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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: durant s. 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 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. 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
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. 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.
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. Sci Adv. 2018 Jun 20;4(6):eaat1719. doi: 10.1126/sciadv.aat1719. eCollection 2018 Jun. Sci Adv. 2018. PMID: 29938225 Free PMC article.
ATM Regulates Differentiation of Myofibroblastic Cancer-Associated Fibroblasts and Can Be Targeted to Overcome Immunotherapy Resistance.
Mellone M, Piotrowska K, Venturi G, James L, Bzura A, Lopez MA, James S, Wang C, Ellis MJ, Hanley CJ, Buckingham JF, Cox KL, Hughes G, Valge-Archer V, King EV, Beers SA, Jaquet V, Jones GDD, Savelyeva N, Sayan E, Parsons JL, Durant S, Thomas GJ. Mellone M, et al. Among authors: durant s. Cancer Res. 2022 Dec 16;82(24):4571-4585. doi: 10.1158/0008-5472.CAN-22-0435. Cancer Res. 2022. PMID: 36353752 Free PMC article.
Targeting DNA damage response components induces enhanced STING-dependent type-I IFN response in ATM deficient cancer cells and drives dendritic cell activation.
Lopez-Pelaez M, Young L, Vazquez-Chantada M, Nelson N, Durant S, Wilkinson RW, Poon E, Gaspar M, Valge-Archer V, Smith P, Dovedi SJ. Lopez-Pelaez M, et al. Among authors: durant s. Oncoimmunology. 2022 Sep 13;11(1):2117321. doi: 10.1080/2162402X.2022.2117321. eCollection 2022. Oncoimmunology. 2022. PMID: 36117525 Free PMC article.
230 results