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Items: 37

1.

DSM265 at 400 Milligrams Clears Asexual Stage Parasites but Not Mature Gametocytes from the Blood of Healthy Subjects Experimentally Infected with Plasmodium falciparum.

Collins KA, Rückle T, Elliott S, Marquart L, Ballard E, Chalon S, Griffin P, Möhrle JJ, McCarthy JS.

Antimicrob Agents Chemother. 2019 Mar 27;63(4). pii: e01837-18. doi: 10.1128/AAC.01837-18. Print 2019 Apr.

2.

Antimalarial activity of single-dose DSM265, a novel plasmodium dihydroorotate dehydrogenase inhibitor, in patients with uncomplicated Plasmodium falciparum or Plasmodium vivax malaria infection: a proof-of-concept, open-label, phase 2a study.

Llanos-Cuentas A, Casapia M, Chuquiyauri R, Hinojosa JC, Kerr N, Rosario M, Toovey S, Arch RH, Phillips MA, Rozenberg FD, Bath J, Ng CL, Cowell AN, Winzeler EA, Fidock DA, Baker M, Möhrle JJ, Hooft van Huijsduijnen R, Gobeau N, Araeipour N, Andenmatten N, Rückle T, Duparc S.

Lancet Infect Dis. 2018 Aug;18(8):874-883. doi: 10.1016/S1473-3099(18)30309-8. Epub 2018 Jun 13. Erratum in: Lancet Infect Dis. 2018 Aug;18(8):829.

3.

Improved safety margin for embryotoxicity in rats for the new endoperoxide artefenomel (OZ439) as compared to artesunate.

Clark RL, Edwards TL, Longo M, Kinney J, Walker DK, Rhodes J, Clode SA, Rückle T, Wells T, Andenmatten N, Huber AC.

Birth Defects Res. 2018 Apr 17;110(7):553-578. doi: 10.1002/bdr2.1170. Epub 2017 Nov 28.

PMID:
29193867
4.

DSM265 for Plasmodium falciparum chemoprophylaxis: a randomised, double blinded, phase 1 trial with controlled human malaria infection.

Sulyok M, Rückle T, Roth A, Mürbeth RE, Chalon S, Kerr N, Samec SS, Gobeau N, Calle CL, Ibáñez J, Sulyok Z, Held J, Gebru T, Granados P, Brückner S, Nguetse C, Mengue J, Lalremruata A, Sim BKL, Hoffman SL, Möhrle JJ, Kremsner PG, Mordmüller B.

Lancet Infect Dis. 2017 Jun;17(6):636-644. doi: 10.1016/S1473-3099(17)30139-1. Epub 2017 Mar 28. Erratum in: Lancet Infect Dis. 2017 Jun;17(6):576.

5.

Safety, tolerability, pharmacokinetics, and activity of the novel long-acting antimalarial DSM265: a two-part first-in-human phase 1a/1b randomised study.

McCarthy JS, Lotharius J, Rückle T, Chalon S, Phillips MA, Elliott S, Sekuloski S, Griffin P, Ng CL, Fidock DA, Marquart L, Williams NS, Gobeau N, Bebrevska L, Rosario M, Marsh K, Möhrle JJ.

Lancet Infect Dis. 2017 Jun;17(6):626-635. doi: 10.1016/S1473-3099(17)30171-8. Epub 2017 Mar 28.

6.

A Phase II pilot trial to evaluate safety and efficacy of ferroquine against early Plasmodium falciparum in an induced blood-stage malaria infection study.

McCarthy JS, Rückle T, Djeriou E, Cantalloube C, Ter-Minassian D, Baker M, O'Rourke P, Griffin P, Marquart L, Hooft van Huijsduijnen R, Möhrle JJ.

Malar J. 2016 Sep 13;15:469. doi: 10.1186/s12936-016-1511-3.

7.

The novel therapeutic effect of phosphoinositide 3-kinase-γ inhibitor AS605240 in autoimmune diabetes.

Azzi J, Moore RF, Elyaman W, Mounayar M, El Haddad N, Yang S, Jurewicz M, Takakura A, Petrelli A, Fiorina P, Ruckle T, Abdi R.

Diabetes. 2012 Jun;61(6):1509-18. doi: 10.2337/db11-0134. Epub 2012 Mar 8.

8.

Critical role for phosphoinositide 3-kinase gamma in parasite invasion and disease progression of cutaneous leishmaniasis.

Cummings HE, Barbi J, Reville P, Oghumu S, Zorko N, Sarkar A, Keiser TL, Lu B, Rückle T, Varikuti S, Lezama-Davila C, Wewers MD, Whitacre C, Radzioch D, Rommel C, Seveau S, Satoskar AR.

Proc Natl Acad Sci U S A. 2012 Jan 24;109(4):1251-6. doi: 10.1073/pnas.1110339109. Epub 2012 Jan 9.

9.

Regulation of the severity of neuroinflammation and demyelination by TLR-ASK1-p38 pathway.

Guo X, Harada C, Namekata K, Matsuzawa A, Camps M, Ji H, Swinnen D, Jorand-Lebrun C, Muzerelle M, Vitte PA, Rückle T, Kimura A, Kohyama K, Matsumoto Y, Ichijo H, Harada T.

EMBO Mol Med. 2010 Dec;2(12):504-15. doi: 10.1002/emmm.201000103.

10.

Phosphoinositide-3 kinase gamma activity contributes to sepsis and organ damage by altering neutrophil recruitment.

Martin EL, Souza DG, Fagundes CT, Amaral FA, Assenzio B, Puntorieri V, Del Sorbo L, Fanelli V, Bosco M, Delsedime L, Pinho JF, Lemos VS, Souto FO, Alves-Filho JC, Cunha FQ, Slutsky AS, Ruckle T, Hirsch E, Teixeira MM, Ranieri VM.

Am J Respir Crit Care Med. 2010 Sep 15;182(6):762-73. doi: 10.1164/rccm.201001-0088OC. Epub 2010 May 27.

PMID:
20508212
11.

Isoform-selective phosphoinositide 3-kinase inhibitors induce apoptosis in chronic lymphocytic leukaemia cells.

de Frias M, Iglesias-Serret D, Cosialls AM, González-Gironès DM, Pérez-Perarnau A, Rubio-Patiño C, Rückle T, Camps M, de Sevilla AF, de la Banda E, Pons G, Gil J.

Br J Haematol. 2010 Jul;150(1):108-11. doi: 10.1111/j.1365-2141.2010.08151.x. Epub 2010 Mar 11. No abstract available.

PMID:
20230409
12.

The p110delta structure: mechanisms for selectivity and potency of new PI(3)K inhibitors.

Berndt A, Miller S, Williams O, Le DD, Houseman BT, Pacold JI, Gorrec F, Hon WC, Liu Y, Rommel C, Gaillard P, Rückle T, Schwarz MK, Shokat KM, Shaw JP, Williams RL.

Nat Chem Biol. 2010 Mar;6(3):244. No abstract available.

PMID:
20154668
13.

The p110 delta structure: mechanisms for selectivity and potency of new PI(3)K inhibitors.

Berndt A, Miller S, Williams O, Le DD, Houseman BT, Pacold JI, Gorrec F, Hon WC, Liu Y, Rommel C, Gaillard P, Rückle T, Schwarz MK, Shokat KM, Shaw JP, Williams RL.

Nat Chem Biol. 2010 Feb;6(2):117-24. doi: 10.1038/nchembio.293.

14.

Phosphoinositide 3-kinase gamma required for lipopolysaccharide-induced transepithelial neutrophil trafficking in the lung.

Reutershan J, Saprito MS, Wu D, Rückle T, Ley K.

Eur Respir J. 2010 May;35(5):1137-47. doi: 10.1183/09031936.00085509. Epub 2009 Sep 24.

15.

PI3Kgamma regulates cartilage damage in chronic inflammatory arthritis.

Hayer S, Pundt N, Peters MA, Wunrau C, Kühnel I, Neugebauer K, Strietholt S, Zwerina J, Korb A, Penninger J, Joosten LA, Gay S, Rückle T, Schett G, Pap T.

FASEB J. 2009 Dec;23(12):4288-98. doi: 10.1096/fj.09-135160. Epub 2009 Sep 4.

PMID:
19734303
16.

Insulin granule recruitment and exocytosis is dependent on p110gamma in insulinoma and human beta-cells.

Pigeau GM, Kolic J, Ball BJ, Hoppa MB, Wang YW, Rückle T, Woo M, Manning Fox JE, MacDonald PE.

Diabetes. 2009 Sep;58(9):2084-92. doi: 10.2337/db08-1371. Epub 2009 Jun 23.

17.

BMP2 induction of actin cytoskeleton reorganization and cell migration requires PI3-kinase and Cdc42 activity.

Gamell C, Osses N, Bartrons R, Rückle T, Camps M, Rosa JL, Ventura F.

J Cell Sci. 2008 Dec 1;121(Pt 23):3960-70. doi: 10.1242/jcs.031286. Epub 2008 Nov 11.

18.

Phosphoinositide 3-kinase p110beta activity: key role in metabolism and mammary gland cancer but not development.

Ciraolo E, Iezzi M, Marone R, Marengo S, Curcio C, Costa C, Azzolino O, Gonella C, Rubinetto C, Wu H, Dastrù W, Martin EL, Silengo L, Altruda F, Turco E, Lanzetti L, Musiani P, Rückle T, Rommel C, Backer JM, Forni G, Wymann MP, Hirsch E.

Sci Signal. 2008 Sep 9;1(36):ra3. doi: 10.1126/scisignal.1161577.

19.

PI3Kgamma (PI3Kgamma) is essential for efficient induction of CXCR3 on activated T cells.

Barbi J, Cummings HE, Lu B, Oghumu S, Rückle T, Rommel C, Lafuse W, Whitacre CC, Satoskar AR.

Blood. 2008 Oct 15;112(8):3048-51. doi: 10.1182/blood-2008-02-135715. Epub 2008 Jul 24.

20.

Genetic and pharmacological targeting of phosphoinositide 3-kinase-gamma reduces atherosclerosis and favors plaque stability by modulating inflammatory processes.

Fougerat A, Gayral S, Gourdy P, Schambourg A, Rückle T, Schwarz MK, Rommel C, Hirsch E, Arnal JF, Salles JP, Perret B, Breton-Douillon M, Wymann MP, Laffargue M.

Circulation. 2008 Mar 11;117(10):1310-7. doi: 10.1161/CIRCULATIONAHA.107.720466. Epub 2008 Feb 11.

PMID:
18268153
21.

Isoform-specific functions of phosphoinositide 3-kinases: p110 delta but not p110 gamma promotes optimal allergic responses in vivo.

Ali K, Camps M, Pearce WP, Ji H, Rückle T, Kuehn N, Pasquali C, Chabert C, Rommel C, Vanhaesebroeck B.

J Immunol. 2008 Feb 15;180(4):2538-44.

22.

Tissue- and stimulus-dependent role of phosphatidylinositol 3-kinase isoforms for neutrophil recruitment induced by chemoattractants in vivo.

Pinho V, Russo RC, Amaral FA, de Sousa LP, Barsante MM, de Souza DG, Alves-Filho JC, Cara DC, Hayflick JS, Rommel C, Ruckle T, Rossi AG, Teixeira MM.

J Immunol. 2007 Dec 1;179(11):7891-8. Erratum in: J Immunol. 2008 Jun 1;180(11):7775. de Castro Russo, Remo [corrected to Russo, Remo Castro].

23.

The p110delta catalytic isoform of PI3K is a key player in NK-cell development and cytokine secretion.

Kim N, Saudemont A, Webb L, Camps M, Ruckle T, Hirsch E, Turner M, Colucci F.

Blood. 2007 Nov 1;110(9):3202-8. Epub 2007 Jul 20.

24.

Inactivation of PI3Kgamma and PI3Kdelta distorts T-cell development and causes multiple organ inflammation.

Ji H, Rintelen F, Waltzinger C, Bertschy Meier D, Bilancio A, Pearce W, Hirsch E, Wymann MP, Rückle T, Camps M, Vanhaesebroeck B, Okkenhaug K, Rommel C.

Blood. 2007 Oct 15;110(8):2940-7. Epub 2007 Jul 12.

25.

Phosphoinositide 3-kinase gamma inhibition plays a crucial role in early steps of inflammation by blocking neutrophil recruitment.

Ferrandi C, Ardissone V, Ferro P, Rückle T, Zaratin P, Ammannati E, Hauben E, Rommel C, Cirillo R.

J Pharmacol Exp Ther. 2007 Sep;322(3):923-30. Epub 2007 May 25.

PMID:
17526805
26.

Importance of phosphoinositide 3-kinase gamma in the host defense against pneumococcal infection.

Maus UA, Backi M, Winter C, Srivastava M, Schwarz MK, Rückle T, Paton JC, Briles D, Mack M, Welte T, Maus R, Bohle RM, Seeger W, Rommel C, Hirsch E, Lohmeyer J, Preissner KT.

Am J Respir Crit Care Med. 2007 May 1;175(9):958-66. Epub 2007 Feb 22.

PMID:
17322108
27.

PI3Kgamma inhibition: towards an 'aspirin of the 21st century'?

Rückle T, Schwarz MK, Rommel C.

Nat Rev Drug Discov. 2006 Nov;5(11):903-18. Epub 2006 Oct 13. Review.

PMID:
17080027
28.

Furan-2-ylmethylene thiazolidinediones as novel, potent, and selective inhibitors of phosphoinositide 3-kinase gamma.

Pomel V, Klicic J, Covini D, Church DD, Shaw JP, Roulin K, Burgat-Charvillon F, Valognes D, Camps M, Chabert C, Gillieron C, Françon B, Perrin D, Leroy D, Gretener D, Nichols A, Vitte PA, Carboni S, Rommel C, Schwarz MK, Rückle T.

J Med Chem. 2006 Jun 29;49(13):3857-71.

PMID:
16789742
29.

Key role of the p110delta isoform of PI3K in B-cell antigen and IL-4 receptor signaling: comparative analysis of genetic and pharmacologic interference with p110delta function in B cells.

Bilancio A, Okkenhaug K, Camps M, Emery JL, Ruckle T, Rommel C, Vanhaesebroeck B.

Blood. 2006 Jan 15;107(2):642-50. Epub 2005 Sep 22.

30.

Blockade of PI3Kgamma suppresses joint inflammation and damage in mouse models of rheumatoid arthritis.

Camps M, Rückle T, Ji H, Ardissone V, Rintelen F, Shaw J, Ferrandi C, Chabert C, Gillieron C, Françon B, Martin T, Gretener D, Perrin D, Leroy D, Vitte PA, Hirsch E, Wymann MP, Cirillo R, Schwarz MK, Rommel C.

Nat Med. 2005 Sep;11(9):936-43. Epub 2005 Aug 28.

31.

PI3Kgamma inhibition blocks glomerulonephritis and extends lifespan in a mouse model of systemic lupus.

Barber DF, Bartolomé A, Hernandez C, Flores JM, Redondo C, Fernandez-Arias C, Camps M, Rückle T, Schwarz MK, Rodríguez S, Martinez-A C, Balomenos D, Rommel C, Carrera AC.

Nat Med. 2005 Sep;11(9):933-5. Epub 2005 Aug 28.

32.

Sequential activation of class IB and class IA PI3K is important for the primed respiratory burst of human but not murine neutrophils.

Condliffe AM, Davidson K, Anderson KE, Ellson CD, Crabbe T, Okkenhaug K, Vanhaesebroeck B, Turner M, Webb L, Wymann MP, Hirsch E, Ruckle T, Camps M, Rommel C, Jackson SP, Chilvers ER, Stephens LR, Hawkins PT.

Blood. 2005 Aug 15;106(4):1432-40. Epub 2005 May 5.

33.

Design, synthesis, and biological activity of novel, potent, and selective (benzoylaminomethyl)thiophene sulfonamide inhibitors of c-Jun-N-terminal kinase.

Rückle T, Biamonte M, Grippi-Vallotton T, Arkinstall S, Cambet Y, Camps M, Chabert C, Church DJ, Halazy S, Jiang X, Martinou I, Nichols A, Sauer W, Gotteland JP.

J Med Chem. 2004 Dec 30;47(27):6921-34.

PMID:
15615541
34.

Chemokine inhibition--why, when, where, which and how?

Johnson Z, Power CA, Weiss C, Rintelen F, Ji H, Ruckle T, Camps M, Wells TN, Schwarz MK, Proudfoot AE, Rommel C.

Biochem Soc Trans. 2004 Apr;32(Pt 2):366-77. Review.

PMID:
15046611
35.

Pharmacological profiles of peptide drug candidates for the treatment of Alzheimer's disease.

Adessi C, Frossard MJ, Boissard C, Fraga S, Bieler S, Ruckle T, Vilbois F, Robinson SM, Mutter M, Banks WA, Soto C.

J Biol Chem. 2003 Apr 18;278(16):13905-11. Epub 2003 Feb 10.

36.

Mapping of synergistic components of weakly interacting protein-protein motifs using arrays of paired peptides.

Espanel X, Wälchli S, Rückle T, Harrenga A, Huguenin-Reggiani M, Hooft van Huijsduijnen R.

J Biol Chem. 2003 Apr 25;278(17):15162-7. Epub 2003 Jan 27.

37.

Crystal structure of a synthetic cyclodecapeptide for template-assembled synthetic protein design.

Peluso S, Rückle T, Lehmann C, Mutter M, Peggion C, Crisma M.

Chembiochem. 2001 Jun 1;2(6):432-7.

PMID:
11828474

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