-
Combination of the MTA-Cooperative PRMT5 Inhibitor BMS-986504 and KRAS Inhibitors Is an Effective Treatment Strategy for MTAP-Deleted KRAS-Mutant Pancreatic Cancer. Cancer Res. 2025 Sep 15; 85(18):3540-3557.
Drizyte-Miller K, Engstrom LD, Klomp JA, Stalnecker CA, Stamey AG, Taylor KE, Roach MK, Robb R, Waters LM, Calinisan A, Degan S, Chang WH, Helu XM, Nguyen D, Baldelli E, Pierobon M, Petricoin EF, Briere DM, Hallin J, Christensen JG, Bryant KL, Cox AD, Olson P, Der CJ. PMID: 40694535.
View in:
PubMed Mentions: Fields:
Translation:
HumansAnimalsCells
-
Impact of Co-mutations and Transcriptional Signatures in Non-Small Cell Lung Cancer Patients Treated with Adagrasib in the KRYSTAL-1 Trial. Clin Cancer Res. 2025 Mar 17; 31(6):1069-1081.
Negrao MV, Paula AG, Molkentine D, Hover L, Nilsson M, Vokes N, Engstrom L, Calinisan A, Briere DM, Waters L, Hallin J, Diao L, Altan M, Blumenschein GR, Skoulidis F, Wang J, Kopetz SE, Hong DS, Gibbons DL, Olson P, Christensen JG, Heymach JV. PMID: 39804166; PMCID: PMC11911804.
View in:
PubMed Mentions:
5 Fields:
Translation:
HumansAnimalsCells
-
The SOS1 Inhibitor MRTX0902 Blocks KRAS Activation and Demonstrates Antitumor Activity in Cancers Dependent on KRAS Nucleotide Loading. Mol Cancer Ther. 2024 Oct 01; 23(10):1418-1430.
Sudhakar N, Yan L, Qiryaqos F, Engstrom LD, Laguer J, Calinisan A, Hebbert A, Waters L, Moya K, Bowcut V, Vegar L, Ketcham JM, Ivetac A, Smith CR, Lawson JD, Rahbaek L, Clarine J, Nguyen N, Saechao B, Parker C, Elliott AJ, Vanderpool D, He L, Hover LD, Fernandez-Banet J, Coma S, Pachter JA, Hallin J, Marx MA, Briere DM, Christensen JG, Olson P, Haling J, Khare S. PMID: 38904222; PMCID: PMC11443210.
View in:
PubMed Mentions:
8 Fields:
Translation:
HumansAnimalsCells
-
Discovery of Pyridopyrimidinones that Selectively Inhibit the H1047R PI3Kα Mutant Protein. J Med Chem. 2024 03 28; 67(6):4936-4949.
Ketcham JM, Harwood SJ, Aranda R, Aloiau AN, Bobek BM, Briere DM, Burns AC, Caddell Haatveit K, Calinisan A, Clarine J, Elliott A, Engstrom LD, Gunn RJ, Ivetac A, Jones B, Kuehler J, Lawson JD, Nguyen N, Parker C, Pearson KE, Rahbaek L, Saechao B, Wang X, Waters A, Waters L, Watkins AH, Olson P, Smith CR, Christensen JG, Marx MA. PMID: 38477582; PMCID: PMC10983000.
View in:
PubMed Mentions:
3 Fields:
Translation:
Animals
-
MRTX1719 Is an MTA-Cooperative PRMT5 Inhibitor That Exhibits Synthetic Lethality in Preclinical Models and Patients with MTAP-Deleted Cancer. Cancer Discov. 2023 11 01; 13(11):2412-2431.
Engstrom LD, Aranda R, Waters L, Moya K, Bowcut V, Vegar L, Trinh D, Hebbert A, Smith CR, Kulyk S, Lawson JD, He L, Hover LD, Fernandez-Banet J, Hallin J, Vanderpool D, Briere DM, Blaj A, Marx MA, Rodon J, Offin M, Arbour KC, Johnson ML, Kwiatkowski DJ, Jänne PA, Haddox CL, Papadopoulos KP, Henry JT, Leventakos K, Christensen JG, Shazer R, Olson P. PMID: 37552839; PMCID: PMC10618744.
View in:
PubMed Mentions:
59 Fields:
Translation:
HumansCellsCTClinical Trials
-
Anti-tumor efficacy of a potent and selective non-covalent KRASG12D inhibitor. Nat Med. 2022 Oct; 28(10):2171-2182.
Hallin J, Bowcut V, Calinisan A, Briere DM, Hargis L, Engstrom LD, Laguer J, Medwid J, Vanderpool D, Lifset E, Trinh D, Hoffman N, Wang X, David Lawson J, Gunn RJ, Smith CR, Thomas NC, Martinson M, Bergstrom A, Sullivan F, Bouhana K, Winski S, He L, Fernandez-Banet J, Pavlicek A, Haling JR, Rahbaek L, Marx MA, Olson P, Christensen JG. PMID: 36216931.
View in:
PubMed Mentions:
207 Fields:
Translation:
HumansCells
-
Design and Discovery of MRTX0902, a Potent, Selective, Brain-Penetrant, and Orally Bioavailable Inhibitor of the SOS1:KRAS Protein-Protein Interaction. J Med Chem. 2022 07 28; 65(14):9678-9690.
Ketcham JM, Haling J, Khare S, Bowcut V, Briere DM, Burns AC, Gunn RJ, Ivetac A, Kuehler J, Kulyk S, Laguer J, Lawson JD, Moya K, Nguyen N, Rahbaek L, Saechao B, Smith CR, Sudhakar N, Thomas NC, Vegar L, Vanderpool D, Wang X, Yan L, Olson P, Christensen JG, Marx MA. PMID: 35833726; PMCID: PMC9340770.
View in:
PubMed Mentions:
28 Fields:
Translation:
HumansAnimalsCells
-
Fragment-Based Discovery of MRTX1719, a Synthetic Lethal Inhibitor of the PRMT5•MTA Complex for the Treatment of MTAP-Deleted Cancers. J Med Chem. 2022 02 10; 65(3):1749-1766.
Smith CR, Aranda R, Bobinski TP, Briere DM, Burns AC, Christensen JG, Clarine J, Engstrom LD, Gunn RJ, Ivetac A, Jean-Baptiste R, Ketcham JM, Kobayashi M, Kuehler J, Kulyk S, Lawson JD, Moya K, Olson P, Rahbaek L, Thomas NC, Wang X, Waters LM, Marx MA. PMID: 35041419.
View in:
PubMed Mentions:
44 Fields:
Translation:
HumansAnimalsCells
-
Identification of MRTX1133, a Noncovalent, Potent, and Selective KRASG12D Inhibitor. J Med Chem. 2022 02 24; 65(4):3123-3133.
Wang X, Allen S, Blake JF, Bowcut V, Briere DM, Calinisan A, Dahlke JR, Fell JB, Fischer JP, Gunn RJ, Hallin J, Laguer J, Lawson JD, Medwid J, Newhouse B, Nguyen P, O'Leary JM, Olson P, Pajk S, Rahbaek L, Rodriguez M, Smith CR, Tang TP, Thomas NC, Vanderpool D, Vigers GP, Christensen JG, Marx MA. PMID: 34889605.
View in:
PubMed Mentions:
300 Fields:
Translation:
HumansAnimals
-
The KRASG12C Inhibitor MRTX849 Reconditions the Tumor Immune Microenvironment and Sensitizes Tumors to Checkpoint Inhibitor Therapy. Mol Cancer Ther. 2021 06; 20(6):975-985.
Briere DM, Li S, Calinisan A, Sudhakar N, Aranda R, Hargis L, Peng DH, Deng J, Engstrom LD, Hallin J, Gatto S, Fernandez-Banet J, Pavlicek A, Wong KK, Christensen JG, Olson P. PMID: 33722854; PMCID: PMC8444277.
View in:
PubMed Mentions:
92 Fields:
Translation:
HumansAnimalsCells
-
Identification of the Clinical Development Candidate MRTX849, a Covalent KRASG12C Inhibitor for the Treatment of Cancer. J Med Chem. 2020 07 09; 63(13):6679-6693.
Fell JB, Fischer JP, Baer BR, Blake JF, Bouhana K, Briere DM, Brown KD, Burgess LE, Burns AC, Burkard MR, Chiang H, Chicarelli MJ, Cook AW, Gaudino JJ, Hallin J, Hanson L, Hartley DP, Hicken EJ, Hingorani GP, Hinklin RJ, Mejia MJ, Olson P, Otten JN, Rhodes SP, Rodriguez ME, Savechenkov P, Smith DJ, Sudhakar N, Sullivan FX, Tang TP, Vigers GP, Wollenberg L, Christensen JG, Marx MA. PMID: 32250617.
View in:
PubMed Mentions:
226 Fields:
Translation:
HumansAnimalsCells
-
The KRASG12C Inhibitor MRTX849 Provides Insight toward Therapeutic Susceptibility of KRAS-Mutant Cancers in Mouse Models and Patients. Cancer Discov. 2020 01; 10(1):54-71.
Hallin J, Engstrom LD, Hargis L, Calinisan A, Aranda R, Briere DM, Sudhakar N, Bowcut V, Baer BR, Ballard JA, Burkard MR, Fell JB, Fischer JP, Vigers GP, Xue Y, Gatto S, Fernandez-Banet J, Pavlicek A, Velastagui K, Chao RC, Barton J, Pierobon M, Baldelli E, Patricoin EF, Cassidy DP, Marx MA, Rybkin II, Johnson ML, Ou SI, Lito P, Papadopoulos KP, Jänne PA, Olson P, Christensen JG. PMID: 31658955; PMCID: PMC6954325.
View in:
PubMed Mentions:
648 Fields:
Translation:
HumansAnimalsCells
-
Discovery of Tetrahydropyridopyrimidines as Irreversible Covalent Inhibitors of KRAS-G12C with In Vivo Activity. ACS Med Chem Lett. 2018 Dec 13; 9(12):1230-1234.
Fell JB, Fischer JP, Baer BR, Ballard J, Blake JF, Bouhana K, Brandhuber BJ, Briere DM, Burgess LE, Burkard MR, Chiang H, Chicarelli MJ, Davidson K, Gaudino JJ, Hallin J, Hanson L, Hee K, Hicken EJ, Hinklin RJ, Marx MA, Mejia MJ, Olson P, Savechenkov P, Sudhakar N, Tang TP, Vigers GP, Zecca H, Christensen JG. PMID: 30613331; PMCID: PMC6295846.
View in:
PubMed Mentions:
40
-
The class I/IV HDAC inhibitor mocetinostat increases tumor antigen presentation, decreases immune suppressive cell types and augments checkpoint inhibitor therapy. Cancer Immunol Immunother. 2018 03; 67(3):381-392.
Briere D, Sudhakar N, Woods DM, Hallin J, Engstrom LD, Aranda R, Chiang H, Sodré AL, Olson P, Weber JS, Christensen JG. PMID: 29124315; PMCID: PMC11028326.
View in:
PubMed Mentions:
84 Fields:
Translation:
HumansAnimalsCells
-
Glesatinib Exhibits Antitumor Activity in Lung Cancer Models and Patients Harboring MET Exon 14 Mutations and Overcomes Mutation-mediated Resistance to Type I MET Inhibitors in Nonclinical Models. Clin Cancer Res. 2017 Nov 01; 23(21):6661-6672.
Engstrom LD, Aranda R, Lee M, Tovar EA, Essenburg CJ, Madaj Z, Chiang H, Briere D, Hallin J, Lopez-Casas PP, Baños N, Menendez C, Hidalgo M, Tassell V, Chao R, Chudova DI, Lanman RB, Olson P, Bazhenova L, Patel SP, Graveel C, Nishino M, Shapiro GI, Peled N, Awad MM, Jänne PA, Christensen JG. PMID: 28765324.
-
A novel antiandrogen, Compound 30, suppresses castration-resistant and MDV3100-resistant prostate cancer growth in vitro and in vivo. Mol Cancer Ther. 2013 May; 12(5):567-76.
Kuruma H, Matsumoto H, Shiota M, Bishop J, Lamoureux F, Thomas C, Briere D, Los G, Gleave M, Fanjul A, Zoubeidi A. PMID: 23493310.
View in:
PubMed Mentions:
62 Fields:
Translation:
HumansAnimalsCells
-
Dose-dependent effects of small-molecule antagonists on the genomic landscape of androgen receptor binding. BMC Genomics. 2012 Jul 31; 13:355.
Zhu Z, Shi M, Hu W, Estrella H, Engebretsen J, Nichols T, Briere D, Hosea N, Los G, Rejto PA, Fanjul A. PMID: 22849360; PMCID: PMC3507642.
View in:
PubMed Mentions:
6 Fields:
Translation:
HumansAnimalsCells
-
Discovery of aryloxy tetramethylcyclobutanes as novel androgen receptor antagonists. J Med Chem. 2011 Nov 10; 54(21):7693-704.
Guo C, Linton A, Kephart S, Ornelas M, Pairish M, Gonzalez J, Greasley S, Nagata A, Burke BJ, Edwards M, Hosea N, Kang P, Hu W, Engebretsen J, Briere D, Shi M, Gukasyan H, Richardson P, Dack K, Underwood T, Johnson P, Morell A, Felstead R, Kuruma H, Matsimoto H, Zoubeidi A, Gleave M, Los G, Fanjul AN. PMID: 21936524.
View in:
PubMed Mentions:
22 Fields:
Translation:
HumansAnimalsCells
-
Design of selective, ATP-competitive inhibitors of Akt. J Med Chem. 2010 Jun 24; 53(12):4615-22.
Freeman-Cook KD, Autry C, Borzillo G, Gordon D, Barbacci-Tobin E, Bernardo V, Briere D, Clark T, Corbett M, Jakubczak J, Kakar S, Knauth E, Lippa B, Luzzio MJ, Mansour M, Martinelli G, Marx M, Nelson K, Pandit J, Rajamohan F, Robinson S, Subramanyam C, Wei L, Wythes M, Morris J. PMID: 20481595.
View in:
PubMed Mentions:
24 Fields:
Translation:
AnimalsCells
-
PF-03814735, an orally bioavailable small molecule aurora kinase inhibitor for cancer therapy. Mol Cancer Ther. 2010 Apr; 9(4):883-94.
Jani JP, Arcari J, Bernardo V, Bhattacharya SK, Briere D, Cohen BD, Coleman K, Christensen JG, Emerson EO, Jakowski A, Hook K, Los G, Moyer JD, Pruimboom-Brees I, Pustilnik L, Rossi AM, Steyn SJ, Su C, Tsaparikos K, Wishka D, Yoon K, Jakubczak JL. PMID: 20354118.
View in:
PubMed Mentions:
42 Fields:
Translation:
HumansAnimalsCells