BIOMARKERS

Molecular Biopsy of Human Tumors

- a resource for Precision Medicine *

266 related articles for article (PubMed ID: 25402320)

  • 1. Discovery of (2S)-8-[(3R)-3-methylmorpholin-4-yl]-1-(3-methyl-2-oxobutyl)-2-(trifluoromethyl)-3,4-dihydro-2H-pyrimido[1,2-a]pyrimidin-6-one: a novel potent and selective inhibitor of Vps34 for the treatment of solid tumors.
    Pasquier B; El-Ahmad Y; Filoche-Rommé B; Dureuil C; Fassy F; Abecassis PY; Mathieu M; Bertrand T; Benard T; Barrière C; El Batti S; Letallec JP; Sonnefraud V; Brollo M; Delbarre L; Loyau V; Pilorge F; Bertin L; Richepin P; Arigon J; Labrosse JR; Clément J; Durand F; Combet R; Perraut P; Leroy V; Gay F; Lefrançois D; Bretin F; Marquette JP; Michot N; Caron A; Castell C; Schio L; McCort G; Goulaouic H; Garcia-Echeverria C; Ronan B
    J Med Chem; 2015 Jan; 58(1):376-400. PubMed ID: 25402320
    [TBL] [Abstract][Full Text] [Related]  

  • 2. Discovery and optimization of pyrimidone indoline amide PI3Kβ inhibitors for the treatment of phosphatase and tensin homologue (PTEN)-deficient cancers.
    Certal V; Carry JC; Halley F; Virone-Oddos A; Thompson F; Filoche-Rommé B; El-Ahmad Y; Karlsson A; Charrier V; Delorme C; Rak A; Abecassis PY; Amara C; Vincent L; Bonnevaux H; Nicolas JP; Mathieu M; Bertrand T; Marquette JP; Michot N; Benard T; Perrin MA; Lemaitre O; Guerif S; Perron S; Monget S; Gruss-Leleu F; Doerflinger G; Guizani H; Brollo M; Delbarre L; Bertin L; Richepin P; Loyau V; Garcia-Echeverria C; Lengauer C; Schio L
    J Med Chem; 2014 Feb; 57(3):903-20. PubMed ID: 24387221
    [TBL] [Abstract][Full Text] [Related]  

  • 3. A highly potent and selective Vps34 inhibitor alters vesicle trafficking and autophagy.
    Ronan B; Flamand O; Vescovi L; Dureuil C; Durand L; Fassy F; Bachelot MF; Lamberton A; Mathieu M; Bertrand T; Marquette JP; El-Ahmad Y; Filoche-Romme B; Schio L; Garcia-Echeverria C; Goulaouic H; Pasquier B
    Nat Chem Biol; 2014 Dec; 10(12):1013-9. PubMed ID: 25326666
    [TBL] [Abstract][Full Text] [Related]  

  • 4. In Vitro Characterization of VPS34 Lipid Kinase Inhibition by Small Molecules.
    Fassy F; Dureuil C; Lamberton A; Mathieu M; Michot N; Ronan B; Pasquier B
    Methods Enzymol; 2017; 587():447-464. PubMed ID: 28253972
    [TBL] [Abstract][Full Text] [Related]  

  • 5. 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; 55(10):4788-805. PubMed ID: 22524426
    [TBL] [Abstract][Full Text] [Related]  

  • 6. Targeting the Autophagy Specific Lipid Kinase VPS34 for Cancer Treatment: An Integrative Repurposing Strategy.
    Murali P; Verma K; Rungrotmongkol T; Thangavelu P; Karuppasamy R
    Protein J; 2021 Feb; 40(1):41-53. PubMed ID: 33400087
    [TBL] [Abstract][Full Text] [Related]  

  • 7. Preparation and optimization of new 4-(morpholin-4-yl)-(6-oxo-1,6-dihydropyrimidin-2-yl)amide derivatives as PI3Kβ inhibitors.
    Certal V; Halley F; Virone-Oddos A; Thompson F; Filoche-Rommé B; El-Ahmad Y; Carry JC; Delorme C; Karlsson A; Abecassis PY; Vincent L; Bonnevaux H; Nicolas JP; Morales R; Michot N; Vade I; Louboutin A; Perron S; Doerflinger G; Tric B; Monget S; Lengauer C; Schio L
    Bioorg Med Chem Lett; 2012 Oct; 22(20):6381-4. PubMed ID: 22981333
    [TBL] [Abstract][Full Text] [Related]  

  • 8. Simultaneous inhibition of Vps34 kinase would enhance PI3Kδ inhibitor cytotoxicity in the B-cell malignancies.
    Liu X; Wang A; Liang X; Liu J; Zou F; Chen C; Zhao Z; Deng Y; Wu H; Qi Z; Wang B; Wang L; Liu F; Xu Y; Wang W; Fernandes SM; Stone RM; Galinsky IA; Brown JR; Loh T; Griffin JD; Zhang S; Weisberg EL; Zhang X; Liu J; Liu Q
    Oncotarget; 2016 Aug; 7(33):53515-53525. PubMed ID: 27447747
    [TBL] [Abstract][Full Text] [Related]  

  • 9. SAR405, a PIK3C3/Vps34 inhibitor that prevents autophagy and synergizes with MTOR inhibition in tumor cells.
    Pasquier B
    Autophagy; 2015 Apr; 11(4):725-6. PubMed ID: 25905679
    [TBL] [Abstract][Full Text] [Related]  

  • 10. Optimization of Orally Bioavailable PI3Kδ Inhibitors and Identification of Vps34 as a Key Selectivity Target.
    Henley ZA; Amour A; Barton N; Bantscheff M; Bergamini G; Bertrand SM; Convery M; Down K; Dümpelfeld B; Edwards CD; Grandi P; Gore PM; Keeling S; Livia S; Mallett D; Maxwell A; Price M; Rau C; Reinhard FBM; Rowedder J; Rowland P; Taylor JA; Thomas DA; Hessel EM; Hamblin JN
    J Med Chem; 2020 Jan; 63(2):638-655. PubMed ID: 31855425
    [TBL] [Abstract][Full Text] [Related]  

  • 11. Targeting autophagy by small molecule inhibitors of vacuolar protein sorting 34 (Vps34) improves the sensitivity of breast cancer cells to Sunitinib.
    Dyczynski M; Yu Y; Otrocka M; Parpal S; Braga T; Henley AB; Zazzi H; Lerner M; Wennerberg K; Viklund J; Martinsson J; Grandér D; De Milito A; Pokrovskaja Tamm K
    Cancer Lett; 2018 Oct; 435():32-43. PubMed ID: 30055290
    [TBL] [Abstract][Full Text] [Related]  

  • 12. The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor agent.
    Sampson PB; Liu Y; Forrest B; Cumming G; Li SW; Patel NK; Edwards L; Laufer R; Feher M; Ban F; Awrey DE; Mao G; Plotnikova O; Hodgson R; Beletskaya I; Mason JM; Luo X; Nadeem V; Wei X; Kiarash R; Madeira B; Huang P; Mak TW; Pan G; Pauls HW
    J Med Chem; 2015 Jan; 58(1):147-69. PubMed ID: 25723005
    [TBL] [Abstract][Full Text] [Related]  

  • 13. Discovery of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): a potent and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity.
    Foote KM; Blades K; Cronin A; Fillery S; Guichard SS; Hassall L; Hickson I; Jacq X; Jewsbury PJ; McGuire TM; Nissink JW; Odedra R; Page K; Perkins P; Suleman A; Tam K; Thommes P; Broadhurst R; Wood C
    J Med Chem; 2013 Mar; 56(5):2125-38. PubMed ID: 23394205
    [TBL] [Abstract][Full Text] [Related]  

  • 14. Structure-Based Design of Potent, Selective, and Orally Bioavailable VPS34 Kinase Inhibitors.
    Hu DX; Patel S; Chen H; Wang S; Staben ST; Dimitrova YN; Wallweber HA; Lee JY; Chan GKY; Sneeringer CJ; Prangley MS; Moffat JG; Wu KC; Schutt LK; Salphati L; Pang J; McNamara E; Huang H; Chen Y; Wang Y; Zhao W; Lim J; Murthy A; Siu M
    J Med Chem; 2022 Sep; 65(17):11500-11512. PubMed ID: 34779204
    [TBL] [Abstract][Full Text] [Related]  

  • 15. 2-Substituted aminopyrido[2,3-d]pyrimidin-7(8H)-ones. structure-activity relationships against selected tyrosine kinases and in vitro and in vivo anticancer activity.
    Klutchko SR; Hamby JM; Boschelli DH; Wu Z; Kraker AJ; Amar AM; Hartl BG; Shen C; Klohs WD; Steinkampf RW; Driscoll DL; Nelson JM; Elliott WL; Roberts BJ; Stoner CL; Vincent PW; Dykes DJ; Panek RL; Lu GH; Major TC; Dahring TK; Hallak H; Bradford LA; Showalter HD; Doherty AM
    J Med Chem; 1998 Aug; 41(17):3276-92. PubMed ID: 9703473
    [TBL] [Abstract][Full Text] [Related]  

  • 16. Structure-based design of novel 2-amino-6-phenyl-pyrimido[5',4':5,6]pyrimido[1,2-a]benzimidazol-5(6H)-ones as potent and orally active inhibitors of lymphocyte specific kinase (Lck): synthesis, SAR, and in vivo anti-inflammatory activity.
    Martin MW; Newcomb J; Nunes JJ; Boucher C; Chai L; Epstein LF; Faust T; Flores S; Gallant P; Gore A; Gu Y; Hsieh F; Huang X; Kim JL; Middleton S; Morgenstern K; Oliveira-dos-Santos A; Patel VF; Powers D; Rose P; Tudor Y; Turci SM; Welcher AA; Zack D; Zhao H; Zhu L; Zhu X; Ghiron C; Ermann M; Johnston D; Saluste CG
    J Med Chem; 2008 Mar; 51(6):1637-48. PubMed ID: 18278858
    [TBL] [Abstract][Full Text] [Related]  

  • 17. Cinderella finds her shoe: the first Vps34 inhibitor uncovers a new PI3K-AGC protein kinase connection.
    Bilanges B; Vanhaesebroeck B
    Biochem J; 2014 Dec; 464(2):e7-10. PubMed ID: 25395352
    [TBL] [Abstract][Full Text] [Related]  

  • 18. The discovery of Polo-like kinase 4 inhibitors: design and optimization of spiro[cyclopropane-1,3'[3H]indol]-2'(1'H).ones as orally bioavailable antitumor agents.
    Sampson PB; Liu Y; Patel NK; Feher M; Forrest B; Li SW; Edwards L; Laufer R; Lang Y; Ban F; Awrey DE; Mao G; Plotnikova O; Leung G; Hodgson R; Mason JM; Wei X; Kiarash R; Green E; Qiu W; Chirgadze NY; Mak TW; Pan G; Pauls HW
    J Med Chem; 2015 Jan; 58(1):130-46. PubMed ID: 24867403
    [TBL] [Abstract][Full Text] [Related]  

  • 19. Beclin 1-ATG14L Protein-Protein Interaction Inhibitor Selectively Inhibits Autophagy through Disruption of VPS34 Complex I.
    Pavlinov I; Salkovski M; Aldrich LN
    J Am Chem Soc; 2020 May; 142(18):8174-8182. PubMed ID: 32320221
    [TBL] [Abstract][Full Text] [Related]  

  • 20. Design and Discovery of N-(2-Methyl-5'-morpholino-6'-((tetrahydro-2H-pyran-4-yl)oxy)-[3,3'-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide (RAF709): A Potent, Selective, and Efficacious RAF Inhibitor Targeting RAS Mutant Cancers.
    Nishiguchi GA; Rico A; Tanner H; Aversa RJ; Taft BR; Subramanian S; Setti L; Burger MT; Wan L; Tamez V; Smith A; Lou Y; Barsanti PA; Appleton BA; Mamo M; Tandeske L; Dix I; Tellew JE; Huang S; Mathews Griner LA; Cooke VG; Van Abbema A; Merritt H; Ma S; Gampa K; Feng F; Yuan J; Wang Y; Haling JR; Vaziri S; Hekmat-Nejad M; Jansen JM; Polyakov V; Zang R; Sethuraman V; Amiri P; Singh M; Lees E; Shao W; Stuart DD; Dillon MP; Ramurthy S
    J Med Chem; 2017 Jun; 60(12):4869-4881. PubMed ID: 28557458
    [TBL] [Abstract][Full Text] [Related]  

    [Next]    [New Search]
    of 14.