CHP1与NHE1的C端两亲性螺旋HC1结合,并在NHE1的内向和外向构象之间呈现不同的结合角度。小分子药物Cariporide与底物钠离子竞争性结合在NHE1靠近胞外侧的底物结合口袋中,并且阻滞了结构域间的相对运动,从而抑制了NHE1-CHP1复合物的转运活性。 中国科学院生物物理所赵岩研究员、张凯研究员和加拿大McGill University的Jo...
Sodium/proton exchanger 1 (NHE1) is an electroneutral secondary active transporter present on the plasma membrane of most mammalian cells and plays critical roles in regulating intracellular pH and volume homeostasis. Calcineurin B-homologous protein 1 (CHP1) is an obligate binding partner that ...
Human NHE1 features a long C-terminal tail that interacts with a variety of cytoplasmic partners involved in modulating its activity at the cell surface3,6. For instance, calcineurin B-homologous proteins (CHP1−3) are a family of EF-hand calcium binding proteins that serve as obligatory bin...
While several proteins, lipids and kinases are responsible for regulating NHE, two proteins, calcineurin homologous protein isoform 1 (CHP1) and 2 (CHP2) are of particular interest in lung cancer cells. While CHP1 binds NHE1 and is responsible for basal activation of NHE1, CHP2 expression ...
The Calcineurin homologous B protein isoforms 1 and 2 (CHP1/2) interact with NHE1 at the same 40aa domain (CHP binding domain (CBD)) both impacting NHE1 function. CHP1 is ubiquitously expressed and its interaction with NHE promotes basal activity. While CHP2 expression is limited to the ...
CHP3 as well as both regions of NHE1 in question were produced and purified. CHP3 specifically formed stable complexes with the CHP-binding region (CBD) of NHE1 (residues 503–545) in size-exclusion chromatography (SEC), but not with the C-terminal region (CTD, residues 633–815). CTD...
We studied the role of the interaction of calcineurin homologous protein 1 (CHP1) with the Na(+)/H(+) exchanger 1 (NHE1), particularly its EF-hand Ca(2+) b... ‡ Tianxiang Pang,‡ Takashi Hisamitsu,⊥ Hidezo Mori,... - 《Biochemistry》 被引量: 154发表: 2004年 Critical role ...
We studied the role of the interaction of calcineurin homologous protein 1 (CHP1) with the Na(+)/H(+) exchanger 1 (NHE1), particularly its EF-hand Ca(2+) b... ‡ Tianxiang Pang,‡ Takashi Hisamitsu,⊥ Hidezo Mori,... - 《Biochemistry》 被引量: 154发表: 2004年 Critical role ...
Crystal structure of CHP2 complexed with NHE1-cytosolic region and an implication for pH regulation. EMBO J. 25:2315- 2325.Ammar YB, Takeda S, Hisamitsu T, Mori H & Wakabayashi S (2006) Crystal structure of CHP2 complexed with NHE1-cytosolic region and an implication for pH regulation. ...