Structures of soluble rabbit neprilysin complexed with phosphoramidon or thiorphan

Neutral endopeptidase (neprilysin; NEP) is a proteinase that cleaves a wide variety of peptides and has been implicated in Alzheimer's disease, cardiovascular conditions, arthritis and other inflammatory diseases. The structure of the soluble extracellular domain (residues 55 – 750) of rabbit neprilysin was solved both in its native form at 2.1   Å resolution, and bound to the inhibitors phosphoramidon and thiorphan at 2.8 and 3.0   Å resolution, respectively. Consistent with the extracellular domain of human neprilysin, the structure reveals a large central cavity which contains the active site and the location for inhibitor binding.
Source: Acta Crystallographica Section F - Category: Biochemistry Authors: Tags: neutral endopeptidase neprilysin phosphoramidon thiorphan research communications Source Type: research

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Source: Bioorganic and Medicinal Chemistry Letters - Category: Chemistry Authors: Tags: Bioorg Med Chem Lett Source Type: research
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Source: ClinicalTrials.gov - Category: Research Source Type: clinical trials
Condition:   Rheumatoid Arthritis Interventions:   Drug: Tocilizumab;   Drug: Abatacept Sponsors:   Brigham and Women's Hospital;   National Institute on Aging (NIA);   Rutgers University;   Johns Hopkins University Active, not recruiting
Source: ClinicalTrials.gov - Category: Research Source Type: clinical trials
Condition:   Rheumatoid Arthritis Interventions:   Drug: Tumor Necrosis Factor Inhibitors;   Drug: Abatacept Sponsors:   Brigham and Women's Hospital;   National Institute on Aging (NIA);   Rutgers University;   Johns Hopkins University Active, not recruiting
Source: ClinicalTrials.gov - Category: Research Source Type: clinical trials
Condition:   Rheumatoid Arthritis Interventions:   Drug: Tofacitinib;   Drug: Abatacept Sponsors:   Brigham and Women's Hospital;   National Institute on Aging (NIA);   Rutgers University;   Johns Hopkins University Active, not recruiting
Source: ClinicalTrials.gov - Category: Research Source Type: clinical trials
Condition:   Rheumatoid Arthritis Interventions:   Drug: Tocilizumab;   Drug: Abatacept Sponsors:   Brigham and Women's Hospital;   National Institute on Aging (NIA);   Rutgers University;   Johns Hopkins University Active, not recruiting
Source: ClinicalTrials.gov - Category: Research Source Type: clinical trials
Condition:   Rheumatoid Arthritis Interventions:   Drug: Tumor Necrosis Factor Inhibitors;   Drug: Abatacept Sponsors:   Brigham and Women's Hospital;   National Institute on Aging (NIA);   Rutgers University;   Johns Hopkins University Active, not recruiting
Source: ClinicalTrials.gov - Category: Research Source Type: clinical trials
Condition:   Rheumatoid Arthritis Interventions:   Drug: Tofacitinib;   Drug: Abatacept Sponsors:   Brigham and Women's Hospital;   National Institute on Aging (NIA);   Rutgers University;   Johns Hopkins University Active, not recruiting
Source: ClinicalTrials.gov - Category: Research Source Type: clinical trials
Condition:   Rheumatoid Arthritis Interventions:   Drug: Tocilizumab;   Drug: Abatacept Sponsors:   Brigham and Women's Hospital;   National Institute on Aging (NIA);   Rutgers University;   Johns Hopkins University Active, not recruiting
Source: ClinicalTrials.gov - Category: Research Source Type: clinical trials
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