Did you know ? If you order before Friday 14h we deliver 90PCT of the the time next Tuesday, GENTAUR another in time delivery

Pubmed ID :29392954
Publication Date : //

Heparin and Heparan Sulfate Binding of the Antiparasitic Drug Imidocarb: Circular Dichroism Spectroscopy, Isothermal Titration Calorimetry, and Computational Studies.


This study is aimed to assess the binding interaction between the antiparasitic cationic drug imidocarb (IMD) and sulfated glycosaminoglycans (GAGs), the ubiquitious nonprotein macromolecules of living organisms. These complex, heterogeneous polyanions are the integral constituents of cell membranes and the extracellular matrix and display affinity toward basic compounds, the binding of which may affect their biological functions. Exciton-type circular dichroism (CD) spectroscopic features measured at low salt concentration verify the heparin and heparan sulfate binding of IMD, which occurs in a cooperative manner by association of several drug molecules to a disaccharide unit. Isothermal titration calorimetry (ITC) measurements reassured the heparin interaction, resulting in a K value in the low micromolar range. In contrast, when considering high molar excess of the heparin-binding sites, closer resembling in vivo conditions, an entirely different CD signature was induced, suggesting a shift from the oligo- to monomeric binding mode. This observation was also supported by ITC measurements using an identical sample setup. To better mimic in vivo conditions, several measurements were performed in physiological salt concentration ranges. On the basis of these, the inter- and intramolecular origin of CD activity observed under low- and high-salt conditions refer to electrostatically held oligomeric and intermolecular H-bonded monomeric drug-GAG adducts, respectively. To complement the experimental data, quantum chemical calculations were performed to assess the photophysical and conformational properties of IMD, indicating the existence of nonlinear, nonplanar interconverting conformer populations. Such a structural flexibility may be important in the multiple, cooperative binding of IMD to sterically adjacent GAG sites.

Authors : Zsila Ferenc , Juhász Tünde , Kohut Gergely , Beke-Somfai Tamás ,

Related products :

Catalog number Product name Quantity
30-524 Heparan sulfate proteoglycans (HSPGs) act as coreceptors for numerous heparin-binding growth factors and cytokines and are involved in cell signaling. Heparan sulfate 6-O-endosulfatases, such as SULF2 0.1 mg
26-392 Heparan sulfate proteoglycans (HSPGs) act as coreceptors for numerous heparin-binding growth factors and cytokines and are involved in cell signaling. Heparan sulfate 6-O-endosulfatases, such as SULF2 0.1 mg
AM01144PU-N Heparin _ Heparan Sulfate 0.1 mg
AM01144PU-N Heparin _ Heparan Sulfate 0.1 mg
GWB-C6D66D HEPARIN HEPARAN SULFATE, Antibody
DS-MB-01450 Mouse Anti-Heparin _ Heparan Sulfate 100
AM01144PU-N Heparin _ Heparan Sulfate Mouse IgG1 antibody Ab Purified 0.1 mg
'AM01144PU-N Heparin Heparan Sulfate IgG1 antibody Ab host: Mouse 0.1 mg
OBT1698 Heparin, Heparan Sulfate, Clone T320.11, Mab anti_Human; WB_EIA_RIA 100 µg.
28-712 Cell surface heparan sulfate proteoglycans are composed of a membrane-associated protein core substituted with a variable number of heparan sulfate chains. Members of the glypican-related integral mem 0.1 mg
DMABT-54795MH Mouse Anti Heparin per Heparan Sulfate Monoclonal Antibody 0.1 mg
DMABT-54795MH Mouse Anti Heparin Heparan Sulfate Monoclonal Antibody 0.1 mg
AM01144PU-N Heparin _ Heparan Sulfate Clone T320.11 antibody Isotype IgG1 Host Mouse 0.1 mg
EIAAB26688 Bifunctional heparan sulfate N-deacetylase_N-sulfotransferase 3,Glucosaminyl N-deacetylase_N-sulfotransferase 3,hNDST-3,Homo sapiens,HSST3,Human,NDST3,NDST-3,N-heparan sulfate sulfotransferase 3,N-HSS
EIAAB26685 Bifunctional heparan sulfate N-deacetylase_N-sulfotransferase 2,Glucosaminyl N-deacetylase_N-sulfotransferase 2,Homo sapiens,HSST2,Human,NDST2,NDST-2,N-heparan sulfate sulfotransferase 2,N-HSST 2
EIAAB26681 [Heparan sulfate]-glucosamine N-sulfotransferase 1,Bifunctional heparan sulfate N-deacetylase_N-sulfotransferase 1,Glucosaminyl N-deacetylase_N-sulfotransferase 1,HSNST 1,Hsst,Hsst1,Ndanst,Ndst1,NDST-
EIAAB26683 [Heparan sulfate]-glucosamine N-sulfotransferase 1,Bifunctional heparan sulfate N-deacetylase_N-sulfotransferase 1,Glucosaminyl N-deacetylase_N-sulfotransferase 1,Homo sapiens,HSNST 1,HSST,HSST1,Human
EIAAB26686 Bifunctional heparan sulfate N-deacetylase_N-sulfotransferase 2,Glucosaminyl N-deacetylase_N-sulfotransferase 2,Hsst2,Mndns,Mouse,Mus musculus,Ndst2,NDST-2,N-heparan sulfate sulfotransferase 2,N-HSST
EIAAB26690 Bifunctional heparan sulfate N-deacetylase_N-sulfotransferase 4,Glucosaminyl N-deacetylase_N-sulfotransferase 4,Homo sapiens,HSST4,Human,NDST4,NDST-4,N-heparan sulfate sulfotransferase 4,N-HSST 4
EIAAB26687 Bifunctional heparan sulfate N-deacetylase_N-sulfotransferase 3,Glucosaminyl N-deacetylase_N-sulfotransferase 3,Hsst3,Mouse,Mus musculus,Ndst3,NDST-3,N-heparan sulfate sulfotransferase 3,N-HSST 3
EIAAB26682 [Heparan sulfate]-glucosamine N-sulfotransferase 1,Bifunctional heparan sulfate N-deacetylase_N-sulfotransferase 1,Glucosaminyl N-deacetylase_N-sulfotransferase 1,HSNST 1,Mouse,Mus musculus,Ndst1,NDST
EIAAB26689 Bifunctional heparan sulfate N-deacetylase_N-sulfotransferase 4,Glucosaminyl N-deacetylase_N-sulfotransferase 4,Hsst4,Mouse,Mus musculus,Ndst4,NDST-4,N-heparan sulfate sulfotransferase 4,N-HSST 4
E1309h ELISA HBBM,HB-GAM,HBGF-8,HBNF1,HBNF-1,Heparin-binding brain mitogen,Heparin-binding growth factor 8,Heparin-binding growth-associated molecule,Heparin-binding neurite outgrowth-promoting factor 1,Homo 96T
U1309h CLIA HBBM,HB-GAM,HBGF-8,HBNF1,HBNF-1,Heparin-binding brain mitogen,Heparin-binding growth factor 8,Heparin-binding growth-associated molecule,Heparin-binding neurite outgrowth-promoting factor 1,Homo 96T
E1309b ELISA Bos taurus,Bovine,HBBM,HB-GAM,HBGF-8,Heparin-binding brain mitogen,Heparin-binding growth factor 8,Heparin-binding growth-associated molecule,Heparin-binding neurite-promoting factor,p18,Pleiotr 96T


 

GENTAUR Belgium BVBA BE0473327336
Voortstraat 49, 1910 Kampenhout BELGIUM
Tel 0032 16 58 90 45

Fax 0032 16 50 90 45
info@gentaur.com | Gentaur





GENTAUR Ltd.
Howard Frank Turnberry House
1404-1410 High Road
Whetstone London N20 9BH
Tel 020 3393 8531 Fax 020 8445 9411
uk@gentaur.com | Gentaur

 

 




GENTAUR France SARL
9, rue Lagrange, 75005 Paris
Tel 01 43 25 01 50

Fax 01 43 25 01 60
RCS Paris B 484 237 888

SIRET 48423788800017

BNP PARIBAS PARIS PL MAUBERT BIC BNPAFRPPPRG

france@gentaur.com | Gentaur

GENTAUR GmbH
Marienbongard 20
52062 Aachen Deutschland
Support Karolina Elandt
Tel: 0035929830070
Fax: (+49) 241 56 00 47 88

Logistic :0241 40 08 90 86
Bankleitzahl 39050000
IBAN lautet DE8839050000107569353
Handelsregister Aachen HR B 16058
Umsatzsteuer-Identifikationsnummer *** DE 815175831
Steuernummer 201/5961/3925
de@gentaur.com | Gentaur

GENTAUR U.S.A
Genprice Inc, Logistics
547, Yurok Circle
San Jose, CA 95123
CA 95123
Tel (408) 780-0908,
Fax (408) 780-0908,
sales@genprice.com

Genprice Inc, Invoices and accounting
6017 Snell Ave, Ste 357
San Jose, CA 95123




GENTAUR Nederland BV
NL850396268B01 KVK nummer 52327027
Kuiper 1
5521 DG Eersel Nederland
Tel:  0208-080893  Fax: 0497-517897
nl@gentaur.com | Gentaur
IBAN: NL04 RABO 0156 9854 62   SWIFT RABONL2U






GENTAUR Spain
tel:0911876558
spain@gentaur.com | Gentaur






ГЕНТАУЪР БЪЛГАРИЯ
ID # 201 358 931 /BULSTAT
София 1000, ул. "Граф Игнатиев" 53 вх. В, ет. 2
Tel 0035924682280 Fax 0035924808322
e-mail: Sofia@gentaur.com | Gentaur
IBAN: BG11FINV91501014771636
BIC: FINVBGSF

GENTAUR Poland Sp. z o.o.


ul. Grunwaldzka 88/A m.2
81-771 Sopot, Poland
TEL Gdansk 058 710 33 44 FAX  058 710 33 48              

poland@gentaur.com | Gentaur

Other countries

Österreich +43720880899

Canada Montreal +15149077481

Ceská republika Praha +420246019719

Danmark +4569918806

Finland Helsset +358942419041

Magyarország Budapest +3619980547

Ireland Dublin+35316526556

Luxembourg+35220880274

Norge Oslo+4721031366

Sverige Stockholm+46852503438

Schweiz Züri+41435006251

US New York+17185132983

GENTAUR Italy
SRL IVA IT03841300167
Piazza Giacomo Matteotti, 6
24122 Bergamo Tel 02 36 00 65 93
Fax 02 36 00 65 94
italia@gentaur.com | Gentaur