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Page 1
Identification of Novel, Selective Ataxia-Telangiectasia Mutated Kinase Inhibitors with the Ability to Penetrate the Blood-Brain Barrier: The Discovery of AZD1390.
Pike KG, Hunt TA, Barlaam B, Benstead D, Cadogan E, Chen K, Cook CR, Colclough N, Deng C, Durant ST, Eatherton A, Goldberg K, Johnström P, Liu L, Liu Z, Nissink JWM, Pang C, Pass M, Robb GR, Roberts C, Schou M, Steward O, Sykes A, Yan Y, Zhai B, Zheng L. Pike KG, et al. Among authors: pass m. J Med Chem. 2024 Feb 22;67(4):3090-3111. doi: 10.1021/acs.jmedchem.3c02277. Epub 2024 Feb 2. J Med Chem. 2024. PMID: 38306388
The Identification of Potent, Selective, and Orally Available Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase: The Discovery of AZD0156 (8-{6-[3-(Dimethylamino)propoxy]pyridin-3-yl}-3-methyl-1-(tetrahydro-2 H-pyran-4-yl)-1,3-dihydro-2 H-imidazo[4,5- c]quinolin-2-one).
Pike KG, Barlaam B, Cadogan E, Campbell A, Chen Y, Colclough N, Davies NL, de-Almeida C, Degorce SL, Didelot M, Dishington A, Ducray R, Durant ST, Hassall LA, Holmes J, Hughes GD, MacFaul PA, Mulholland KR, McGuire TM, Ouvry G, Pass M, Robb G, Stratton N, Wang Z, Wilson J, Zhai B, Zhao K, Al-Huniti N. Pike KG, et al. Among authors: pass m. J Med Chem. 2018 May 10;61(9):3823-3841. doi: 10.1021/acs.jmedchem.7b01896. Epub 2018 May 2. J Med Chem. 2018. PMID: 29683659
Discovery of a Series of 3-Cinnoline Carboxamides as Orally Bioavailable, Highly Potent, and Selective ATM Inhibitors.
Barlaam B, Cadogan E, Campbell A, Colclough N, Dishington A, Durant S, Goldberg K, Hassall LA, Hughes GD, MacFaul PA, McGuire TM, Pass M, Patel A, Pearson S, Petersen J, Pike KG, Robb G, Stratton N, Xin G, Zhai B. Barlaam B, et al. Among authors: pass m. ACS Med Chem Lett. 2018 Jul 13;9(8):809-814. doi: 10.1021/acsmedchemlett.8b00200. eCollection 2018 Aug 9. ACS Med Chem Lett. 2018. PMID: 30128072 Free PMC article.
The brain-penetrant clinical ATM inhibitor AZD1390 radiosensitizes and improves survival of preclinical brain tumor models.
Durant ST, Zheng L, Wang Y, Chen K, Zhang L, Zhang T, Yang Z, Riches L, Trinidad AG, Fok JHL, Hunt T, Pike KG, Wilson J, Smith A, Colclough N, Reddy VP, Sykes A, Janefeldt A, Johnström P, Varnäs K, Takano A, Ling S, Orme J, Stott J, Roberts C, Barrett I, Jones G, Roudier M, Pierce A, Allen J, Kahn J, Sule A, Karlin J, Cronin A, Chapman M, Valerie K, Illingworth R, Pass M. Durant ST, et al. Among authors: pass m. Sci Adv. 2018 Jun 20;4(6):eaat1719. doi: 10.1126/sciadv.aat1719. eCollection 2018 Jun. Sci Adv. 2018. PMID: 29938225 Free PMC article.
Discovery of AZD3147: a potent, selective dual inhibitor of mTORC1 and mTORC2.
Pike KG, Morris J, Ruston L, Pass SL, Greenwood R, Williams EJ, Demeritt J, Culshaw JD, Gill K, Pass M, Finlay MR, Good CJ, Roberts CA, Currie GS, Blades K, Eden JM, Pearson SE. Pike KG, et al. Among authors: pass sl, pass m. J Med Chem. 2015 Mar 12;58(5):2326-49. doi: 10.1021/jm501778s. Epub 2015 Feb 18. J Med Chem. 2015. PMID: 25643210
Orally Bioavailable and Blood-Brain Barrier-Penetrating ATM Inhibitor (AZ32) Radiosensitizes Intracranial Gliomas in Mice.
Karlin J, Allen J, Ahmad SF, Hughes G, Sheridan V, Odedra R, Farrington P, Cadogan EB, Riches LC, Garcia-Trinidad A, Thomason AG, Patel B, Vincent J, Lau A, Pike KG, Hunt TA, Sule A, Valerie NCK, Biddlestone-Thorpe L, Kahn J, Beckta JM, Mukhopadhyay N, Barlaam B, Degorce SL, Kettle J, Colclough N, Wilson J, Smith A, Barrett IP, Zheng L, Zhang T, Wang Y, Chen K, Pass M, Durant ST, Valerie K. Karlin J, et al. Among authors: pass m. Mol Cancer Ther. 2018 Aug;17(8):1637-1647. doi: 10.1158/1535-7163.MCT-17-0975. Epub 2018 May 16. Mol Cancer Ther. 2018. PMID: 29769307 Free PMC article.
Brain exposure of the ATM inhibitor AZD1390 in humans-a positron emission tomography study.
Jucaite A, Stenkrona P, Cselényi Z, De Vita S, Buil-Bruna N, Varnäs K, Savage A, Varrone A, Johnström P, Schou M, Davison C, Sykes A, Pilla Reddy V, Hoch M, Vazquez-Romero A, Moein MM, Halldin C, Merchant MS, Pass M, Farde L. Jucaite A, et al. Among authors: pass m. Neuro Oncol. 2021 Apr 12;23(4):687-696. doi: 10.1093/neuonc/noaa238. Neuro Oncol. 2021. PMID: 33123736 Free PMC article. Clinical Trial.
Pharmacology of the ATM Inhibitor AZD0156: Potentiation of Irradiation and Olaparib Responses Preclinically.
Riches LC, Trinidad AG, Hughes G, Jones GN, Hughes AM, Thomason AG, Gavine P, Cui A, Ling S, Stott J, Clark R, Peel S, Gill P, Goodwin LM, Smith A, Pike KG, Barlaam B, Pass M, O'Connor MJ, Smith G, Cadogan EB. Riches LC, et al. Among authors: pass m. Mol Cancer Ther. 2020 Jan;19(1):13-25. doi: 10.1158/1535-7163.MCT-18-1394. Epub 2019 Sep 18. Mol Cancer Ther. 2020. PMID: 31534013
Discovery of 4-amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide (AZD5363), an orally bioavailable, potent inhibitor of Akt kinases.
Addie M, Ballard P, Buttar D, Crafter C, Currie G, Davies BR, Debreczeni J, Dry H, Dudley P, Greenwood R, Johnson PD, Kettle JG, Lane C, Lamont G, Leach A, Luke RW, Morris J, Ogilvie D, Page K, Pass M, Pearson S, Ruston L. Addie M, et al. Among authors: pass m. J Med Chem. 2013 Mar 14;56(5):2059-73. doi: 10.1021/jm301762v. Epub 2013 Feb 26. J Med Chem. 2013. PMID: 23394218
154 results