• Je něco špatně v tomto záznamu ?

In vitro modulatory effects of functionalized pyrimidines and piperidine derivatives on Aryl hydrocarbon receptor (AhR) and glucocorticoid receptor (GR) activities

M. Yar, L. Shahzadi, A. Farooq, S. Jalil Imran, JP. Cerón-Carrasco, H. den-Haan, S. Kumar, J. Peña-García, H. Pérez-Sánchez, A. Grycova, Z. Dvorak, R. Vrzal,

. 2017 ; 71 (-) : 285-293. [pub] 20170221

Jazyk angličtina Země Spojené státy americké

Typ dokumentu časopisecké články

Perzistentní odkaz   https://www.medvik.cz/link/bmc17023221

The development of biologically active molecules based on molecular recognition is an attractive and challenging task in medicinal chemistry and the molecules that can activate/deactivate certain receptors are of great medical interest. In this contribution, selected pyrimidine/piperidine derivatives were synthesized and tested for the ability to activate/deactivate Aryl hydrocarbon receptor (AhR) and Glucocorticoid receptor (GR). Tested compounds are shown to activate the receptors but to much lesser extent than positive controls, dioxin and dexamethasone for Ahr and GR, respectively. However, some of them antagonized the positive controls action. Although further in vivo studies are needed to fully characterize the bioactivities of these compounds, the reported in vitro evidences demonstrate that they might be used as the modulators of AhR and GR activities.

Citace poskytuje Crossref.org

000      
00000naa a2200000 a 4500
001      
bmc17023221
003      
CZ-PrNML
005      
20170828130514.0
007      
ta
008      
170720s2017 xxu f 000 0|eng||
009      
AR
024    7_
$a 10.1016/j.bioorg.2017.02.013 $2 doi
035    __
$a (PubMed)28267985
040    __
$a ABA008 $b cze $d ABA008 $e AACR2
041    0_
$a eng
044    __
$a xxu
100    1_
$a Yar, Muhammad $u Interdisciplinary Research Center in Biomedical Materials, COMSATS Institute of Information Technology, Lahore 54000, Pakistan. Electronic address: drmyar@ciitlahore.edu.pk.
245    10
$a In vitro modulatory effects of functionalized pyrimidines and piperidine derivatives on Aryl hydrocarbon receptor (AhR) and glucocorticoid receptor (GR) activities / $c M. Yar, L. Shahzadi, A. Farooq, S. Jalil Imran, JP. Cerón-Carrasco, H. den-Haan, S. Kumar, J. Peña-García, H. Pérez-Sánchez, A. Grycova, Z. Dvorak, R. Vrzal,
520    9_
$a The development of biologically active molecules based on molecular recognition is an attractive and challenging task in medicinal chemistry and the molecules that can activate/deactivate certain receptors are of great medical interest. In this contribution, selected pyrimidine/piperidine derivatives were synthesized and tested for the ability to activate/deactivate Aryl hydrocarbon receptor (AhR) and Glucocorticoid receptor (GR). Tested compounds are shown to activate the receptors but to much lesser extent than positive controls, dioxin and dexamethasone for Ahr and GR, respectively. However, some of them antagonized the positive controls action. Although further in vivo studies are needed to fully characterize the bioactivities of these compounds, the reported in vitro evidences demonstrate that they might be used as the modulators of AhR and GR activities.
650    _2
$a objevování léků $7 D055808
650    _2
$a HeLa buňky $7 D006367
650    _2
$a buňky Hep G2 $7 D056945
650    _2
$a lidé $7 D006801
650    _2
$a molekulární modely $7 D008958
650    _2
$a piperidiny $x chemie $x farmakologie $7 D010880
650    _2
$a pyrimidiny $x chemie $x farmakologie $7 D011743
650    _2
$a receptory aromatických uhlovodíků $x agonisté $x antagonisté a inhibitory $x metabolismus $7 D018336
650    _2
$a receptory glukokortikoidů $x agonisté $x antagonisté a inhibitory $x metabolismus $7 D011965
655    _2
$a časopisecké články $7 D016428
700    1_
$a Shahzadi, Lubna $u Interdisciplinary Research Center in Biomedical Materials, COMSATS Institute of Information Technology, Lahore 54000, Pakistan.
700    1_
$a Farooq, Ariba $u Interdisciplinary Research Center in Biomedical Materials, COMSATS Institute of Information Technology, Lahore 54000, Pakistan; Department of Chemistry, The Islamia University of Bahawalpur, Bahawalpur 63100, Pakistan.
700    1_
$a Jalil Imran, Saima $u Department of Cell Biology and Genetics, Palacky University, Olomouc, Czech Republic.
700    1_
$a Cerón-Carrasco, José P $u Bioinformatics and High Performance Computing Research Group (BIO-HPC), Universidad Católica San Antonio de Murcia (UCAM), 30107 Murcia, Spain.
700    1_
$a den-Haan, Helena $u Bioinformatics and High Performance Computing Research Group (BIO-HPC), Universidad Católica San Antonio de Murcia (UCAM), 30107 Murcia, Spain.
700    1_
$a Kumar, Sanjay $u Bioinformatics Centre, Biotech Park, Sector G, Jankipuram, Lucknow 226021, Uttar Pradesh, India.
700    1_
$a Peña-García, Jorge $u Bioinformatics and High Performance Computing Research Group (BIO-HPC), Universidad Católica San Antonio de Murcia (UCAM), 30107 Murcia, Spain.
700    1_
$a Pérez-Sánchez, Horacio $u Bioinformatics and High Performance Computing Research Group (BIO-HPC), Universidad Católica San Antonio de Murcia (UCAM), 30107 Murcia, Spain.
700    1_
$a Grycova, Aneta $u Department of Cell Biology and Genetics, Palacky University, Olomouc, Czech Republic.
700    1_
$a Dvorak, Zdenek $u Department of Cell Biology and Genetics, Palacky University, Olomouc, Czech Republic.
700    1_
$a Vrzal, Radim $u Department of Cell Biology and Genetics, Palacky University, Olomouc, Czech Republic. Electronic address: radim.vrzal@email.cz.
773    0_
$w MED00000771 $t Bioorganic chemistry $x 1090-2120 $g Roč. 71, č. - (2017), s. 285-293
856    41
$u https://pubmed.ncbi.nlm.nih.gov/28267985 $y Pubmed
910    __
$a ABA008 $b sig $c sign $y a $z 0
990    __
$a 20170720 $b ABA008
991    __
$a 20170828131100 $b ABA008
999    __
$a ok $b bmc $g 1238902 $s 984134
BAS    __
$a 3
BAS    __
$a PreBMC
BMC    __
$a 2017 $b 71 $c - $d 285-293 $e 20170221 $i 1090-2120 $m Bioorganic chemistry $n Bioorg Chem $x MED00000771
LZP    __
$a Pubmed-20170720

Najít záznam

Citační ukazatele

Pouze přihlášení uživatelé

Možnosti archivace