1HV7

PORCINE PANCREATIC ELASTASE COMPLEXED WITH GW311616A

Summary for 1HV7

• Entry DOI: 10.2210/pdb1hv7/pdb
• Descriptor: ELASTASE 1, SULFATE ION, N-[2-(1-FORMYL-2-METHYL-PROPYL)-1-(4-PIPERIDIN-1-YL-BUT-2-ENOYL)-PYRROLIDIN-3-YL]-METHANESULFONAMIDE, ... (4 entities in total)
• Functional Keywords: serine protease-inhibitor complex, hydrolase
• Biological source: Sus scrofa (pig)
• Cellular location: Secreted: P00772
• Total number of polymer chains: 1
• Total formula weight: 26424.63

Authors

Skarzynski, T.,Singh, O.M. (deposition date: 2001-01-08, release date: 2001-01-17, Last modification date: 2024-11-13)

Primary citation

Macdonald, S.J.,Dowle, M.D.,Harrison, L.A.,Shah, P.,Johnson, M.R.,Inglis, G.G.,Clarke, G.D.,Smith, R.A.,Humphreys, D.,Molloy, C.R.,Amour, A.,Dixon, M.,Murkitt, G.,Godward, R.E.,Padfield, T.,Skarzynski, T.,Singh, O.M.,Kumar, K.A.,Fleetwood, G.,Hodgson, S.T.,Hardy, G.W.,Finch, H.
The discovery of a potent, intracellular, orally bioavailable, long duration inhibitor of human neutrophil elastase--GW311616A a development candidate
Bioorg.Med.Chem.Lett., 11:895-898, 2001

PubMed Abstract: The discovery of a potent intracellular inhibitor of human neutrophil elastase which is orally active and has a long duration of action is described. The pharmacodynamic and pharmacokinetic properties of a trans-lactam development candidate, GW311616A, are described.

PubMed: 11294386
DOI: 10.1016/S0960-894X(01)00078-6

Experimental method

X-RAY DIFFRACTION (1.7 Å)