2023年12月21日 · p85亚单位主要负责pi3k的调节和定位功能，而p110亚单位则是pi3k的催化亚基，具有激酶活性，将磷脂酰肌醇磷酸化为次级信号分子。两者合作共同完成pi3k信号通路的调控和传递。

2009年10月16日 · We found that PI3K Class-IA p110 α and p110 β have distinct functions in myoblasts. Inhibition of p110 α reduced insulin-like growth factor-I (IGF-I)-stimulated Akt activity and prevented...

2010年1月10日 · Structures of this enzyme in complex with a broad panel of isoform- and pan-selective class I PI (3)K inhibitors reveal that selectivity toward p110δ can be achieved by exploiting its...

1997年4月29日 · We report herein the cloning and characterization of p110δ, a novel class I PI3K. Like p110α and p110β, other class I PI3Ks, p110δ displays a broad phosphoinositide lipid substrate specificity and interacts with SH2/SH3 domain-containing p85 adaptor proteins and with GTP-bound Ras.

1997年8月1日 · We have identified a novel p110 isoform of phosphatidylinositol 3-kinase from human leukocytes that we have termed p110δ. In addition, we have independently isolated p110δ from a mouse embryo library on the basis of its ability to interact with Ha-Ras V12 in the yeast two-hybrid system.

The present invention relates to a DNA sequence encoding a novel neuronal protein kinase (NPK) which phosphorylates tau proteins as well as other microtubule associated proteins (MAPs) in...

To elucidate the molecular mechanisms of isoform-selectivity of PI3Kδ inhibitors, we report the crystal structure of the catalytic core of p110δ, both free and in complexes with a broad panel of novel and mostly p110δ-selective PI3K inhibitors.

Deregulation of the phosphoinositide-3-OH kinase (PI(3)K) pathway has been implicated in numerous pathologies including cancer, diabetes, thrombosis, rheumatoid arthritis and asthma. Recently, small-molecule and ATP-competitive PI(3)K inhibitors with a wide range of selectivities have entered clinical development.

2010年3月1日 · In order to understand the mechanisms underlying the isoform selectivity of these inhibitors, we developed a new expression strategy that enabled us to determine to our knowledge the first crystal...

2010年1月10日 · We have used these observations to rationalize and synthesize highly selective inhibitors for p110δ with greatly improved potencies. Domain organization, construct design and overall crystal...