Detail
Článek
Článek online
FT
Medvik - BMČ
  • Je něco špatně v tomto záznamu ?

Synthesis and biological evaluation of sphingosine kinase 2 inhibitors with anti-inflammatory activity

M. Vettorazzi, L. Vila, S. Lima, L. Acosta, F. Yépes, A. Palma, J. Cobo, J. Tengler, I. Malik, S. Alvarez, P. Marqués, N. Cabedo, MJ. Sanz, J. Jampilek, S. Spiegel, RD. Enriz,

. 2019 ; 352 (3) : e1800298. [pub] 20190116

Jazyk angličtina Země Německo

Typ dokumentu časopisecké články

Perzistentní odkaz   https://www.medvik.cz/link/bmc19027904

Grantová podpora
Universidad Nacional de San Luis
110265842651 Colombian Institute for Science and Research
CONICET-Argentina
APVV-0516-12 Slovak Research and Development Agency
SANOFI-AVENTIS Pharma Slovakia
SAF2014-57845R Spanish Ministry of Economy and Competiveness
SAF2017-89714-R Spanish Ministry of Economy and Competiveness
CP15/00150 Spanish Ministry of Economy and Competiveness
Carlos III Institute of Health (ISCIII)
European Regional Development Fund
Spanish Ministry of Innovation and Competitiveness

The synthesis of inhibitors of SphK2 with novel structural scaffolds is reported. These compounds were designed from a molecular modeling study, in which the molecular interactions stabilizing the different complexes were taken into account. Particularly interesting is that 7-bromo-2-(2-phenylethyl)-2,3,4,5-tetrahydro-1,4-epoxynaphtho[1,2-b]azepine, which is a selective inhibitor of SphK2, does not exert any cytotoxic effects and has a potent anti-inflammatory effect. It was found to inhibit mononuclear cell adhesion to the dysfunctional endothelium with minimal impact on neutrophil-endothelial cell interactions. The information obtained from our theoretical and experimental study can be useful in the search for inhibitors of SphK2 that play a prominent role in different diseases, especially in inflammatory and cardiovascular disorders.

Citace poskytuje Crossref.org

000      
00000naa a2200000 a 4500
001      
bmc19027904
003      
CZ-PrNML
005      
20190816104504.0
007      
ta
008      
190813s2019 gw f 000 0|eng||
009      
AR
024    7_
$a 10.1002/ardp.201800298 $2 doi
035    __
$a (PubMed)30648282
040    __
$a ABA008 $b cze $d ABA008 $e AACR2
041    0_
$a eng
044    __
$a gw
100    1_
$a Vettorazzi, Marcela $u Facultad de Química, Bioquímica y Farmacia, Universidad Nacional de San Luis, Instituto Multidisciplinario de Investigaciones Biológicas (IMIBIO-SL), San Luis, Argentina.
245    10
$a Synthesis and biological evaluation of sphingosine kinase 2 inhibitors with anti-inflammatory activity / $c M. Vettorazzi, L. Vila, S. Lima, L. Acosta, F. Yépes, A. Palma, J. Cobo, J. Tengler, I. Malik, S. Alvarez, P. Marqués, N. Cabedo, MJ. Sanz, J. Jampilek, S. Spiegel, RD. Enriz,
520    9_
$a The synthesis of inhibitors of SphK2 with novel structural scaffolds is reported. These compounds were designed from a molecular modeling study, in which the molecular interactions stabilizing the different complexes were taken into account. Particularly interesting is that 7-bromo-2-(2-phenylethyl)-2,3,4,5-tetrahydro-1,4-epoxynaphtho[1,2-b]azepine, which is a selective inhibitor of SphK2, does not exert any cytotoxic effects and has a potent anti-inflammatory effect. It was found to inhibit mononuclear cell adhesion to the dysfunctional endothelium with minimal impact on neutrophil-endothelial cell interactions. The information obtained from our theoretical and experimental study can be useful in the search for inhibitors of SphK2 that play a prominent role in different diseases, especially in inflammatory and cardiovascular disorders.
650    _2
$a antiflogistika $x chemická syntéza $x chemie $x farmakologie $x toxicita $7 D000893
650    _2
$a azepiny $x chemická syntéza $x chemie $x farmakologie $7 D001381
650    _2
$a buněčná adheze $x účinky léků $7 D002448
650    _2
$a viabilita buněk $x účinky léků $7 D002470
650    _2
$a racionální návrh léčiv $7 D015195
650    _2
$a cévní endotel $x účinky léků $x imunologie $7 D004730
650    _2
$a inhibitory enzymů $x chemická syntéza $x chemie $x farmakologie $x toxicita $7 D004791
650    _2
$a epoxidové sloučeniny $x chemická syntéza $x chemie $x farmakologie $7 D004852
650    _2
$a endoteliální buňky pupečníkové žíly (lidské) $7 D061307
650    _2
$a lidé $7 D006801
650    _2
$a simulace molekulového dockingu $7 D062105
650    _2
$a neutrofily $x účinky léků $x imunologie $7 D009504
650    _2
$a fosfotransferasy s alkoholovou skupinou jako akceptorem $x antagonisté a inhibitory $7 D017853
650    _2
$a vazba proteinů $7 D011485
650    _2
$a vztahy mezi strukturou a aktivitou $7 D013329
655    _2
$a časopisecké články $7 D016428
700    1_
$a Vila, Laura $u Department of Pharmacology, University of Valencia, Valencia, Spain. Institute of Health Research INCLIVA University Clinic Hospital of Valencia, Valencia, Spain.
700    1_
$a Lima, Santiago $u Department of Biology and Department of Biochemistry and Molecular Biology, Virginia Commonwealth University School of Medicine, Richmond, Virginia.
700    1_
$a Acosta, Lina $u Laboratorio de Síntesis Orgánica, Escuela de Química, Universidad Industrial de Santander, Bucaramanga, Colombia.
700    1_
$a Yépes, Felipe $u Laboratorio de Síntesis Orgánica, Escuela de Química, Universidad Industrial de Santander, Bucaramanga, Colombia.
700    1_
$a Palma, Alirio $u Laboratorio de Síntesis Orgánica, Escuela de Química, Universidad Industrial de Santander, Bucaramanga, Colombia.
700    1_
$a Cobo, Justo $u Inorganic and Organic Department, University of Jaén, Jaén, Spain.
700    1_
$a Tengler, Jan $u Medis International a.s., Bolatice, Czech Republic.
700    1_
$a Malik, Ivan $u Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Comenius University, Bratislava, Slovakia.
700    1_
$a Alvarez, Sergio $u Facultad de Química, Bioquímica y Farmacia, Universidad Nacional de San Luis, Instituto Multidisciplinario de Investigaciones Biológicas (IMIBIO-SL), San Luis, Argentina.
700    1_
$a Marqués, Patrice $u Department of Pharmacology, University of Valencia, Valencia, Spain. Institute of Health Research INCLIVA University Clinic Hospital of Valencia, Valencia, Spain.
700    1_
$a Cabedo, Nuria $u Department of Pharmacology, University of Valencia, Valencia, Spain. Institute of Health Research INCLIVA University Clinic Hospital of Valencia, Valencia, Spain.
700    1_
$a Sanz, María J $u Department of Pharmacology, University of Valencia, Valencia, Spain. Institute of Health Research INCLIVA University Clinic Hospital of Valencia, Valencia, Spain.
700    1_
$a Jampilek, Josef $u Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Comenius University, Bratislava, Slovakia.
700    1_
$a Spiegel, Sarah $u Department of Biology and Department of Biochemistry and Molecular Biology, Virginia Commonwealth University School of Medicine, Richmond, Virginia.
700    1_
$a Enriz, Ricardo D $u Facultad de Química, Bioquímica y Farmacia, Universidad Nacional de San Luis, Instituto Multidisciplinario de Investigaciones Biológicas (IMIBIO-SL), San Luis, Argentina.
773    0_
$w MED00000507 $t Archiv der Pharmazie $x 1521-4184 $g Roč. 352, č. 3 (2019), s. e1800298
856    41
$u https://pubmed.ncbi.nlm.nih.gov/30648282 $y Pubmed
910    __
$a ABA008 $b sig $c sign $y a $z 0
990    __
$a 20190813 $b ABA008
991    __
$a 20190816104734 $b ABA008
999    __
$a ok $b bmc $g 1433053 $s 1066364
BAS    __
$a 3
BAS    __
$a PreBMC
BMC    __
$a 2019 $b 352 $c 3 $d e1800298 $e 20190116 $i 1521-4184 $m Archiv der Pharmazie $n Arch Pharm $x MED00000507
GRA    __
$p Universidad Nacional de San Luis
GRA    __
$a 110265842651 $p Colombian Institute for Science and Research
GRA    __
$p CONICET-Argentina
GRA    __
$a APVV-0516-12 $p Slovak Research and Development Agency
GRA    __
$p SANOFI-AVENTIS Pharma Slovakia
GRA    __
$a SAF2014-57845R $p Spanish Ministry of Economy and Competiveness
GRA    __
$a SAF2017-89714-R $p Spanish Ministry of Economy and Competiveness
GRA    __
$a CP15/00150 $p Spanish Ministry of Economy and Competiveness
GRA    __
$p Carlos III Institute of Health (ISCIII)
GRA    __
$p European Regional Development Fund
GRA    __
$p Spanish Ministry of Innovation and Competitiveness
LZP    __
$a Pubmed-20190813

Najít záznam

Citační ukazatele

Možnosti archivace