Literature summary for 2.7.1.153 extracted from

Somoza, J.R.; Koditek, D.; Villasenor, A.G.; Novikov, N.; Wong, M.H.; Liclican, A.; Xing, W.; Lagpacan, L.; Wang, R.; Schultz, B.E.; Papalia, G.A.; Samuel, D.; Lad, L.; McGrath, M.E.
Structural, biochemical, and biophysical characterization of idelalisib binding to phosphoinositide 3-kinase delta (2015), J. Biol. Chem., 290, 8439-8446.

Search for more literature for 2.7.1.153

Cloned(Commentary)

Cloned (Comment)	Organism
coexpression of N-terminally His6-tagged p110 and nontagged p85 subunits in Spodoptera frugiperda Sf21 cells via baculovirus transfection method, recombinant expression of DELTAABC mutant p110delta with the iSH2 domain of p85alpha	Homo sapiens

Crystallization (Commentary)

Crystallization (Comment)	Organism
purified enzyme mutant, mixing of 25 nl 11 mg/ml protein with 0.9 mM inhibitor delalisib in 20 mM Tris, pH 7.2, 50 mM (NH4)2SO4, 1% v/v ethylene glycol, 1% w/v betaine, 300 mM CHAPS, and 5 mM TCEP, with 25 nl of reservoir solution containing 25% w/v PEG 3350, 0.1 M Bis-Tris, pH 6.5, microseeding in 480 nl of 2.5% w/v n-dodecyl-beta-D-maltoside, 300 nl of 20 mM ligand, and 0.12 ml of 12 mg/ml DELTAABD-p110delta in storage buffer 20 mM Tris, pH 7.2, 50 mM (NH4)2SO4, 1% v/v ethylene glycol, 1% w/v betaine, 300 nM CHAPS, and 5mM TCEP, X-ray diffraction structure determination and analysis at 2.4-2.5 A resolution	Homo sapiens

Crystallization (Comment)

Organism

purified enzyme mutant, mixing of 25 nl 11 mg/ml protein with 0.9 mM inhibitor delalisib in 20 mM Tris, pH 7.2, 50 mM (NH4)2SO4, 1% v/v ethylene glycol, 1% w/v betaine, 300 mM CHAPS, and 5 mM TCEP, with 25 nl of reservoir solution containing 25% w/v PEG 3350, 0.1 M Bis-Tris, pH 6.5, microseeding in 480 nl of 2.5% w/v n-dodecyl-beta-D-maltoside, 300 nl of 20 mM ligand, and 0.12 ml of 12 mg/ml DELTAABD-p110delta in storage buffer 20 mM Tris, pH 7.2, 50 mM (NH4)2SO4, 1% v/v ethylene glycol, 1% w/v betaine, 300 nM CHAPS, and 5mM TCEP, X-ray diffraction structure determination and analysis at 2.4-2.5 A resolution

Homo sapiens

Inhibitors

Inhibitors	Comment	Organism	Structure
idelalisib	5-fluoro-3-phenyl-2-[(1S)-1-(9H-purin-6-ylamino)propyl]quinazolin-4(3H)-one, a PI3Kdelta inhibitor used to treat hematological malignancies. The inhibitor idelalisib is selective, noncovalent, reversible, and ATP-competitive. The compound binds reversibly and noncovalently to the p110delta subunit of the kinase, analysis of binding interactions that confer the potency and selectivity of idelalisib, overview. Idelalisib is a propeller-shaped inhibitor	Homo sapiens

Metals/Ions

Metals/Ions	Comment	Organism	Structure
Mg2+	required	Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates	Organism	Comment (Nat. Sub.)	Natural Products	Comment (Nat. Pro.)	Rev.	Reac.
ATP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate	Homo sapiens	-	ADP + 1-phosphatidyl-1D-myo-inositol 3,4,5-trisphosphate	-	?

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	O00329	isozyme PI3Kdelta	-

Purification (Commentary)

Purification (Comment)	Organism
recombinant N-terminally His6-tagged p110 and nontagged p85 subunits from Spodoptera frugiperda Sf21 cells by nickel affinity chromatography	Homo sapiens

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
ATP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate	-	Homo sapiens	ADP + 1-phosphatidyl-1D-myo-inositol 3,4,5-trisphosphate	-	?

Synonyms

Synonyms	Comment	Organism
PI3Kdelta	-	Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C]	Temperature Optimum Maximum [°C]	Comment	Organism
25	-	assay at	Homo sapiens

pH Optimum

pH Optimum Minimum	pH Optimum Maximum	Comment	Organism
7.4	-	assay at	Homo sapiens

Cofactor

Cofactor	Comment	Organism	Structure
ATP	-	Homo sapiens