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Items: 36

1.

Structural basis of species-selective antagonist binding to the succinate receptor.

Haffke M, Fehlmann D, Rummel G, Boivineau J, Duckely M, Gommermann N, Cotesta S, Sirockin F, Freuler F, Littlewood-Evans A, Kaupmann K, Jaakola VP.

Nature. 2019 Oct;574(7779):581-585. doi: 10.1038/s41586-019-1663-8. Epub 2019 Oct 23.

PMID:
31645725
2.

Small-molecule factor B inhibitor for the treatment of complement-mediated diseases.

Schubart A, Anderson K, Mainolfi N, Sellner H, Ehara T, Adams CM, Mac Sweeney A, Liao SM, Crowley M, Littlewood-Evans A, Sarret S, Wieczorek G, Perrot L, Dubost V, Flandre T, Zhang Y, Smith RJH, Risitano AM, Karki RG, Zhang C, Valeur E, Sirockin F, Gerhartz B, Erbel P, Hughes N, Smith TM, Cumin F, Argikar UA, Haraldsson B, Mogi M, Sedrani R, Wiesmann C, Jaffee B, Maibaum J, Flohr S, Harrison R, Eder J.

Proc Natl Acad Sci U S A. 2019 Apr 16;116(16):7926-7931. doi: 10.1073/pnas.1820892116. Epub 2019 Mar 29.

3.

Discovery of CDZ173 (Leniolisib), Representing a Structurally Novel Class of PI3K Delta-Selective Inhibitors.

Hoegenauer K, Soldermann N, Zécri F, Strang RS, Graveleau N, Wolf RM, Cooke NG, Smith AB, Hollingworth GJ, Blanz J, Gutmann S, Rummel G, Littlewood-Evans A, Burkhart C.

ACS Med Chem Lett. 2017 Aug 25;8(9):975-980. doi: 10.1021/acsmedchemlett.7b00293. eCollection 2017 Sep 14.

4.

Design and synthesis of potent and orally active GPR4 antagonists with modulatory effects on nociception, inflammation, and angiogenesis.

Miltz W, Velcicky J, Dawson J, Littlewood-Evans A, Ludwig MG, Seuwen K, Feifel R, Oberhauser B, Meyer A, Gabriel D, Nash M, Loetscher P.

Bioorg Med Chem. 2017 Aug 15;25(16):4512-4525. doi: 10.1016/j.bmc.2017.06.050. Epub 2017 Jun 29.

PMID:
28689977
5.

Development of Selective, Orally Active GPR4 Antagonists with Modulatory Effects on Nociception, Inflammation, and Angiogenesis.

Velcicky J, Miltz W, Oberhauser B, Orain D, Vaupel A, Weigand K, Dawson King J, Littlewood-Evans A, Nash M, Feifel R, Loetscher P.

J Med Chem. 2017 May 11;60(9):3672-3683. doi: 10.1021/acs.jmedchem.6b01703. Epub 2017 Apr 26.

PMID:
28445047
6.

GPR91 deficiency exacerbates allergic contact dermatitis while reducing arthritic disease in mice.

Rubić-Schneider T, Carballido-Perrig N, Regairaz C, Raad L, Jost S, Rauld C, Christen B, Wieczorek G, Kreutzer R, Dawson J, Lametschwandner G, Littlewood-Evans A, Carballido JM.

Allergy. 2017 Mar;72(3):444-452. doi: 10.1111/all.13005. Epub 2016 Sep 12.

7.

GPR91 senses extracellular succinate released from inflammatory macrophages and exacerbates rheumatoid arthritis.

Littlewood-Evans A, Sarret S, Apfel V, Loesle P, Dawson J, Zhang J, Muller A, Tigani B, Kneuer R, Patel S, Valeaux S, Gommermann N, Rubic-Schneider T, Junt T, Carballido JM.

J Exp Med. 2016 Aug 22;213(9):1655-62. doi: 10.1084/jem.20160061. Epub 2016 Aug 1.

8.

A Novel Potent Oral Series of VEGFR2 Inhibitors Abrogate Tumor Growth by Inhibiting Angiogenesis.

Bold G, Schnell C, Furet P, McSheehy P, Brüggen J, Mestan J, Manley PW, Drückes P, Burglin M, Dürler U, Loretan J, Reuter R, Wartmann M, Theuer A, Bauer-Probst B, Martiny-Baron G, Allegrini P, Goepfert A, Wood J, Littlewood-Evans A.

J Med Chem. 2016 Jan 14;59(1):132-46. doi: 10.1021/acs.jmedchem.5b01582. Epub 2015 Dec 21.

PMID:
26629594
9.

Discovery and profiling of a selective and efficacious Syk inhibitor.

Thoma G, Smith AB, van Eis MJ, Vangrevelinghe E, Blanz J, Aichholz R, Littlewood-Evans A, Lee CC, Liu H, Zerwes HG.

J Med Chem. 2015 Feb 26;58(4):1950-63. doi: 10.1021/jm5018863. Epub 2015 Feb 9.

PMID:
25633741
10.

Contextual compound screening for improved therapeutic discovery.

Evensen L, Odlo K, Micklem DR, Littlewood-Evans A, Wood J, Kuzniewski C, Altmann KH, Hansen TV, Lorens JB.

Chembiochem. 2013 Dec 16;14(18):2512-8. doi: 10.1002/cbic.201300409. Epub 2013 Nov 12.

PMID:
24222525
11.

The tyrosine kinase BMX is an essential mediator of inflammatory arthritis in a kinase-independent manner.

Gottar-Guillier M, Dodeller F, Huesken D, Iourgenko V, Mickanin C, Labow M, Gaveriaux S, Kinzel B, Mueller M, Alitalo K, Littlewood-Evans A, Cenni B.

J Immunol. 2011 May 15;186(10):6014-23. doi: 10.4049/jimmunol.1002813. Epub 2011 Apr 6.

12.

Th17 cells, not IL-17+ γδ T cells, drive arthritic bone destruction in mice and humans.

Pöllinger B, Junt T, Metzler B, Walker UA, Tyndall A, Allard C, Bay S, Keller R, Raulf F, Di Padova F, O'Reilly T, Horwood NJ, Patel DD, Littlewood-Evans A.

J Immunol. 2011 Feb 15;186(4):2602-12. doi: 10.4049/jimmunol.1003370. Epub 2011 Jan 7.

13.

Angiogenesis is present in experimental autoimmune encephalomyelitis and pro-angiogenic factors are increased in multiple sclerosis lesions.

Seabrook TJ, Littlewood-Evans A, Brinkmann V, Pöllinger B, Schnell C, Hiestand PC.

J Neuroinflammation. 2010 Dec 22;7:95. doi: 10.1186/1742-2094-7-95.

14.

Biological evidence for dual antiangiogenic-antiaromatase activity of the VEGFR inhibitor PTK787/ZK222584 in vivo.

Banerjee S, A'Hern R, Detre S, Littlewood-Evans AJ, Evans DB, Dowsett M, Martin LA.

Clin Cancer Res. 2010 Aug 15;16(16):4178-87. doi: 10.1158/1078-0432.CCR-10-0456. Epub 2010 Aug 3.

15.

In vivo and in vitro SAR of tetracyclic MAPKAP-K2 (MK2) inhibitors. Part II.

Revesz L, Schlapbach A, Aichholz R, Dawson J, Feifel R, Hawtin S, Littlewood-Evans A, Koch G, Kroemer M, Möbitz H, Scheufler C, Velcicky J, Huppertz C.

Bioorg Med Chem Lett. 2010 Aug 1;20(15):4719-23. doi: 10.1016/j.bmcl.2010.04.023. Epub 2010 Apr 11.

PMID:
20591669
16.

Everolimus and PTK/ZK show synergistic growth inhibition in the orthotopic BL16/BL6 murine melanoma model.

O'Reilly T, Lane HA, Wood JM, Schnell C, Littlewood-Evans A, Brueggen J, McSheehy PM.

Cancer Chemother Pharmacol. 2011 Jan;67(1):193-200. doi: 10.1007/s00280-010-1307-z. Epub 2010 May 30.

PMID:
20512579
17.

Mural cell associated VEGF is required for organotypic vessel formation.

Evensen L, Micklem DR, Blois A, Berge SV, Aarsaether N, Littlewood-Evans A, Wood J, Lorens JB.

PLoS One. 2009 Jun 4;4(6):e5798. doi: 10.1371/journal.pone.0005798.

18.

The critical role of kinase activity of interleukin-1 receptor-associated kinase 4 in animal models of joint inflammation.

Koziczak-Holbro M, Littlewood-Evans A, Pöllinger B, Kovarik J, Dawson J, Zenke G, Burkhart C, Müller M, Gram H.

Arthritis Rheum. 2009 Jun;60(6):1661-71. doi: 10.1002/art.24552.

19.

mTOR inhibitor RAD001 (everolimus) has antiangiogenic/vascular properties distinct from a VEGFR tyrosine kinase inhibitor.

Lane HA, Wood JM, McSheehy PM, Allegrini PR, Boulay A, Brueggen J, Littlewood-Evans A, Maira SM, Martiny-Baron G, Schnell CR, Sini P, O'Reilly T.

Clin Cancer Res. 2009 Mar 1;15(5):1612-22. doi: 10.1158/1078-0432.CCR-08-2057. Epub 2009 Feb 17.

20.

Differential effects of the vascular endothelial growth factor receptor inhibitor PTK787/ZK222584 on tumor angiogenesis and tumor lymphangiogenesis.

Schomber T, Zumsteg A, Strittmatter K, Crnic I, Antoniadis H, Littlewood-Evans A, Wood J, Christofori G.

Mol Cancer Ther. 2009 Jan;8(1):55-63. doi: 10.1158/1535-7163.MCT-08-0679.

21.

Effects of the dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor NVP-BEZ235 on the tumor vasculature: implications for clinical imaging.

Schnell CR, Stauffer F, Allegrini PR, O'Reilly T, McSheehy PM, Dartois C, Stumm M, Cozens R, Littlewood-Evans A, García-Echeverría C, Maira SM.

Cancer Res. 2008 Aug 15;68(16):6598-607. doi: 10.1158/0008-5472.CAN-08-1044.

22.

Inhibition of chronic and acute skin inflammation by treatment with a vascular endothelial growth factor receptor tyrosine kinase inhibitor.

Halin C, Fahrngruber H, Meingassner JG, Bold G, Littlewood-Evans A, Stuetz A, Detmar M.

Am J Pathol. 2008 Jul;173(1):265-77. doi: 10.2353/ajpath.2008.071074. Epub 2008 Jun 5.

23.

Inhibition of multiple vascular endothelial growth factor receptors (VEGFR) blocks lymph node metastases but inhibition of VEGFR-2 is sufficient to sensitize tumor cells to platinum-based chemotherapeutics.

Sini P, Samarzija I, Baffert F, Littlewood-Evans A, Schnell C, Theuer A, Christian S, Boos A, Hess-Stumpp H, Foekens JA, Setyono-Han B, Wood J, Hynes NE.

Cancer Res. 2008 Mar 1;68(5):1581-92. doi: 10.1158/0008-5472.CAN-06-4685.

24.

Antagonism of sphingosine-1-phosphate receptors by FTY720 inhibits angiogenesis and tumor vascularization.

LaMontagne K, Littlewood-Evans A, Schnell C, O'Reilly T, Wyder L, Sanchez T, Probst B, Butler J, Wood A, Liau G, Billy E, Theuer A, Hla T, Wood J.

Cancer Res. 2006 Jan 1;66(1):221-31.

25.

Beta1-integrins are critical for cerebellar granule cell precursor proliferation.

Blaess S, Graus-Porta D, Belvindrah R, Radakovits R, Pons S, Littlewood-Evans A, Senften M, Guo H, Li Y, Miner JH, Reichardt LF, Müller U.

J Neurosci. 2004 Mar 31;24(13):3402-12.

26.

The Usher syndrome proteins cadherin 23 and harmonin form a complex by means of PDZ-domain interactions.

Siemens J, Kazmierczak P, Reynolds A, Sticker M, Littlewood-Evans A, Müller U.

Proc Natl Acad Sci U S A. 2002 Nov 12;99(23):14946-51. Epub 2002 Oct 29.

27.

Conditional disruption of beta 1 integrin in Schwann cells impedes interactions with axons.

Feltri ML, Graus Porta D, Previtali SC, Nodari A, Migliavacca B, Cassetti A, Littlewood-Evans A, Reichardt LF, Messing A, Quattrini A, Mueller U, Wrabetz L.

J Cell Biol. 2002 Jan 7;156(1):199-209. Epub 2002 Jan 3.

28.

Beta1-class integrins regulate the development of laminae and folia in the cerebral and cerebellar cortex.

Graus-Porta D, Blaess S, Senften M, Littlewood-Evans A, Damsky C, Huang Z, Orban P, Klein R, Schittny JC, Müller U.

Neuron. 2001 Aug 16;31(3):367-79.

29.

Mechanisms that regulate mechanosensory hair cell differentiation.

Müller U, Littlewood-Evans A.

Trends Cell Biol. 2001 Aug;11(8):334-42. Review.

PMID:
11489639
30.
31.

Regulation of epidermal homeostasis through P2Y2 receptors.

Dixon CJ, Bowler WB, Littlewood-Evans A, Dillon JP, Bilbe G, Sharpe GR, Gallagher JA.

Br J Pharmacol. 1999 Aug;127(7):1680-6.

32.

P2Y2 receptors are expressed by human osteoclasts of giant cell tumor but do not mediate ATP-induced bone resorption.

Bowler WB, Littlewood-Evans A, Bilbe G, Gallagher JA, Dixon CJ.

Bone. 1998 Mar;22(3):195-200.

PMID:
9514211
33.

The osteoclast-associated protease cathepsin K is expressed in human breast carcinoma.

Littlewood-Evans AJ, Bilbe G, Bowler WB, Farley D, Wlodarski B, Kokubo T, Inaoka T, Sloane J, Evans DB, Gallagher JA.

Cancer Res. 1997 Dec 1;57(23):5386-90.

34.

Local expression of tumor necrosis factor alpha in an experimental model of acute osteomyelitis in rats.

Littlewood-Evans AJ, Hattenberger MR, Lüscher C, Pataki A, Zak O, O'Reilly T.

Infect Immun. 1997 Aug;65(8):3438-43.

35.

Effect of combination therapy of rifampicin and azithromycin on TNF levels during a rat model of chronic osteomyelitis.

Littlewood-Evans AJ, Hattenberger M, Zak O, O'Reilly T.

J Antimicrob Chemother. 1997 Apr;39(4):493-8.

PMID:
9145822
36.

Localization of cathepsin K in human osteoclasts by in situ hybridization and immunohistochemistry.

Littlewood-Evans A, Kokubo T, Ishibashi O, Inaoka T, Wlodarski B, Gallagher JA, Bilbe G.

Bone. 1997 Feb;20(2):81-6.

PMID:
9028530

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