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Article

Identification of PDE4B Over 4D subtype-selective inhibitors revealing an unprecedented binding mode.

Bioorganic & medicinal chemistry - 15 Jul 2009

Kranz Michael, Wall Michael, Evans Brian, Miah Afjal, Ballantine Stuart, Delves Chris, Dombroski Brian, Gross Jeffrey, Schneck Jessica, Villa James P, Neu Margarete, Somers Don O

Abstract excerpt

A PDE4B over 4D-selective inhibitor programme was initiated to capitalise on the recently discovered predominance of the PDE4B subtype in inflammatory cell regulation. The SAR of a tetrahydrobenzothiophene (THBT) series did not agree with either of two proposed docking modes in the 4B binding site. A subsequent X-ray co-crystal structure determination revealed that the THBT ligand displaces the Gln-443 residue,...

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Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

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Identifiers

PMID: 19525117
DOI: 10.1016/j.bmc.2009.03.061

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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