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Results: 1 to 20 of 106

1.

Designing allosteric regulators of thrombin. Monosulfated benzofuran dimers selectively interact with Arg173 of exosite 2 to induce inhibition.

Abdel Aziz MH, Sidhu PS, Liang A, Kim JY, Mosier PD, Zhou Q, Farrell DH, Desai UR.

J Med Chem. 2012 Aug 9;55(15):6888-97. doi: 10.1021/jm300670q. Epub 2012 Jul 25.

PMID:
22788964
[PubMed - indexed for MEDLINE]
Free PMC Article
2.

Designing allosteric regulators of thrombin. Exosite 2 features multiple subsites that can be targeted by sulfated small molecules for inducing inhibition.

Sidhu PS, Abdel Aziz MH, Sarkar A, Mehta AY, Zhou Q, Desai UR.

J Med Chem. 2013 Jun 27;56(12):5059-70. doi: 10.1021/jm400369q. Epub 2013 Jun 13.

PMID:
23718540
[PubMed - indexed for MEDLINE]
Free PMC Article
3.

First steps in the direction of synthetic, allosteric, direct inhibitors of thrombin and factor Xa.

Verghese J, Liang A, Sidhu PP, Hindle M, Zhou Q, Desai UR.

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4126-9. doi: 10.1016/j.bmcl.2009.06.013. Epub 2009 Jun 6.

PMID:
19540113
[PubMed - indexed for MEDLINE]
Free PMC Article
4.

A novel allosteric pathway of thrombin inhibition: Exosite II mediated potent inhibition of thrombin by chemo-enzymatic, sulfated dehydropolymers of 4-hydroxycinnamic acids.

Henry BL, Monien BH, Bock PE, Desai UR.

J Biol Chem. 2007 Nov 2;282(44):31891-9. Epub 2007 Sep 5.

PMID:
17804413
[PubMed - indexed for MEDLINE]
Free PMC Article
5.

Fibrinogen gamma' chain binds thrombin exosite II.

Lovely RS, Moaddel M, Farrell DH.

J Thromb Haemost. 2003 Jan;1(1):124-31.

PMID:
12871549
[PubMed - indexed for MEDLINE]
6.

Rational design of potent, small, synthetic allosteric inhibitors of thrombin.

Sidhu PS, Liang A, Mehta AY, Abdel Aziz MH, Zhou Q, Desai UR.

J Med Chem. 2011 Aug 11;54(15):5522-31. doi: 10.1021/jm2005767. Epub 2011 Jul 18.

PMID:
21714536
[PubMed - indexed for MEDLINE]
Free PMC Article
7.

Designing allosteric inhibitors of factor XIa. Lessons from the interactions of sulfated pentagalloylglucopyranosides.

Al-Horani RA, Desai UR.

J Med Chem. 2014 Jun 12;57(11):4805-18. doi: 10.1021/jm500311e. Epub 2014 May 29.

PMID:
24844380
[PubMed - indexed for MEDLINE]
8.

Lysine-heparin interactions in antithrombin. Properties of K125M and K290M,K294M,K297M variants.

Fan B, Turko IV, Gettins PG.

Biochemistry. 1994 Nov 29;33(47):14156-61.

PMID:
7947827
[PubMed - indexed for MEDLINE]
9.

Long range communication between exosites 1 and 2 modulates thrombin function.

Petrera NS, Stafford AR, Leslie BA, Kretz CA, Fredenburgh JC, Weitz JI.

J Biol Chem. 2009 Sep 18;284(38):25620-9. doi: 10.1074/jbc.M109.000042. Epub 2009 Jul 9.

PMID:
19589779
[PubMed - indexed for MEDLINE]
Free PMC Article
11.

Molecular mapping of the thrombin-heparin cofactor II complex.

Fortenberry YM, Whinna HC, Gentry HR, Myles T, Leung LL, Church FC.

J Biol Chem. 2004 Oct 8;279(41):43237-44. Epub 2004 Aug 2.

PMID:
15292227
[PubMed - indexed for MEDLINE]
Free Article
12.

Allosteric inhibition of human factor XIa: discovery of monosulfated benzofurans as a class of promising inhibitors.

Argade MD, Mehta AY, Sarkar A, Desai UR.

J Med Chem. 2014 Apr 24;57(8):3559-69. doi: 10.1021/jm5002698. Epub 2014 Apr 7.

PMID:
24666186
[PubMed - indexed for MEDLINE]
13.

Profiling the structural determinants for the selectivity of representative factor-Xa and thrombin inhibitors using combined ligand-based and structure-based approaches.

Bhunia SS, Roy KK, Saxena AK.

J Chem Inf Model. 2011 Aug 22;51(8):1966-85. doi: 10.1021/ci200185q. Epub 2011 Aug 1.

PMID:
21761917
[PubMed - indexed for MEDLINE]
14.

Inhibition of a thrombin anion-binding exosite-2 mutant by the glycosaminoglycan-dependent serpins protein C inhibitor and heparin cofactor II.

Cooper ST, Rezaie AR, Esmon CT, Church FC.

Thromb Res. 2002 Jul 15;107(1-2):67-73.

PMID:
12413592
[PubMed - indexed for MEDLINE]
15.

Evidence that both exosites on thrombin participate in its high affinity interaction with fibrin.

Pospisil CH, Stafford AR, Fredenburgh JC, Weitz JI.

J Biol Chem. 2003 Jun 13;278(24):21584-91. Epub 2003 Apr 7.

PMID:
12682049
[PubMed - indexed for MEDLINE]
Free Article
16.

Heparin chain-length dependence of factor Xa inhibition by antithrombin in plasma.

Rezaie AR.

Thromb Res. 2007;119(4):481-8. Epub 2006 Mar 2.

PMID:
16515805
[PubMed - indexed for MEDLINE]
18.

Essential thrombin residues for inhibition by protein C inhibitor with the cofactors heparin and thrombomodulin.

Fortenberry YM, Whinna HC, Cooper ST, Myles T, Leung LL, Church FC.

J Thromb Haemost. 2007 Jul;5(7):1486-92.

PMID:
17635698
[PubMed - indexed for MEDLINE]
19.

Binding of exosite ligands to human thrombin. Re-evaluation of allosteric linkage between thrombin exosites I and II.

Verhamme IM, Olson ST, Tollefsen DM, Bock PE.

J Biol Chem. 2002 Mar 1;277(9):6788-98. Epub 2001 Nov 27.

PMID:
11724802
[PubMed - indexed for MEDLINE]
Free Article
20.

Molecular mapping of the heparin-binding exosite of thrombin.

Sheehan JP, Sadler JE.

Proc Natl Acad Sci U S A. 1994 Jun 7;91(12):5518-22.

PMID:
8202520
[PubMed - indexed for MEDLINE]
Free PMC Article

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