Abstract:
:We have discovered that phenyltriazolinone is a novel and potent P1 moiety for coagulation factor Xa. X-ray structures of the inhibitors with a phenyltriazolinone in the P1 position revealed that the side chain of Asp189 has reoriented resulting in a novel S1 binding pocket which is larger in size to accommodate the phenyltriazolinone P1 substrate.
journal_name
Bioorg Med Chem Lettjournal_title
Bioorganic & medicinal chemistry lettersauthors
Quan ML,Pinto DJ,Rossi KA,Sheriff S,Alexander RS,Amparo E,Kish K,Knabb RM,Luettgen JM,Morin P,Smallwood A,Woerner FJ,Wexler RRdoi
10.1016/j.bmcl.2010.01.011subject
Has Abstractpub_date
2010-02-15 00:00:00pages
1373-7issue
4eissn
0960-894Xissn
1464-3405pii
S0960-894X(10)00013-2journal_volume
20pub_type
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