Drug-Targeted Genomes: Mutability of Ion Channels and GPCRs

Single‐pill combination of cilnidipine, an l‐/n‐type calcium channel blocker, and valsartan reduces the day‐by‐day variability of morning home systolic blood pressure in patients with treated hypertension: A sub‐analysis of the hope‐combi survey

(2021) Kazuomi Kario et al.   Journal of Clinical Hypertension

Epidemiologic Study of Cystic Fibrosis: 25 years of observational research

(2021) Michael W. Konstan et al.   PEDIATRIC PULMONOLOGY

Therapeutic potential of targeting G protein-gated inwardly rectifying potassium (GIRK) channels in the central nervous system

(2021) Danko Jeremic et al.   PHARMACOLOGY & THERAPEUTICS

A Novel Insecticidal Spider Peptide that Affects the Mammalian Voltage-Gated Ion Channel hKv1.5

(2021) Diana Alvarado et al.   Frontiers in Pharmacology

BOW-GBDT: A GBDT Classifier Combining With Artificial Neural Network for Identifying GPCR–Drug Interaction Based on Wordbook Learning From Sequences

(2021) Wangren Qiu et al.   Frontiers in Cell and Developmental Biology

Effects of electromagnetic fields on neuronal ion channels: a systematic review

(2021) Federico Bertagna et al.   ANNALS OF THE NEW YORK ACADEMY OF SCIENCES

Factors Associated with Mutations: Their Matching Rates to Cardiovascular and Neurological Diseases

(2021) Hannah B. Lucas et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Kinase drug discovery 20 years after imatinib: progress and future directions

(2021) Philip Cohen et al.   NATURE REVIEWS DRUG DISCOVERY

Evolving cryo-EM structural approaches for GPCR drug discovery

(2021) Xin Zhang et al.   STRUCTURE

Biased Allosteric Modulators: New Frontiers in GPCR Drug Discovery

(2021) Lauren M. Slosky et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Acid Sensing Ion Channel 2a Is Reduced in the Reduced Uterine Perfusion Pressure Mouse Model and Increases Seizure Susceptibility in Pregnant Mice

(2021) Maria Jones-Muhammad et al.   Cells

Association of cystic fibrosis transmembrane conductance regulator with epithelial sodium channel subunits carrying Liddle’s syndrome mutations

(2021) Arun K. Rooj et al.   AMERICAN JOURNAL OF PHYSIOLOGY-LUNG CELLULAR AND MOLECULAR PHYSIOLOGY

WHO essential medicines for children 2011–2019: age-appropriateness of enteral formulations

(2021) Ebiowei Samuel F Orubu et al.   ARCHIVES OF DISEASE IN CHILDHOOD

Kids and COVID: why young immune systems are still on top

(2021) Smriti Mallapaty   NATURE

Effectiveness of Covid-19 Vaccines against the B.1.617.2 (Delta) Variant

(2021) Jamie Lopez Bernal et al.   NEW ENGLAND JOURNAL OF MEDICINE

Skin concerns in patients with trisomy 21 (Down syndrome): A Mayo Clinic 22‐year retrospective review

(2021) Ashley B. Wentworth et al.   PEDIATRIC DERMATOLOGY

Trisomy 21-associated increases in chromosomal instability are unmasked by comparing isogenic trisomic/disomic leukocytes from people with mosaic Down syndrome

(2021) Kelly Rafferty et al.   PLoS One

Analysis of the intracellular traffic of IgG in the context of Down syndrome (trisomy 21)

(2021) R. B. Cejas et al.   Scientific Reports

Something Old, Something New: Ion Channel Blockers as Potential Anti-Tuberculosis Agents

(2021) Steven C. Mitini-Nkhoma et al.   Frontiers in Immunology

Germline GATA1s generating mutations predispose to leukemia with acquired trisomy 21 and Down syndrome-like phenotype

(2021) Henrik Hasle et al.   BLOOD

DNA-binding activities of compounds acting as enzyme inhibitors, ion channel blockers and receptor binders

(2021) Ruslans Muhamadejevs et al.   CHEMICO-BIOLOGICAL INTERACTIONS

Comments on “DNA-binding activities of compounds acting as enzyme inhibitors, ion channel blockers and receptor binders.”

(2021) Hartmut Jaeschke   CHEMICO-BIOLOGICAL INTERACTIONS

GPCR activation mechanisms across classes and macro/microscales

(2021) Alexander S. Hauser et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Reprogramming of a human induced pluripotent stem cell line from a long QT syndrome patient harboring a heterozygous mutation of c.1537C > T in SCN5A gene

(2021) Jianan Chen et al.   Stem Cell Research

Trisomy of Human Chromosome 21 Orthologs Mapping to Mouse Chromosome 10 Cause Age and Sex-Specific Learning Differences: Relevance to Down Syndrome

(2021) Ross Minter et al.   Genes

Phylum-Spanning Neuropeptide GPCR Identification and Prioritization: Shaping Drug Target Discovery Pipelines for Nematode Parasite Control

(2021) Louise E. Atkinson et al.   Frontiers in Endocrinology

COVID-19 in Children with Down Syndrome: Data from the Trisomy 21 Research Society Survey

(2021) David Emes et al.   Journal of Clinical Medicine

Multiple Organ Failure Associated with SARS-CoV-2 Infection in a Child with Down Syndrome: Is Trisomy 21 Associated with an Unfavourable Clinical Course?

(2021) Perla Idalia Vazquez-Hernández et al.   Case Reports in Pediatrics

Insights into sympathetic nervous system and GPCR interplay in fetal programming of hypertension: a bridge for new pharmacological strategies

(2020) Maria S. Vieira-Rocha et al.   DRUG DISCOVERY TODAY

Effects of Electrical Stimulation on hiPSC-CM Responses to Classic Ion Channel Blockers

(2020) Feng Wei et al.   TOXICOLOGICAL SCIENCES

Polymorphisms of the MTHFR gene in mothers of children with trisomy 21 (Down syndrome) in a Polish population

(2020) Paulina Czechowicz et al.   Advances in Clinical and Experimental Medicine

Identifying GPCR-drug interaction based on wordbook learning from sequences

(2020) Pu Wang et al.   BMC BIOINFORMATICS

Impact of GPCR Structures on Drug Discovery

(2020) Miles Congreve et al.   CELL

Constitutive Activation of RAS/MAPK Pathway Cooperates with Trisomy 21 and Is Therapeutically Exploitable in Down Syndrome B-cell Leukemia

(2020) Anouchka P. Laurent et al.   CLINICAL CANCER RESEARCH

A child with complementary mosaic trisomy 8 and mosaic trisomy 21; clinical description of Warkany-Down syndrome and mechanism of origin

(2020) Magda McGregor-Schuerman et al.   European Journal of Medical Genetics

Opportunities and challenges for drug discovery in modulating Adhesion G protein-coupled receptor (GPCR) functions

(2020) Andrey D. Bondarev et al.   Expert Opinion on Drug Discovery

Structure-Based Virtual Screening Accelerates GPCR Drug Discovery

(2020) Lei Liu et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Repositioning Lidocaine as an Anticancer Drug: The Role Beyond Anesthesia

(2020) Daipeng Zhou et al.   Frontiers in Cell and Developmental Biology

A Novel GPCR Target in correlation with Androgen Deprivation Therapy for Prostate Cancer Drug Discovery

(2020) Jing‐Yan Tian et al.   BASIC & CLINICAL PHARMACOLOGY & TOXICOLOGY

Mapping Systemic Inflammation and Antibody Responses in Multisystem Inflammatory Syndrome in Children (MIS-C)

(2020) Conor N. Gruber et al.   CELL

Purinergic Signaling: Impact of GPCR Structures on Rational Drug Design

(2020) Veronica Salmaso et al.   ChemMedChem

Releasing the technical ‘shackles’ on GPCR drug discovery: opportunities enabled by detergent-free polymer lipid particle (PoLiPa) purification

(2020) J. Daniel Hothersall et al.   DRUG DISCOVERY TODAY

Machine learning-based QSAR models to predict sodium ion channel (Nav 1.5) blockers

(2020) Noorain Khalifa et al.   Future Medicinal Chemistry

Effects of Selective Calcium Channel Blockers on Ions’ Permeation Through The Human Cav1.2 Ion Channel: A Computational Study

(2020) Farag.E.S. Mosa et al.   JOURNAL OF MOLECULAR GRAPHICS & MODELLING

Soluble ligands as drug targets

(2020) Misty M. Attwood et al.   NATURE REVIEWS DRUG DISCOVERY

TRPV4 antagonists ameliorate ventriculomegaly in a rat model of hydrocephalus

(2020) Alexandra E. Hochstetler et al.   JCI Insight

Location Bias as Emerging Paradigm in GPCR Biology and Drug Discovery

(2020) Mohammad Ali Mohammad Nezhady et al.   iScience

The ligand-gated ion channel P2X7 receptor mediates NLRP3/caspase-1-mediated pyroptosis in cerebral cortical neurons of juvenile rats with sepsis

(2020) Xuemei Sun et al.   BRAIN RESEARCH

Allosteric binding sites at the receptor–lipid bilayer interface: novel targets for GPCR drug discovery

(2020) Ying Wang et al.   DRUG DISCOVERY TODAY

Genes causing congenital hydrocephalus: Their chromosomal characteristics of telomere proximity and DNA compositions

(2020) Ian McKnight et al.   EXPERIMENTAL NEUROLOGY

Dual-Site Binding of Quaternary Ammonium Ions as Internal K+-Ion Channel Blockers: Nonclassical (C–H···O) H Bonding vs Dispersive (C–H···H–C) Interaction

(2020) Rinsha Cholasseri et al.   JOURNAL OF PHYSICAL CHEMISTRY B

Author Correction: Combinatorial expression of GPCR isoforms affects signalling and drug responses

(2020) Maria Marti-Solano et al.   NATURE

Generation of two human iPSC lines (UUIGPi013-A and UUIPGi014-A) from cases with Down syndrome and full trisomy for chromosome 21 (T21)

(2020) Jens Schuster et al.   Stem Cell Research

The Potential of 19F NMR Application in GPCR Biased Drug Discovery

(2020) Xudong Wang et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

An online resource for GPCR structure determination and analysis

(2019) Christian Munk et al.   NATURE METHODS

New Binding Sites, New Opportunities for GPCR Drug Discovery

(2019) H.C. Stephen Chan et al.   TRENDS IN BIOCHEMICAL SCIENCES

Hydrocephalus in a rat model of Meckel Gruber syndrome with a TMEM67 mutation

(2019) Joon W. Shim et al.   Scientific Reports

Advancing Chemokine GPCR Structure Based Drug Discovery

(2019) Suwen Zhao et al.   STRUCTURE

ANK2 functionally interacts with KCNH2 aggravating long QT syndrome in a double mutation carrier

(2019) Guido Gessner et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Assembly of a GPCR-G Protein Complex

(2019) Yang Du et al.   CELL

Monoamines and their derivatives on GPCRs: potential therapy for Alzheimer’s Disease

(2019) Eunice D. Farfan-Garcia et al.   Current Neuropharmacology

Advantages and shortcomings of cell-based electrical impedance measurements as a GPCR drug discovery tool

(2019) Jordi Doijen et al.   BIOSENSORS & BIOELECTRONICS

GPCRomics: An Approach to Discover GPCR Drug Targets

(2019) Paul A. Insel et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Partial trisomy 21 map: Ten cases further supporting the highly restricted Down syndrome critical region (HR-DSCR) on human chromosome 21

(2019) Maria Chiara Pelleri et al.   Molecular Genetics & Genomic Medicine

A central core disease mutation in the Ca2+-binding site of skeletal muscle ryanodine receptor impairs single-channel regulation

(2019) Venkat R. Chirasani et al.   AMERICAN JOURNAL OF PHYSIOLOGY-CELL PHYSIOLOGY

GPCR Drug Discovery: Emerging Targets, Novel Approaches and Future Trends

(2019) Jia Zhou et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Role of GPCR signaling and calcium dysregulation in Alzheimer's disease

(2019) Sushma et al.   MOLECULAR AND CELLULAR NEUROSCIENCE

Placental development and function in trisomy 21 and mouse models of Down syndrome: Clues for studying mechanisms underlying atypical development

(2019) April D. Adams et al.   PLACENTA

R534C mutation in hERG causes a trafficking defect in iPSC-derived cardiomyocytes from patients with type 2 long QT syndrome

(2019) Fernanda C. P. Mesquita et al.   Scientific Reports

Molecular Interactions between a Fluoride Ion Channel and Synthetic Protein Blockers

(2018) Daniel L. Turman et al.   BIOCHEMISTRY

GPCRs in pulmonary arterial hypertension: tipping the balance

(2018) Jean Iyinikkel et al.   BRITISH JOURNAL OF PHARMACOLOGY

The current state of GPCR-based drug discovery to treat metabolic disease

(2018) Kyle W Sloop et al.   BRITISH JOURNAL OF PHARMACOLOGY

Pharmacogenomics of GPCR Drug Targets

(2018) Alexander S. Hauser et al.   CELL

Somatic Mutations and Clonal Hematopoiesis

(2018) José J. Fuster et al.   CIRCULATION RESEARCH

The impact of mitotic errors on cell proliferation and tumorigenesis

(2018) Michelle S. Levine et al.   GENES & DEVELOPMENT

Ryanodine receptor Ca 2+ release channel post-translational modification: Central player in cardiac and skeletal muscle disease

(2018) Amanda Denniss et al.   INTERNATIONAL JOURNAL OF BIOCHEMISTRY & CELL BIOLOGY

Computer Simulations Reveal a Novel Blocking Mode of the hERG Ion Channel by the Antiarrhythmic Agent Clofilium

(2018) Daniel Șterbuleac et al.   Molecular Informatics

Cnidarian peptide neurotoxins: a new source of various ion channel modulators or blockers against central nervous systems disease

(2018) Qiwen Liao et al.   DRUG DISCOVERY TODAY

Controlling Ca2+ Permeable α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptors with Photochromic Ion Channel Blockers

(2018) Niels G. Nørager et al.   JOURNAL OF MEDICINAL CHEMISTRY

Application of human induced pluripotent stem cell-derived cardiomyocytes sheets with microelectrode array system to estimate antiarrhythmic properties of multi-ion channel blockers

(2018) Hiroko Izumi-Nakaseko et al.   JOURNAL OF PHARMACOLOGICAL SCIENCES

Importance of GPCR-Mediated Microglial Activation in Alzheimer’s Disease

(2018) Md. Ezazul Haque et al.   Frontiers in Cellular Neuroscience

Fluorescence-Based High Throughput Screening Technologies for Natural Chloride Ion Channel Blockers

(2018) Rong Xu et al.   CHEMICAL RESEARCH IN TOXICOLOGY

GPCR drug discovery: integrating solution NMR data with crystal and cryo-EM structures

(2018) Ichio Shimada et al.   NATURE REVIEWS DRUG DISCOVERY

The antiarrhythmic actions of bisaramil and penticainide result from mixed cardiac ion channel blockade

(2018) M.K. Pugsley et al.   BIOMEDICINE & PHARMACOTHERAPY

An overview of Ca2+mobilization assays in GPCR drug discovery

(2017) Qiang Ma et al.   Expert Opinion on Drug Discovery

Genotype-phenotype correlation for congenital heart disease in Down syndrome through analysis of partial trisomy 21 cases

(2017) Maria Chiara Pelleri et al.   GENOMICS

Down Syndrome, Partial Trisomy 21, and Absence of Alzheimer’s Disease: The Role of APP

(2017) Eric Doran et al.   JOURNAL OF ALZHEIMERS DISEASE

Functional selectivity of GPCR-directed drug action through location bias

(2017) Roshanak Irannejad et al.   Nature Chemical Biology

Trends in GPCR drug discovery: new agents, targets and indications

(2017) Alexander S. Hauser et al.   NATURE REVIEWS DRUG DISCOVERY

Knockdown of Myo-Inositol Transporter SMIT1 Normalizes Cholinergic and Glutamatergic Function in an Immortalized Cell Line Established from the Cerebral Cortex of a Trisomy 16 Fetal Mouse, an Animal Model of Human Trisomy 21 (Down Syndrome)

(2017) Ana María Cárdenas et al.   NEUROTOXICITY RESEARCH

Divalent ions are potential permeating blockers of the non-selective NaK ion channel: combined QM and MD based investigations

(2017) Biswajit Sadhu et al.   PHYSICAL CHEMISTRY CHEMICAL PHYSICS

Potential of GPCRs to modulate MAPK and mTOR pathways in Alzheimer’s disease

(2017) Rafael Franco et al.   PROGRESS IN NEUROBIOLOGY

The burden of trisomy 21 disrupts the proteostasis network in Down syndrome

(2017) Stefanos Aivazidis et al.   PLoS One

Glucose Deficiency Elevates Acid-Sensing Ion Channel 2a Expression and Increases Seizure Susceptibility in Temporal Lobe Epilepsy

(2017) Haitao Zhang et al.   Scientific Reports

Generation of improved human cerebral organoids from single copyDYRK1Aknockout induced pluripotent stem cells in trisomy 21: hypothetical solutions for neurodevelopmental models and therapeutic alternatives in down syndrome

(2016) E. Sacide Çağlayan   CELL BIOLOGY INTERNATIONAL

An antiarrhythmic agent as a promising lead compound for targeting the hEAG1 ion channel in cancer therapy: insights from molecular dynamics simulations

(2016) Daniel Șterbuleac et al.   Chemical Biology & Drug Design

Systematic reanalysis of partial trisomy 21 cases with or without Down syndrome suggests a small region on 21q22.13 as critical to the phenotype

(2016) Maria Chiara Pelleri et al.   HUMAN MOLECULAR GENETICS

GRK2 targeted knock-down results in spontaneous hypertension, and altered vascular GPCR signaling.

(2016) Elena Tutunea-Fatan et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

From CFTR biology toward combinatorial pharmacotherapy: expanded classification of cystic fibrosis mutations

(2016) Gudio Veit et al.   MOLECULAR BIOLOGY OF THE CELL

Partial trisomy of chromosome 21 without the Down syndrome phenotype

(2016) Mei-Tsz Su et al.   PRENATAL DIAGNOSIS

Ion channels find a pathway for therapeutic success: Table 1.

(2016) Maria L. Garcia et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

G Protein-Coupled Receptors (GPCRs) in Alzheimer’s Disease: A Focus on BACE1 Related GPCRs

(2016) Juan Zhao et al.   Frontiers in Aging Neuroscience

Therapeutic Approaches to Genetic Ion Channelopathies and Perspectives in Drug Discovery

(2016) Paola Imbrici et al.   Frontiers in Pharmacology

A cluster of protein kinases and phosphatases modulated in fetal Down syndrome (trisomy 21) brain

(2015) Rachel Weitzdoerfer et al.   AMINO ACIDS

Interaction of PEGylated anti-hypertensive drugs, amlodipine, atenolol and lisinopril with lipid bilayer membrane: A molecular dynamics simulation study

(2015) Abbas Yousefpour et al.   BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES

GPCR dimerization in brainstem nuclei contributes to the development of hypertension

(2015) Gwo-Ching Sun et al.   BRITISH JOURNAL OF PHARMACOLOGY

A multicenter, non-comparative study to evaluate the efficacy and safety of fixed-dose olmesartan/amlodipine in Korean patients with hypertension who are naïve or non-responders to anti-hypertensive monotherapy (ACE-HY study)

(2015) Hee-Won Jung et al.   CLINICAL AND EXPERIMENTAL HYPERTENSION

Fetal nasal bone hypoplasia in the second trimester: Comparison of diagnostic methods for predicting trisomy 21 (Down syndrome)

(2015) Recep Has et al.   JOURNAL OF CLINICAL ULTRASOUND

A global reference for human genetic variation

(2015) Richard A. Gibbs et al.   NATURE

The Incudomalleolar Articulation in Down Syndrome (Trisomy 21)

(2015) Christian Fausch et al.   OTOLOGY & NEUROTOLOGY

Disomy 21 in spermatozoa and the paternal origin of trisomy 21 Down syndrome

(2015) Erik Iwarsson et al.   Molecular Cytogenetics

Antiarrhythmic efficacy of CPUY102122, a multiple ion channel blocker, on rabbits with ischemia/reperfusion injury

(2014) Minhui Wang et al.   Pharmacological Reports

Differentially Expressed MicroRNAs in Maternal Plasma for the Noninvasive Prenatal Diagnosis of Down Syndrome (Trisomy 21)

(2014) Julian Kamhieh-Milz et al.   Biomed Research International

Maternal Germinal Trisomy 21 in Down Syndrome

(2014) Maj Hultén et al.   Journal of Clinical Medicine

Partial trisomy and tetrasomy of chromosome 21 without Down Syndrome phenotype and short overview of genotype-phenotype correlation. A case report

(2013) Pavlina Capkova et al.   BIOMEDICAL PAPERS-OLOMOUC

Modelling and rescuing neurodevelopmental defect of Down syndrome using induced pluripotent stem cells from monozygotic twins discordant for trisomy 21

(2013) Youssef Hibaoui et al.   EMBO Molecular Medicine

A patient with partial trisomy 21 and 7q deletion expresses mild Down syndrome phenotype

(2013) I. Papoulidis et al.   GENE

Octreotide-induced hepatitis in a child with persistent hyperinsulinemia hypoglycemia of infancy

(2013) Josef Ben-Ari et al.   JOURNAL OF PEDIATRIC ENDOCRINOLOGY & METABOLISM

Engineering a Potent and Specific Blocker of Voltage-Gated Potassium Channel Kv1.3, a Target for Autoimmune Diseases

(2012) Rong Chen et al.   BIOCHEMISTRY

Ion Channels as Therapeutic Targets: A Drug Discovery Perspective

(2012) Sharan K. Bagal et al.   JOURNAL OF MEDICINAL CHEMISTRY

Regulation of GPCR-mediated smooth muscle contraction: Implications for asthma and pulmonary hypertension

(2012) D.B. Wright et al.   PULMONARY PHARMACOLOGY & THERAPEUTICS

Hereditary hypophosphatemic rickets with hypercalciuria and nephrolithiasis-Identification of a novel SLC34A3/NaPi-IIc mutation

(2011) Priya Phulwani et al.   AMERICAN JOURNAL OF MEDICAL GENETICS PART A

Amlodipine and Loop Diuretics as the Second Anti-Hypertensive Medication for the Treatment of Hypertension with Chronic Kidney Diseases

(2011) Tsuneo Takenaka et al.   CLINICAL AND EXPERIMENTAL HYPERTENSION

Comparison of Daily Anti-Hypertensive Effects of Amlodipine and Nifedipine Coat-Core Using Ambulatory Blood Pressure Monitoring - Utility of“Hypobaric Curve”and“Hypobaric Area”

(2011) Keisuke Kuga et al.   CLINICAL AND EXPERIMENTAL HYPERTENSION

Regulation of GPCR signaling in Hypertension

(2010) Henriette L. Brinks et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR BASIS OF DISEASE

GPCR agonist-induced transactivation of the EGFR upregulates MLC II expression and promotes hypertension in insulin-resistant rats

(2010) Prabhakara Reddy Nagareddy et al.   CARDIOVASCULAR RESEARCH

Differential role of sodium channelsSCN1AandSCN2Agene polymorphisms with epilepsy and multiple drug resistance in the north Indian population

(2009) Ram Lakhan et al.   BRITISH JOURNAL OF CLINICAL PHARMACOLOGY

GPCR signalling in hypertension: role of GRKs

(2008) David M. Harris et al.   CLINICAL SCIENCE

Liddle??s syndrome caused by a novel missense mutation (P617L) of the epithelial sodium channel ?? subunit

(2008) Ermanno Rossi et al.   JOURNAL OF HYPERTENSION