 as Tool Compounds to Study Signaling Bias	5
Decoding Cinnabarinic Acid–Specific Stanniocalcin 2 Induction by Aryl Hydrocarbon Receptor	5
Degraders: The Ultimate Weapon Against Amplified Driver Kinases in Cancer	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
A Benzodiazepine Ligand with Improved GABAA Receptor α5-Subunit Selectivity Driven by Interactions with Loop C	5
Thermal Proteome Profiling Reveals Glutathione Peroxidase 4 as the Target of the Autophagy Inducer Conophylline	4
Inhibition of Human Uracil DNA Glycosylase Sensitizes a Large Fraction of Colorectal Cancer Cells to 5-Fluorodeoxyuridine and Raltitrexed but Not Fluorouracil	4
Current Understanding of Membrane Transporters as Regulators or Targets for Cisplatin-Induced Hearing Loss	4
Therapeutic Neuroprotection by an Engineered Neurotrophin that Selectively Activates Tropomyosin Receptor Kinase (Trk) Family Neurotrophin Receptors but Not the p75 Neurotrophin Receptor	4
CCT and CCT-Like Modular Protein Interaction Domains in WNK Signaling	4
Influence of Tyrosine Kinase Inhibition on Organic Anion Transporting Polypeptide 1B3-Mediated Uptake	4
Opioid Research: Past and Future	4
Allosteric Modulator KM822 Attenuates Behavioral Actions of Amphetamine in Caenorhabditis elegans through Interactions with the Dopamine Transporter DAT-1	4
Hsp70:CHIP Ubiquitinates Dysfunctional but Not Native Neuronal NO Synthase	4
Ethnic-Related Sodium Voltage-Gated Channel α Subunit 5 Polymorphisms Shape the In Vitro Pharmacological Action of Amiodarone upon Nav1.5	4
Automated Intracellular Pharmacological Electrophysiology for Ligand-Gated Ionotropic Receptor and Pharmacology Screening	4
Mutual Cooperativity of Three Allosteric Sites on the Dopamine D1 Receptor	4
The Influence of Tobacco Smoke/Nicotine on CYP2A Expression in Human and African Green Monkey Lungs	4
Structural Refinement of the Tubulin Ligand (+)-Discodermolide to Attenuate Chemotherapy-Mediated Senescence	4
Live Tissue Imaging Reveals Distinct Transcellular Pathways for Organic Cations and Anions at the Blood-Cerebrospinal Fluid Barrier	4