Peptide Macrocycle Inhibitor of Coagulation Factor XII with Subnanomolar Affinity and High Target Selectivity
نویسندگان
چکیده
منابع مشابه
Interactions of β-amyloid peptide with fibrinogen and coagulation factor XII may contribute to Alzheimer's disease.
PURPOSE OF REVIEW To review the evidence that the Alzheimer peptide β-amyloid interacts with the blood coagulation system and influences the pathophysiology of the disease. RECENT FINDINGS β-amyloid can interact with fibrinogen and blood coagulation factor XII and trigger ischemia and inflammation. SUMMARY β-amyloid interacts with fibrinogen and factor XII. These interactions can lead to in...
متن کاملCoagulation Factor XII Gene Mutation in Brazilian Families with Hereditary Angioedema with Normal C1 Inhibitor.
BACKGROUND Hereditary angioedema (HAE) with normal C1 inhibitor (C1-INH) is a rare disorder. Mutations of the gene encoding coagulation factor XII have been identified in a subset of patients with this condition. Our aim was to investigate mutations in the F12 gene in patients with HAE with normal C1-INH from Brazil. METHODS We studied 5 Brazilian families with index female patients who prese...
متن کاملCoagulation factor XII protease domain crystal structure
BACKGROUND Coagulation factor XII is a serine protease that is important for kinin generation and blood coagulation, cleaving the substrates plasma kallikrein and FXI. OBJECTIVE To investigate FXII zymogen activation and substrate recognition by determining the crystal structure of the FXII protease domain. METHODS AND RESULTS A series of recombinant FXII protease constructs were characteri...
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Factor XII (Hageman factor) is an important protease that plays a major role in the initiation of the intrinsic pathway of blood coagulation and fibrinolysis and kinin formation. It is still unclear whether factor XII deficiency causes any disorders during pregnancy. Because the main clinical feature in patients with factor XII deficiency is thrombosis rather than bleeding, low dose aspirin wou...
متن کاملThe Alzheimer's disease peptide β-amyloid promotes thrombin generation through activation of coagulation factor XII.
UNLABELLED Essentials How the Alzheimer's disease (AD) peptide β-amyloid (Aβ) disrupts neuronal function in the disease is unclear. Factor (F) XII initiates blood clotting via FXI, and thrombosis has been implicated in AD. Aβ triggers FXII-dependent FXI and thrombin activation, evidence of which is seen in AD plasma. Aβ-triggered clotting could contribute to neuronal dysfunction in AD and be a ...
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ژورنال
عنوان ژورنال: Journal of Medicinal Chemistry
سال: 2017
ISSN: 0022-2623,1520-4804
DOI: 10.1021/acs.jmedchem.6b01548