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Abstract 3345: ERAS-601, a potent inhibitor of SHP2, synergistically enhances the activity of a FLT3 inhibitor, gilteritinib, in FLT3-mutated AML tumor models

Autor: Leenus Martin, Roopal Patel, Jingchuan Zhang, Robin Nevarez, Taylor Congdon, Les Brail, Robert Shoemaker

Publikováno v: Cancer Research. 82:3345-3345

ERAS-601 is a potent, small molecule allosteric inhibitor of wildtype SHP2, a non-receptor protein tyrosine phosphatase (PTP) encoded by the PTPN11 gene. ERAS-601 inhibits wildtype SHP2 biochemically with an IC50 of 4.6 nM and demonstrates selectivit

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::d0080ecb628c7d3f0cbcb35c3c83753c
https://doi.org/10.1158/1538-7445.am2022-3345

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Abstract 2669: ERAS-007 (ERK inhibitor) + ERAS-601 (SHP2 inhibitor) exhibit nonclinical combination activity across KRAS mutated NSCLC, CRC, and PDAC tumor models

Autor: Leenus Martin, Erin D. Lew, Roopal Patel, Joanne Oh, Jingchuan Zhang, Robin Nevarez, Taylor Congdon, Wei Lin, Les Brail, Robert Shoemaker

Publikováno v: Cancer Research. 82:2669-2669

KRAS mutations occur in about 25% of all cancers and promote oncogenesis via constitutive activation of the RAS/MAPK pathway. Targeting KRAS mutant tumors by inhibiting individual nodes in the RAS/MAPK pathway, including SHP2, SOS1, KRAS, RAF, MEK, a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::60b038ca8f5fed99c0184034f96168a6
https://doi.org/10.1158/1538-7445.am2022-2669

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Abstract 2670: ERAS-601, a potent allosteric inhibitor of SHP2, synergistically enhances the efficacy of sotorasib/adagrasib and cetuximab in NSCLC, CRC, and HNSCC tumor models

Autor: Leenus Martin, Roopal Patel, Jingchuan Zhang, Robin Nevarez, Taylor Congdon, Les Brail, Robert Shoemaker

Publikováno v: Cancer Research. 82:2670-2670

ERAS-601 is a potent, small molecule allosteric inhibitor of wildtype SHP2, a non-receptor protein tyrosine phosphatase (PTP) encoded by the PTPN11 gene. ERAS-601 inhibits wild type SHP2 biochemically with an IC50 of 4.6 nM and demonstrates selectivi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::c90fa8e7628b87f728cb760e0cc35865
https://doi.org/10.1158/1538-7445.am2022-2670

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Abstract 2671: ERAS-601, a potent allosteric inhibitor of SHP2, demonstrates anti-tumor activity in RAS/MAPK-driven tumor models

Autor: Leenus Martin, Roopal Patel, Jingchuan Zhang, Jennifer Yang, Robin Nevarez, Taylor Congdon, Les Brail, Robert Shoemaker

Publikováno v: Cancer Research. 82:2671-2671

SHP2 is a non-receptor protein tyrosine phosphatase (PTP) encoded by the PTPN11 gene. SHP2 transduces upstream receptor tyrosine kinase (RTK) signaling to the RAS/MAPK pathway via its phosphatase-mediated regulation of guanine nucleotide exchange fac

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::84abeb7491994e27f8761c4f64de95a6
https://doi.org/10.1158/1538-7445.am2022-2671

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Phase I and Pharmacokinetic Study of LY293111, an Orally Bioavailable LTB4 Receptor Antagonist, in Patients With Advanced Solid Tumors

Autor: Ann Cleverly, Barbara Barile-Thiem, Aaron Weitzman, Daniel R. Budman, Dinesh P. de Alwis, Les Brail, Eileen M. O'Reilly, Gary K. Schwartz, Vincent Vinciguerra

Publikováno v: Journal of Clinical Oncology. 23:5365-5373

Purpose LY293111, a novel diaryl ether carboxylic acid derivative, is a potent and selective inhibitor of the lipoxygenase pathway either directly through 5′-lipoxygenase or via antagonism of the leukotriene B4 (LTB4) receptor. More recently it has

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::367ba0680951df892bf4a8356bbb89ec
https://doi.org/10.1200/jco.2005.02.766

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In Vivo Measurements of Tumor Metabolism and Growth after Administration of Enzastaurin Using Small Animal FDG Positron Emission Tomography

Autor: Ann M. McNulty, Michael Lahn, Nathan Enas, Les Brail, Karen E. Pollok, Donald Thornton, Jennifer R. Hartwell, Shanbao Cai, Jeremy R. Graff, Gary D. Hutchins, Aaron Ernstberger

Publikováno v: Journal of Oncology
Journal of Oncology, Vol 2009 (2009)

Background. The use of 2-[]fluoro-2-deoxy-D-glucose ([]FDG) may help to establish the antitumor activity of enzastaurin, a novel protein kinase C-beta II (PKC-II) inhibitor, in mouse xenografts.Methods. The hematologic cell line RAJI and the solid tu

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9fcbc2828b6206e185a8b0e249735468
http://europepmc.org/articles/PMC2688651

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