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Items: 1 to 20 of 91

1.

Mechanisms of PI3Kβ-selective inhibition revealed by reciprocal mutagenesis.

Zheng Z, Miller MS, Jennings IG, Thompson PE.

ACS Chem Biol. 2013 Apr 19;8(4):679-83. doi: 10.1021/cb300666s. Epub 2013 Feb 6.

PMID:
23360067
2.

Theoretical studies on beta and delta isoform-specific binding mechanisms of phosphoinositide 3-kinase inhibitors.

Zhu J, Pan P, Li Y, Wang M, Li D, Cao B, Mao X, Hou T.

Mol Biosyst. 2014 Mar 4;10(3):454-66. doi: 10.1039/c3mb70314b. Epub 2013 Dec 16.

PMID:
24336903
3.

Dissecting isoform selectivity of PI3K inhibitors: the role of non-conserved residues in the catalytic pocket.

Frazzetto M, Suphioglu C, Zhu J, Schmidt-Kittler O, Jennings IG, Cranmer SL, Jackson SP, Kinzler KW, Vogelstein B, Thompson PE.

Biochem J. 2008 Sep 15;414(3):383-90. doi: 10.1042/BJ20080512.

4.

Rational design of phosphoinositide 3-kinase α inhibitors that exhibit selectivity over the phosphoinositide 3-kinase β isoform.

Heffron TP, Wei B, Olivero A, Staben ST, Tsui V, Do S, Dotson J, Folkes AJ, Goldsmith P, Goldsmith R, Gunzner J, Lesnick J, Lewis C, Mathieu S, Nonomiya J, Shuttleworth S, Sutherlin DP, Wan NC, Wang S, Wiesmann C, Zhu BY.

J Med Chem. 2011 Nov 24;54(22):7815-33. doi: 10.1021/jm2007084. Epub 2011 Oct 21.

PMID:
21985639
5.

Discovery of new aminopyrimidine-based phosphoinositide 3-kinase beta (PI3Kβ) inhibitors with selectivity over PI3Kα.

Kim J, Hong S, Hong S.

Bioorg Med Chem Lett. 2011 Dec 1;21(23):6977-81. doi: 10.1016/j.bmcl.2011.09.118. Epub 2011 Oct 8.

PMID:
22030027
6.

Regulation and roles of PI3Kβ, a major actor in platelet signaling and functions.

Gratacap MP, Guillermet-Guibert J, Martin V, Chicanne G, Tronchère H, Gaits-Iacovoni F, Payrastre B.

Adv Enzyme Regul. 2011;51(1):106-16. doi: 10.1016/j.advenzreg.2010.09.011. Epub 2010 Oct 28. Review.

PMID:
21035500
7.

Isoform selective phosphoinositide 3-kinase gamma and delta inhibitors and their therapeutic potential.

Ghigo A, Hirsch E.

Recent Pat Inflamm Allergy Drug Discov. 2008 Jan;2(1):1-10. Review.

PMID:
19075988
8.

Discovery and antiplatelet activity of a selective PI3Kβ inhibitor (MIPS-9922).

Zheng Z, Pinson JA, Mountford SJ, Orive S, Schoenwaelder SM, Shackleford D, Powell A, Nelson EM, Hamilton JR, Jackson SP, Jennings IG, Thompson PE.

Eur J Med Chem. 2016 Oct 21;122:339-51. doi: 10.1016/j.ejmech.2016.06.010. Epub 2016 Jun 10.

PMID:
27387421
9.

Discovery of Highly Isoform Selective Thiazolopiperidine Inhibitors of Phosphoinositide 3-Kinase γ.

Collier PN, Messersmith D, Le Tiran A, Bandarage UK, Boucher C, Come J, Cottrell KM, Damagnez V, Doran JD, Griffith JP, Khare-Pandit S, Krueger EB, Ledeboer MW, Ledford B, Liao Y, Mahajan S, Moody CS, Roday S, Wang T, Xu J, Aronov AM.

J Med Chem. 2015 Jul 23;58(14):5684-8. doi: 10.1021/acs.jmedchem.5b00498. Epub 2015 Jul 6.

PMID:
26121481
10.

The Rational Design of Selective Benzoxazepin Inhibitors of the α-Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of (S)-2-((2-(1-Isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide (GDC-0326).

Heffron TP, Heald RA, Ndubaku C, Wei B, Augistin M, Do S, Edgar K, Eigenbrot C, Friedman L, Gancia E, Jackson PS, Jones G, Kolesnikov A, Lee LB, Lesnick JD, Lewis C, McLean N, Mörtl M, Nonomiya J, Pang J, Price S, Prior WW, Salphati L, Sideris S, Staben ST, Steinbacher S, Tsui V, Wallin J, Sampath D, Olivero AG.

J Med Chem. 2016 Feb 11;59(3):985-1002. doi: 10.1021/acs.jmedchem.5b01483. Epub 2016 Jan 20.

PMID:
26741947
11.

Design, Synthesis and Biological Evaluation of Novel Benzothiazole Derivatives as Selective PI3Kβ Inhibitors.

Cao S, Cao R, Liu X, Luo X, Zhong W.

Molecules. 2016 Jul 2;21(7). pii: E876. doi: 10.3390/molecules21070876.

12.

L-Aminoacyl-triazine derivatives are isoform-selective PI3Kβ inhibitors that target non-conserved Asp862 of PI3Kβ

Pinson JA, Zheng Z, Miller MS, Chalmers DK, Jennings IG, Thompson PE.

ACS Med Chem Lett. 2013 Feb 14;4(2):206-210.

13.

Discovery of a potent and isoform-selective targeted covalent inhibitor of the lipid kinase PI3Kα.

Nacht M, Qiao L, Sheets MP, St Martin T, Labenski M, Mazdiyasni H, Karp R, Zhu Z, Chaturvedi P, Bhavsar D, Niu D, Westlin W, Petter RC, Medikonda AP, Singh J.

J Med Chem. 2013 Feb 14;56(3):712-21. doi: 10.1021/jm3008745. Epub 2013 Feb 5.

PMID:
23360348
14.

Binding selectivity studies of phosphoinositide 3-kinases using free energy calculations.

Sabbah DA, Vennerstrom JL, Zhong HA.

J Chem Inf Model. 2012 Dec 21;52(12):3213-24. doi: 10.1021/ci3003057. Epub 2012 Nov 30.

PMID:
23157418
15.

Discovery and optimization of new benzimidazole- and benzoxazole-pyrimidone selective PI3Kβ inhibitors for the treatment of phosphatase and TENsin homologue (PTEN)-deficient cancers.

Certal V, Halley F, Virone-Oddos A, Delorme C, Karlsson A, Rak A, Thompson F, Filoche-Rommé B, El-Ahmad Y, Carry JC, Abecassis PY, Lejeune P, Vincent L, Bonnevaux H, Nicolas JP, Bertrand T, Marquette JP, Michot N, Benard T, Below P, Vade I, Chatreaux F, Lebourg G, Pilorge F, Angouillant-Boniface O, Louboutin A, Lengauer C, Schio L.

J Med Chem. 2012 May 24;55(10):4788-805. doi: 10.1021/jm300241b. Epub 2012 May 2.

PMID:
22524426
16.

Structural basis for selective inhibition of Src family kinases by PP1.

Liu Y, Bishop A, Witucki L, Kraybill B, Shimizu E, Tsien J, Ubersax J, Blethrow J, Morgan DO, Shokat KM.

Chem Biol. 1999 Sep;6(9):671-8.

17.

Discovery of thiazolobenzoxepin PI3-kinase inhibitors that spare the PI3-kinase β isoform.

Staben ST, Ndubaku C, Blaquiere N, Belvin M, Bull RJ, Dudley D, Edgar K, Gray D, Heald R, Heffron TP, Jones GE, Jones M, Kolesnikov A, Lee L, Lesnick J, Lewis C, Murray J, McLean NJ, Nonomiya J, Olivero AG, Ord R, Pang J, Price S, Prior WW, Rouge L, Salphati L, Sampath D, Wallin J, Wang L, Wei B, Weismann C, Wu P.

Bioorg Med Chem Lett. 2013 May 1;23(9):2606-13. doi: 10.1016/j.bmcl.2013.02.102. Epub 2013 Mar 7.

PMID:
23540645
18.

Isoform-selective inhibition of phosphoinositide 3-kinase: identification of a new region of nonconserved amino acids critical for p110α inhibition.

Zheng Z, Amran SI, Thompson PE, Jennings IG.

Mol Pharmacol. 2011 Oct;80(4):657-64. doi: 10.1124/mol.111.072546. Epub 2011 Jul 21.

19.

A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling.

Knight ZA, Gonzalez B, Feldman ME, Zunder ER, Goldenberg DD, Williams O, Loewith R, Stokoe D, Balla A, Toth B, Balla T, Weiss WA, Williams RL, Shokat KM.

Cell. 2006 May 19;125(4):733-47. Epub 2006 Apr 27.

20.

Definition of the binding mode of a new class of phosphoinositide 3-kinase α-selective inhibitors using in vitro mutagenesis of non-conserved amino acids and kinetic analysis.

Zheng Z, Amran SI, Zhu J, Schmidt-Kittler O, Kinzler KW, Vogelstein B, Shepherd PR, Thompson PE, Jennings IG.

Biochem J. 2012 Jun 15;444(3):529-35. doi: 10.1042/BJ20120499.

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