Cerebrovascular dilation via selective targeting of the cholane steroid-recognition site in the BK channel β1-subunit by a novel nonsteroidal agent.

PubWeight™: 0.90‹?›

🔗 View Article (PMC 3629834)

Published in Mol Pharmacol on March 01, 2013

Authors

Anna N Bukiya1, Jacob E McMillan, Alexander L Fedinec, Shivaputra A Patil, Duane D Miller, Charles W Leffler, Abby L Parrill, Alex M Dopico

Author Affiliations

1: Departments of Pharmacology, University of Tennessee Health Science Center, Memphis, TN 38163, USA.

Articles citing this

Pharmacological consequences of the coexpression of BK channel α and auxiliary β subunits. Front Physiol (2014) 0.88

Bisphenol A activates BK channels through effects on α and β1 subunits. Channels (Austin) (2014) 0.83

Lipid regulation of BK channel function. Front Physiol (2014) 0.81

Both transmembrane domains of BK β1 subunits are essential to confer the normal phenotype of β1-containing BK channels. PLoS One (2014) 0.81

Modulation of BK Channel Function by Auxiliary Beta and Gamma Subunits. Int Rev Neurobiol (2016) 0.78

Dietary cholesterol protects against alcohol-induced cerebral artery constriction. Alcohol Clin Exp Res (2014) 0.78

Multi-generational pharmacophore modeling for ligands to the cholane steroid-recognition site in the β₁ modulatory subunit of the BKCa channel. J Mol Graph Model (2014) 0.75

Endothelial Nitric Oxide Mediates Caffeine Antagonism of Alcohol-Induced Cerebral Artery Constriction. J Pharmacol Exp Ther (2015) 0.75

Alcohol modulation of BK channel gating depends on β subunit composition. J Gen Physiol (2016) 0.75

Activation of calcium- and voltage-gated potassium channels of large conductance by leukotriene B4. J Biol Chem (2014) 0.75

BK channels in rat and human pulmonary smooth muscle cells are BKα-β1 functional complexes lacking the oxygen-sensitive stress axis regulated exon insert. Pulm Circ (2016) 0.75

Distinct mechanisms underlying cholesterol protection against alcohol-induced BK channel inhibition and resulting vasoconstriction. Biochim Biophys Acta (2016) 0.75

Articles cited by this

Vasoregulation by the beta1 subunit of the calcium-activated potassium channel. Nature (2000) 6.04

Viability thresholds and the penumbra of focal ischemia. Ann Neurol (1994) 4.49

High-conductance potassium channels of the SLO family. Nat Rev Neurosci (2006) 4.26

Regulation of arterial diameter and wall [Ca2+] in cerebral arteries of rat by membrane potential and intravascular pressure. J Physiol (1998) 4.16

Cloning and functional characterization of novel large conductance calcium-activated potassium channel beta subunits, hKCNMB3 and hKCNMB4. J Biol Chem (2000) 3.75

Functional role of the beta subunit of high conductance calcium-activated potassium channels. Neuron (1995) 3.75

Vitamin D receptor as an intestinal bile acid sensor. Science (2002) 3.64

Identification of membrane-type receptor for bile acids (M-BAR). Biochem Biophys Res Commun (2002) 3.41

Acute activation of Maxi-K channels (hSlo) by estradiol binding to the beta subunit. Science (1999) 3.05

A neuronal beta subunit (KCNMB4) makes the large conductance, voltage- and Ca2+-activated K+ channel resistant to charybdotoxin and iberiotoxin. Proc Natl Acad Sci U S A (2000) 2.95

New disguises for an old channel: MaxiK channel beta-subunits. News Physiol Sci (2002) 2.91

Mice with disrupted BK channel beta1 subunit gene feature abnormal Ca(2+) spark/STOC coupling and elevated blood pressure. Circ Res (2000) 2.76

Micromolar Ca(2+) from sparks activates Ca(2+)-sensitive K(+) channels in rat cerebral artery smooth muscle. Am J Physiol Cell Physiol (2001) 2.04

Ca2+ channels, ryanodine receptors and Ca(2+)-activated K+ channels: a functional unit for regulating arterial tone. Acta Physiol Scand (1998) 1.91

Heme is a carbon monoxide receptor for large-conductance Ca2+-activated K+ channels. Circ Res (2005) 1.80

Large-conductance, calcium-activated potassium channels: structural and functional implications. Pharmacol Ther (2005) 1.74

BK potassium channel modulation by leucine-rich repeat-containing proteins. Proc Natl Acad Sci U S A (2012) 1.71

Gain-of-function mutation in the KCNMB1 potassium channel subunit is associated with low prevalence of diastolic hypertension. J Clin Invest (2004) 1.70

Effect of pharmaceutical treatment on vasospasm, delayed cerebral ischemia, and clinical outcome in patients with aneurysmal subarachnoid hemorrhage: a systematic review and meta-analysis. J Cereb Blood Flow Metab (2011) 1.58

Activation of NFATc3 down-regulates the beta1 subunit of large conductance, calcium-activated K+ channels in arterial smooth muscle and contributes to hypertension. J Biol Chem (2006) 1.58

An activator of calcium-dependent potassium channels isolated from a medicinal herb. Biochemistry (1993) 1.55

Morphology of cerebral arteries. Pharmacol Ther (1995) 1.40

Bile acids induce Ca2+ release from both the endoplasmic reticulum and acidic intracellular calcium stores through activation of inositol trisphosphate receptors and ryanodine receptors. J Biol Chem (2006) 1.35

Beta1 (KCNMB1) subunits mediate lithocholate activation of large-conductance Ca2+-activated K+ channels and dilation in small, resistance-size arteries. Mol Pharmacol (2007) 1.34

Essential role for smooth muscle BK channels in alcohol-induced cerebrovascular constriction. Proc Natl Acad Sci U S A (2004) 1.29

Ethanol sensitivity of BK(Ca) channels from arterial smooth muscle does not require the presence of the beta 1-subunit. Am J Physiol Cell Physiol (2003) 1.27

Cytotoxic effects of dimethyl sulphoxide (DMSO) on cochlear organotypic cultures. Hear Res (2007) 1.21

Natural bile acids and synthetic analogues modulate large conductance Ca2+-activated K+ (BKCa) channel activity in smooth muscle cells. J Gen Physiol (2002) 1.20

Endothelial K(+) channel lacks the Ca(2+) sensitivity-regulating beta subunit. FASEB J (2000) 1.17

The KCNMB1 Glu65Lys polymorphism associates with reduced systolic and diastolic blood pressure in the Inter99 study of 5729 Danes. J Hypertens (2008) 1.13

The BK channel accessory beta1 subunit determines alcohol-induced cerebrovascular constriction. FEBS Lett (2009) 1.12

Modulation of the Ca(2+)-dependent K+ channel, hslo, by the substituted diphenylurea NS 1608, paxilline and internal Ca2+. Neuropharmacology (1996) 1.08

The second transmembrane domain of the large conductance, voltage- and calcium-gated potassium channel beta(1) subunit is a lithocholate sensor. FEBS Lett (2008) 1.06

Characteristics of reactive hyperemia in the cerebral circulation. Am J Physiol (1984) 1.06

Role of BK channels in hypertension and potassium secretion. Curr Opin Nephrol Hypertens (2011) 1.03

Channel beta2-4 subunits fail to substitute for beta1 in sensitizing BK channels to lithocholate. Biochem Biophys Res Commun (2009) 1.02

Bile acids as endogenous vasodilators? Biochem Pharmacol (1995) 1.02

Nuclear bile acid receptor FXR as pharmacological target: are we there yet? FEBS Lett (2006) 1.01

Voltage-sensitive oxonol dyes are novel large-conductance Ca2+-activated K+ channel activators selective for beta1 and beta4 but not for beta2 subunits. Mol Pharmacol (2007) 0.93

Regional, segmental, and temporal heterogeneity of cerebral vascular autoregulation. Ann Biomed Eng (1985) 0.93

Role of potassium channels in regulation of cerebral vascular tone. J Cereb Blood Flow Metab (1998) 0.92

Structural determinants of monohydroxylated bile acids to activate beta 1 subunit-containing BK channels. J Lipid Res (2008) 0.92

Plant anticancer agents, L. cytotoxic triterpenes from Sandoricum koetjape stems. J Nat Prod (1992) 0.91

A clinical review of cerebral vasospasm and delayed ischaemia following aneurysm rupture. Acta Neurochir Suppl (2011) 0.90

Estradiol binding to maxi-K channels induces their down-regulation via proteasomal degradation. J Biol Chem (2003) 0.89

The steroid interaction site in transmembrane domain 2 of the large conductance, voltage- and calcium-gated potassium (BK) channel accessory β1 subunit. Proc Natl Acad Sci U S A (2011) 0.89

Systematic review of reversible cerebral vasoconstriction syndrome. Expert Rev Cardiovasc Ther (2010) 0.88

Selective, direct activation of high-conductance, calcium-activated potassium channels causes smooth muscle relaxation. Mol Pharmacol (2012) 0.86

BK channels in cardiovascular disease: a complex story of channel dysregulation. Am J Physiol Heart Circ Physiol (2009) 0.85

Structure-activity relationships of a novel group of large-conductance Ca(2+)-activated K(+) (BK) channel modulators: the GoSlo-SR family. ChemMedChem (2012) 0.85

Posttraumatic vasospasm detected by continuous brain tissue oxygen monitoring: treatment with intraarterial verapamil and balloon angioplasty. Neurocrit Care (2008) 0.84

Transient splenial lesion after recovery of cerebral vasoconstriction and posterior reversible encephalopathy syndrome: a case report of eclampsia. Intern Med (2012) 0.83

Calcium- and voltage-gated potassium (BK) channel activators in the 5β-cholanic acid-3α-ol analogue series with modifications in the lateral chain. ChemMedChem (2012) 0.81

Biomarkers and vasospasm after aneurysmal subarachnoid hemorrhage. Neurosurg Clin N Am (2010) 0.81

Localization of a site of action for benzofuroindole-induced potentiation of BKCa channels. Mol Pharmacol (2012) 0.80

Identification of pentacyclic triterpenes derivatives as potent inhibitors against glycogen phosphorylase based on 3D-QSAR studies. Eur J Med Chem (2011) 0.78

Abrupt-onset severe headaches. Semin Neurol (2010) 0.77

New amido derivatives as potential BKCa potassium channel activators. XI. Eur J Med Chem (2007) 0.76

Articles by these authors

S1P1-selective in vivo-active agonists from high-throughput screening: off-the-shelf chemical probes of receptor interactions, signaling, and fate. Chem Biol (2005) 2.98

Structural basis for antagonism and resistance of bicalutamide in prostate cancer. Proc Natl Acad Sci U S A (2005) 2.89

Comparison of the pharmacological effects of a novel selective androgen receptor modulator, the 5alpha-reductase inhibitor finasteride, and the antiandrogen hydroxyflutamide in intact rats: new approach for benign prostate hyperplasia. Endocrinology (2004) 2.54

Status of PharmD/PhD programs in colleges of pharmacy: the University of Tennessee dual PharmD/PhD program. Am J Pharm Educ (2006) 2.35

Heme is a carbon monoxide receptor for large-conductance Ca2+-activated K+ channels. Circ Res (2005) 1.80

Pharmacodynamics of selective androgen receptor modulators. J Pharmacol Exp Ther (2003) 1.73

Key structural features of nonsteroidal ligands for binding and activation of the androgen receptor. Mol Pharmacol (2003) 1.65

Design, synthesis, and biological characterization of metabolically stable selective androgen receptor modulators. J Med Chem (2004) 1.64

Synthesis and antiproliferative activity of 2-aryl-4-oxo-thiazolidin-3-yl-amides for prostate cancer. Bioorg Med Chem Lett (2004) 1.57

Structural basis for accommodation of nonsteroidal ligands in the androgen receptor. J Biol Chem (2005) 1.54

Dual activity lysophosphatidic acid receptor pan-antagonist/autotaxin inhibitor reduces breast cancer cell migration in vitro and causes tumor regression in vivo. Cancer Res (2009) 1.54

Nox4 NADPH oxidase mediates oxidative stress and apoptosis caused by TNF-alpha in cerebral vascular endothelial cells. Am J Physiol Cell Physiol (2008) 1.53

An overview of tubulin inhibitors that interact with the colchicine binding site. Pharm Res (2012) 1.49

Molecular mechanisms of lysophosphatidic acid action. Prog Lipid Res (2003) 1.46

Compound 49b prevents diabetes-induced apoptosis through increased IGFBP-3 levels. Invest Ophthalmol Vis Sci (2012) 1.46

The lysophosphatidic acid type 2 receptor is required for protection against radiation-induced intestinal injury. Gastroenterology (2007) 1.42

Pharmacology, pharmacokinetics, and metabolism of acetothiolutamide, a novel nonsteroidal agonist for the androgen receptor. J Pharmacol Exp Ther (2003) 1.41

Synthesis, structure-activity relationships, and biological evaluation of fatty alcohol phosphates as lysophosphatidic acid receptor ligands, activators of PPARgamma, and inhibitors of autotaxin. J Med Chem (2005) 1.40

Nonsteroidal selective androgen receptor modulators enhance female sexual motivation. J Pharmacol Exp Ther (2010) 1.39

Novel nonsteroidal ligands with high binding affinity and potent functional activity for the androgen receptor. Eur J Med Chem (2002) 1.39

Glutamate induces oxidative stress and apoptosis in cerebral vascular endothelial cells: contributions of HO-1 and HO-2 to cytoprotection. Am J Physiol Cell Physiol (2005) 1.38

Carbon monoxide dilates cerebral arterioles by enhancing the coupling of Ca2+ sparks to Ca2+-activated K+ channels. Circ Res (2002) 1.38

GPRC6A mediates the non-genomic effects of steroids. J Biol Chem (2010) 1.38

A ligand-based approach to identify quantitative structure-activity relationships for the androgen receptor. J Med Chem (2004) 1.35

Carbon monoxide activates KCa channels in newborn arteriole smooth muscle cells by increasing apparent Ca2+ sensitivity of alpha-subunits. Am J Physiol Heart Circ Physiol (2003) 1.32

Unique ligand selectivity of the GPR92/LPA5 lysophosphatidate receptor indicates role in human platelet activation. J Biol Chem (2009) 1.27

Selective androgen receptor modulator treatment improves muscle strength and body composition and prevents bone loss in orchidectomized rats. Endocrinology (2005) 1.27

Discovery of 4-substituted methoxybenzoyl-aryl-thiazole as novel anticancer agents: synthesis, biological evaluation, and structure-activity relationships. J Med Chem (2009) 1.27

HO-2 provides endogenous protection against oxidative stress and apoptosis caused by TNF-alpha in cerebral vascular endothelial cells. Am J Physiol Cell Physiol (2006) 1.25

A selective androgen receptor modulator for hormonal male contraception. J Pharmacol Exp Ther (2004) 1.25

Emerging trends in oral delivery of peptide and protein drugs. Crit Rev Ther Drug Carrier Syst (2003) 1.25

Fatty alcohol phosphates are subtype-selective agonists and antagonists of lysophosphatidic acid receptors. Mol Pharmacol (2003) 1.25

Photo-conversion of two epimers (20R and 20S) of pregna-5,7-diene-3beta, 17alpha, 20-triol and their bioactivity in melanoma cells. Steroids (2008) 1.24

Phospholipase D2-dependent inhibition of the nuclear hormone receptor PPARgamma by cyclic phosphatidic acid. Mol Cell (2010) 1.23

Discovery of novel 2-aryl-4-benzoyl-imidazoles targeting the colchicines binding site in tubulin as potential anticancer agents. J Med Chem (2010) 1.21

Nonsteroidal selective androgen receptor modulators (SARMs): dissociating the anabolic and androgenic activities of the androgen receptor for therapeutic benefit. J Med Chem (2009) 1.20

Synthesis and pharmacological evaluation of second-generation phosphatidic acid derivatives as lysophosphatidic acid receptor ligands. Bioorg Med Chem Lett (2005) 1.19

Contributions of astrocytes and CO to pial arteriolar dilation to glutamate in newborn pigs. Am J Physiol Heart Circ Physiol (2006) 1.19

Identification of the hydrophobic ligand binding pocket of the S1P1 receptor. J Biol Chem (2006) 1.19

Lysophosphatidic acid induces prostate cancer PC3 cell migration via activation of LPA(1), p42 and p38alpha. Biochim Biophys Acta (2007) 1.18

Molecular basis for lysophosphatidic acid receptor antagonist selectivity. Biochim Biophys Acta (2002) 1.18

Assessment of cerebrovascular autoregulation: changes of highest modal frequency of cerebrovascular pressure transmission with cerebral perfusion pressure. Stroke (2004) 1.13

Novel branched poly(ethylenimine)-cholesterol water-soluble lipopolymers for gene delivery. Biomacromolecules (2002) 1.12

A comprehensive approach to faculty development. Am J Pharm Educ (2006) 1.11

Selective androgen receptor modulators in preclinical and clinical development. Nucl Recept Signal (2008) 1.11

Hydrogen sulfide and cerebral microvascular tone in newborn pigs. Am J Physiol Heart Circ Physiol (2010) 1.10

The para substituent of S-3-(phenoxy)-2-hydroxy-2-methyl-N-(4-nitro-3-trifluoromethyl-phenyl)-propionamides is a major structural determinant of in vivo disposition and activity of selective androgen receptor modulators. J Pharmacol Exp Ther (2005) 1.10

Synthesis and photo-conversion of androsta- and pregna-5,7-dienes to vitamin D3-like derivatives. Photochem Photobiol Sci (2008) 1.09

Design, synthesis, and SAR studies of 4-substituted methoxylbenzoyl-aryl-thiazoles analogues as potent and orally bioavailable anticancer agents. J Med Chem (2011) 1.09

Sphingosine 1-phosphate analogue recognition and selectivity at S1P4 within the endothelial differentiation gene family of receptors. Biochem J (2005) 1.07

Micellar delivery of bicalutamide and embelin for treating prostate cancer. Pharm Res (2009) 1.07

Cerebroprotective functions of HO-2. Curr Pharm Des (2008) 1.07

(S)-FTY720-vinylphosphonate, an analogue of the immunosuppressive agent FTY720, is a pan-antagonist of sphingosine 1-phosphate GPCR signaling and inhibits autotaxin activity. Cell Signal (2010) 1.07

Nitric oxide increases carbon monoxide production by piglet cerebral microvessels. Am J Physiol Heart Circ Physiol (2005) 1.05

Pharmacokinetic optimization of 4-substituted methoxybenzoyl-aryl-thiazole and 2-aryl-4-benzoyl-imidazole for improving oral bioavailability. Drug Metab Dispos (2011) 1.04

Role of cGMP in carbon monoxide-induced cerebral vasodilation in piglets. Am J Physiol Heart Circ Physiol (2004) 1.03

Steroidogenic enzyme AKR1C3 is a novel androgen receptor-selective coactivator that promotes prostate cancer growth. Clin Cancer Res (2013) 1.03

Nox4 NADPH oxidase-derived reactive oxygen species, via endogenous carbon monoxide, promote survival of brain endothelial cells during TNF-α-induced apoptosis. Am J Physiol Cell Physiol (2010) 1.02

Novel tubulin polymerization inhibitors overcome multidrug resistance and reduce melanoma lung metastasis. Pharm Res (2012) 1.02

Discovery of novel 2-aryl-4-benzoyl-imidazole (ABI-III) analogues targeting tubulin polymerization as antiproliferative agents. J Med Chem (2012) 1.02

Estrogen receptor-{beta}-selective ligands alleviate high-fat diet- and ovariectomy-induced obesity in mice. J Biol Chem (2010) 1.01

Specificity of cholesterol and analogs to modulate BK channels points to direct sterol-channel protein interactions. J Gen Physiol (2010) 1.01

Synthesis, in vitro structure-activity relationship, and in vivo studies of 2-arylthiazolidine-4-carboxylic acid amides as anticancer agents. Bioorg Med Chem (2009) 1.01

Controlling cancer through the autotaxin-lysophosphatidic acid receptor axis. Biochem Soc Trans (2012) 1.01

MicroRNAs are mediators of androgen action in prostate and muscle. PLoS One (2010) 1.01

Synthesis and photochemical transformation of 3β,21-dihydroxypregna-5,7-dien-20-one to novel secosteroids that show anti-melanoma activity. Steroids (2010) 1.01

Structural determinants of P-glycoprotein-mediated transport of glucocorticoids. Pharm Res (2003) 1.00

Hydrogen sulfide activates Ca²⁺ sparks to induce cerebral arteriole dilatation. J Physiol (2012) 1.00

Steroidal androgens and nonsteroidal, tissue-selective androgen receptor modulator, S-22, regulate androgen receptor function through distinct genomic and nongenomic signaling pathways. Mol Endocrinol (2008) 1.00

The permissive role of endothelial NO in CO-induced cerebrovascular dilation. Am J Physiol Heart Circ Physiol (2004) 0.99

Pharmacophore development and application toward the identification of novel, small-molecule autotaxin inhibitors. J Med Chem (2010) 0.99

Cerebroprotective effects of the CO-releasing molecule CORM-A1 against seizure-induced neonatal vascular injury. Am J Physiol Heart Circ Physiol (2007) 0.99

Astrocyte-derived CO is a diffusible messenger that mediates glutamate-induced cerebral arteriolar dilation by activating smooth muscle Cell KCa channels. Circ Res (2007) 0.99

Synthesis and antiproliferative activity of novel 2-aryl-4-benzoyl-imidazole derivatives targeting tubulin polymerization. Bioorg Med Chem (2011) 0.99

Role of carbon monoxide in glutamate receptor-induced dilation of newborn pig pial arterioles. Am J Physiol Heart Circ Physiol (2002) 0.98

Optimization of a pipemidic acid autotaxin inhibitor. J Med Chem (2010) 0.98

Age and species dependence of pial arteriolar responses to topical carbon monoxide in vivo. Exp Biol Med (Maywood) (2007) 0.98

Endogenous heme oxygenase prevents impairment of cerebral vascular functions caused by seizures. Am J Physiol Heart Circ Physiol (2003) 0.98

Structure-activity relationship studies of arylthiazolidine amides as selective cytotoxic agents for melanoma. Anticancer Res (2007) 0.97

Selective Androgen Receptor Modulator (SARM) treatment prevents bone loss and reduces body fat in ovariectomized rats. Pharm Res (2006) 0.97

Mode changes of cerebrovascular pressure transmission induced by cerebral vasodilation. J Neurotrauma (2007) 0.97

Recent and emerging anti-diabetes targets. Med Res Rev (2009) 0.97

In vitro and in vivo structure-activity relationships of novel androgen receptor ligands with multiple substituents in the B-ring. Endocrinology (2005) 0.97

Regulation of CO production in cerebral microvessels of newborn pigs. Am J Physiol Heart Circ Physiol (2003) 0.97

Hydrogen sulfide dilates cerebral arterioles by activating smooth muscle cell plasma membrane KATP channels. Am J Physiol Heart Circ Physiol (2011) 0.96

Crystal structure of the T877A human androgen receptor ligand-binding domain complexed to cyproterone acetate provides insight for ligand-induced conformational changes and structure-based drug design. J Biol Chem (2007) 0.96

Synthesis and antiproliferative activity of thiazolidine analogs for melanoma. Bioorg Med Chem Lett (2007) 0.96

Permissive contributions of NO and prostacyclin in CO-induced cerebrovascular dilation in piglets. Am J Physiol Heart Circ Physiol (2005) 0.96

Benzyl and naphthalene methylphosphonic acid inhibitors of autotaxin with anti-invasive and anti-metastatic activity. ChemMedChem (2011) 0.95

Novel vitamin D analogs as potential therapeutics: metabolism, toxicity profiling, and antiproliferative activity. Anticancer Res (2014) 0.95

Ionotropic glutamate receptors in cerebral microvascular endothelium are functionally linked to heme oxygenase. J Cereb Blood Flow Metab (2003) 0.95

Virtual screening for LPA2-specific agonists identifies a nonlipid compound with antiapoptotic actions. Mol Pharmacol (2012) 0.95