PDBsum entry 2y7x

Blood clotting

PDB id: 2y7x

Contents

Protein chains

235 a.a.

53 a.a.

Ligands

MZA

Metals

_MG

_CA

Waters ×245

PDB id:

2y7x

Name:

Blood clotting

Title:

The discovery of potent and long-acting oral factor xa inhibitors with tetrahydroisoquinoline and benzazepine p4 motifs

Structure:

Activated factor xa heavy chain. Chain: a. Synonym: coagulation factor x, stuart factor, stuart-prower factor. Other_details: disulphide linked to other chain. Factor x light chain. Chain: b. Fragment: activated desgla, residues 46-179. Synonym: coagulation factor x, stuart factor, stuart-prower factor. Other_details: disulphide linked to other chain

Source:

Homo sapiens. Human. Organism_taxid: 9606. Other_details: purchased from enzyme research labs. Isolated from human blood. Human blood

Resolution:

1.90Å R-factor: 0.188 R-free: 0.230

Authors:

N.S.Watson,C.Adams,D.Belton,D.Brown,C.L.Burns-Kurtis,L.Chaudry, C.Chan,M.A.Convery,D.E.Davies,A.M.Exall,J.D.Harling,W.R.Irving, S.Irvine,S.Kleanthous,I.M.Mclay,A.J.Pateman,A.N.Patikis,T.J.Roethka, S.Senger,G.J.Stelman,J.R.Toomey,R.I.West,C.Whittaker,P.Zhou, R.J.Young

Key ref:

N.S.Watson et al. (2011). The discovery of potent and long-acting oral factor Xa inhibitors with tetrahydroisoquinoline and benzazepine P4 motifs. Bioorg Med Chem Lett, 21, 1588-1592. PubMed id: 21349711

Date:

02-Feb-11 Release date: 16-Mar-11

Protein chain

P00742  (FA10_HUMAN) -  Coagulation factor X from Homo sapiens

Seq: 488 a.a.

Struc: 235 a.a.

Protein chain

P00742  (FA10_HUMAN) -  Coagulation factor X from Homo sapiens

Seq: 488 a.a.

Struc: 53 a.a.

Enzyme reactions

• Enzyme class: Chains A, B: E.C.3.4.21.6 - coagulation factor Xa.
• Reaction: Preferential cleavage: Arg-|-Thr and then Arg-|-Ile bonds in prothrombin to form thrombin.

Bioorg Med Chem Lett 21:1588-1592 (2011)

PubMed id: 21349711

The discovery of potent and long-acting oral factor Xa inhibitors with tetrahydroisoquinoline and benzazepine P4 motifs.

N.S.Watson, C.Adams, D.Belton, D.Brown, C.L.Burns-Kurtis, L.Chaudry, C.Chan, M.A.Convery, D.E.Davies, A.M.Exall, J.D.Harling, S.Irvine, W.R.Irving, S.Kleanthous, I.M.McLay, A.J.Pateman, A.N.Patikis, T.J.Roethke, S.Senger, G.J.Stelman, J.R.Toomey, R.I.West, C.Whittaker, P.Zhou, R.J.Young.

ABSTRACT

No abstract given.