1SOJ

CATALYTIC DOMAIN OF HUMAN PHOSPHODIESTERASE 3B IN COMPLEX WITH IBMX

1SOJ の概要

• エントリーDOI: 10.2210/pdb1soj/pdb
• 関連するPDBエントリー: 1SO2
• 分子名称: cGMP-inhibited 3',5'-cyclic phosphodiesterase B, MAGNESIUM ION, 3-ISOBUTYL-1-METHYLXANTHINE, ... (4 entities in total)
• 機能のキーワード: pde3b phosphodiesterase, hydrolase
• 由来する生物種: Homo sapiens (human)
• 細胞内の位置: Membrane; Multi-pass membrane protein (Potential): Q13370
• タンパク質・核酸の鎖数: 12
• 化学式量合計: 581155.62

構造登録者

Scapin, G.,Patel, S.B.,Chung, C.,Varnerin, J.P.,Edmondson, S.D.,Mastracchio, A.,Parmee, E.R.,Becker, J.W.,Singh, S.B.,Van Der Ploeg, L.H.,Tota, M.R. (登録日: 2004-03-15, 公開日: 2004-05-11, 最終更新日: 2023-08-23)

主引用文献

Scapin, G.,Patel, S.B.,Chung, C.,Varnerin, J.P.,Edmondson, S.D.,Mastracchio, A.,Parmee, E.R.,Singh, S.B.,Becker, J.W.,Van Der Ploeg, L.H.,Tota, M.R.
Crystal Structure of Human Phosphodiesterase 3B: Atomic Basis for Substrate and Inhibitor Specificity
Biochemistry, 43:6091-6100, 2004

PubMed Abstract: Phosphodiesterases (PDEs) are enzymes that modulate cyclic nucleotide signaling and as such are clinical targets for a range of disorders including congestive heart failure, erectile dysfunction, and inflammation. The PDE3 family comprises two highly homologous subtypes expressed in different tissues, and inhibitors of this family have been shown to increase lipolysis in adipocytes. A specific PDE3B (the lipocyte-localized subtype) inhibitor would be a very useful tool to evaluate the effects of PDE3 inhibition on lipolysis and metabolic rate and might become a novel tool for treatment of obesity. We report here the three-dimensional structures of the catalytic domain of human PDE3B in complex with a generic PDE inhibitor and a novel PDE3 selective inhibitor. These structures explain the dual cAMP/cGMP binding capabilities of PDE3, provide the molecular basis for inhibitor specificity, and can supply a valid platform for the design of improved compounds.

PubMed: 15147193
DOI: 10.1021/bi049868i

実験手法

X-RAY DIFFRACTION (2.9 Å)