Search Results - "Manro, Jason R"
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The Folate Pathway Inhibitor Pemetrexed Pleiotropically Enhances Effects of Cancer Immunotherapy
Published in Clinical cancer research (01-12-2019)“…Combination strategies leveraging chemotherapeutic agents and immunotherapy have held the promise as a method to improve benefit for patients with cancer…”
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Targeting the TGFβ pathway with galunisertib, a TGFβRI small molecule inhibitor, promotes anti-tumor immunity leading to durable, complete responses, as monotherapy and in combination with checkpoint blockade
Published in Journal for immunotherapy of cancer (04-06-2018)“…TGFβ signaling plays a pleotropic role in tumor biology, promoting tumor proliferation, invasion and metastasis, and escape from immune surveillance…”
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Activating the Wnt/β-Catenin Pathway for the Treatment of Melanoma--Application of LY2090314, a Novel Selective Inhibitor of Glycogen Synthase Kinase-3
Published in PloS one (27-04-2015)“…It has previously been observed that a loss of β-catenin expression occurs with melanoma progression and that nuclear β-catenin levels are inversely…”
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Treatment with a VEGFR-2 antibody results in intra-tumor immune modulation and enhances anti-tumor efficacy of PD-L1 blockade in syngeneic murine tumor models
Published in PloS one (18-07-2022)“…Prolonged activation of vascular endothelial growth factor receptor-2 (VEGFR-2) due to mis-regulation of the VEGF pathway induces aberrant blood vessel…”
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Developmental expression of the major human hepatic CYP3A enzymes
Published in The Journal of pharmacology and experimental therapeutics (01-11-2003)“…The human cytochrome P4503A forms show expression patterns subject to developmental influence. CYP3A7 and CYP3A4 are generally classified as the major fetal…”
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Developmental expression of human hepatic CYP2C9 and CYP2C19
Published in The Journal of pharmacology and experimental therapeutics (01-03-2004)“…The CYP2C subfamily is responsible for metabolizing many important drugs and accounts for about 20% of the cytochrome p450 in adult liver. To determine…”
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Preclinical assessment of galunisertib (LY2157299 monohydrate), a first-in-class transforming growth factor-β receptor type I inhibitor
Published in Oncotarget (23-01-2018)“…Transforming growth factor-β (TGFβ) is an important driver of tumor growth via intrinsic and extrinsic mechanisms, and is therefore an attractive target for…”
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LY2875358, a neutralizing and internalizing anti-MET bivalent antibody, inhibits HGF-dependent and HGF-independent MET activation and tumor growth
Published in Clinical cancer research (01-12-2014)“…MET, the receptor for hepatocyte growth factor (HGF), has been implicated in driving tumor proliferation and metastasis. High MET expression is correlated with…”
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Utility of Oatp1a/1b-knockout and OATP1B1/3-humanized mice in the study of OATP-mediated pharmacokinetics and tissue distribution: case studies with pravastatin, atorvastatin, simvastatin, and carboxydichlorofluorescein
Published in Drug metabolism and disposition (01-01-2014)“…Although organic anion transporting polypeptide (OATP)-mediated hepatic uptake is generally conserved between rodents and humans at a gross pharmacokinetic…”
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ERK Inhibitor LY3214996-Based Treatment Strategies for RAS -Driven Lung Cancer
Published in Molecular cancer therapeutics (01-04-2021)“…gene mutations are the most frequent oncogenic event in lung cancer. They activate multiple RAS-centric signaling networks among them the MAPK, PI3K, and RB…”
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Aurora A-Selective Inhibitor LY3295668 Leads to Dominant Mitotic Arrest, Apoptosis in Cancer Cells, and Shows Potent Preclinical Antitumor Efficacy
Published in Molecular cancer therapeutics (01-12-2019)“…Although Aurora A, B, and C kinases share high sequence similarity, especially within the kinase domain, they function distinctly in cell-cycle progression…”
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MET-targeting antibody (emibetuzumab) and kinase inhibitor (merestinib) as single agent or in combination in a cancer model bearing MET exon 14 skipping
Published in Investigational new drugs (01-08-2018)“…Summary Purpose Approximately 3% of lung cancer bears mutations leading to MET exon 14 skipping, an oncogenic driver which is further evidenced by case reports…”
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Inhibition of Tumor Growth and Metastasis in Non―Small Cell Lung Cancer by LY2801653, an Inhibitor of Several Oncokinases, Including MET
Published in Clinical cancer research (15-10-2013)“…Lung cancer is the leading cause of cancer-related death worldwide. Sustained activation, overexpression, or mutation of the MET pathway is associated with a…”
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LY2801653 is an orally bioavailable multi-kinase inhibitor with potent activity against MET, MST1R, and other oncoproteins, and displays anti-tumor activities in mouse xenograft models
Published in Investigational new drugs (01-08-2013)“…Summary The HGF/MET signaling pathway regulates a wide variety of normal cellular functions that can be subverted to support neoplasia, including cell…”
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Preclinical bridging studies: understanding dried blood spot and plasma exposure profiles
Published in Bioanalysis (01-01-2013)“…Understanding the distribution of the analyte between the cellular and noncellular (plasma) components of the blood is important, especially in situations…”
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How well do lipophilicity parameters, MEEKC microemulsion capacity factor, and plasma protein binding predict CNS tissue binding?
Published in Journal of pharmaceutical sciences (01-05-2012)“…Brain fraction unbound (Fu) is critical to understanding the pharmacokinetics/dynamics of central nervous system (CNS) drugs, thus several surrogate predictors…”
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Pharmacological characterization of cGMP regulation by the biarylpropylsulfonamide class of positive, allosteric modulators of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors
Published in The Journal of pharmacology and experimental therapeutics (01-10-2006)“…The biarylpropylsulfonamide class of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) potentiators represented by…”
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Abstract 1236: Preclinical characterization of LY3484356, a novel, potent and orally bioavailable selective estrogen receptor degrader (SERD)
Published in Cancer research (Chicago, Ill.) (01-07-2021)“…Abstract Nearly 70% of newly diagnosed breast cancers are estrogen receptor alpha (ERα) positive, for which endocrine therapy is a primary treatment. However,…”
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Abstract A160: Combination of necitumumab with second- or third-generation EGFR tyrosine kinase inhibitors downregulates DNA repair mechanisms and induces durable tumor remissions in xenograft NSCLC models with EGFR mutations
Published in Molecular cancer therapeutics (01-01-2018)“…Abstract First- , second- , and third-generation EGFR tyrosine kinase inhibitors (TKIs) demonstrate profound tumor responses in EGFR mutation-positive NSCLC…”
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Abstract B108: Antitumor efficacy of EGFR antibody necitumumab and dual PI3K/mTOR inhibitor (LY3023414) in preclinical tumor models
Published in Molecular cancer therapeutics (01-01-2018)“…Abstract Necitumumab (Nmab) in combination with chemotherapy has demonstrated overall survival benefit in patients with advanced or metastatic squamous…”
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