Search Results - "Raymon, Heather K"
-
1
CC-115, a dual inhibitor of mTOR kinase and DNA-PK, blocks DNA damage repair pathways and selectively inhibits ATM-deficient cell growth in vitro
Published in Oncotarget (26-09-2017)“…CC-115, a selective dual inhibitor of the mammalian target of rapamycin (mTOR) kinase and DNA-dependent protein kinase (DNA-PK), is undergoing Phase 1 clinical…”
Get full text
Journal Article -
2
The mTOR Kinase Inhibitors, CC214-1 and CC214-2, Preferentially Block the Growth of EGFRvIII-Activated Glioblastomas
Published in Clinical cancer research (15-10-2013)“…mTOR pathway hyperactivation occurs in approximately 90% of glioblastomas, but the allosteric mTOR inhibitor rapamycin has failed in the clinic. Here, we…”
Get full text
Journal Article -
3
1,1-Diarylalkenes as anticancer agents: Dual inhibitors of tubulin polymerization and phosphodiesterase 4
Published in Bioorganic & medicinal chemistry (01-11-2011)“…A series of 1,1-diarylalkene derivatives were prepared to optimize the properties of CC-5079 (1), a dual inhibitor of tubulin polymerization and…”
Get full text
Journal Article -
4
An activin receptor IIA ligand trap promotes erythropoiesis resulting in a rapid induction of red blood cells and haemoglobin
Published in British journal of haematology (01-06-2014)“…Summary Sotatercept (ACE‐011), a recombinant human fusion protein containing the extracellular domain of the human Activin receptor IIA, binds to and inhibits…”
Get full text
Journal Article -
5
Modulation of CD47-SIRPα innate immune checkpoint axis with Fc-function detuned anti-CD47 therapeutic antibody
Published in Cancer Immunology, Immunotherapy (01-02-2022)“…Cluster of differentiation 47 (CD47) is a transmembrane protein ubiquitously expressed on human cells but overexpressed on many different tumor cells. The…”
Get full text
Journal Article -
6
Synthetic Lethal Strategy Identifies a Potent and Selective TTK and CLK1/2 Inhibitor for Treatment of Triple-Negative Breast Cancer with a Compromised G1–S Checkpoint
Published in Molecular cancer therapeutics (01-08-2018)“…Abstract Historically, phenotypic-based drug discovery has yielded a high percentage of novel drugs while uncovering new tumor biology. CC-671 was discovered…”
Get full text
Journal Article -
7
Synthetic Lethal Strategy Identifies a Potent and Selective TTK and CLK1/2 Inhibitor for Treatment of Triple-Negative Breast Cancer with a Compromised G 1 -S Checkpoint
Published in Molecular cancer therapeutics (01-08-2018)“…Historically, phenotypic-based drug discovery has yielded a high percentage of novel drugs while uncovering new tumor biology. CC-671 was discovered using a…”
Get full text
Journal Article -
8
Pomalidomide in combination with dexamethasone results in synergistic anti‐tumour responses in pre‐clinical models of lenalidomide‐resistant multiple myeloma
Published in British journal of haematology (01-03-2016)“…Summary Pomalidomide is an IMiD® immunomodulatory agent, which has shown clinically significant benefits in relapsed and/or refractory multiple myeloma (rrMM)…”
Get full text
Journal Article -
9
Pleiotropic Impact of DNA-PK in Cancer and Implications for Therapeutic Strategies
Published in Clinical cancer research (15-09-2019)“…DNA-dependent protein kinase catalytic subunit (DNA-PK) is a pleiotropic kinase involved in DNA repair and transcriptional regulation. DNA-PK is deregulated in…”
Get full text
Journal Article -
10
CC-223, a Potent and Selective Inhibitor of mTOR Kinase: In Vitro and In Vivo Characterization
Published in Molecular cancer therapeutics (01-06-2015)“…mTOR is a serine/threonine kinase that regulates cell growth, metabolism, proliferation, and survival. mTOR complex-1 (mTORC1) and mTOR complex-2 (mTORC2) are…”
Get full text
Journal Article -
11
Basic fibroblast growth factor increases dopaminergic graft survival and function in a rat model of Parkinson's disease
Published in Nature medicine (01-01-1995)“…The clinical use of fetal neural grafts as an intracerebral source of dopamine for patients with Parkinson's disease has met with limited success. Since basic…”
Get full text
Journal Article -
12
Effect of Mutant α-Synuclein on Dopamine Homeostasis in a New Human Mesencephalic Cell Line
Published in The Journal of biological chemistry (11-10-2002)“…Mutations in α-synuclein have been linked to rare, autosomal dominant forms of Parkinson's disease. Despite its ubiquitous expression, mutant α-synuclein…”
Get full text
Journal Article -
13
Structure-based optimization of aminothiadiazole inhibitors of AKT
Published in Medicinal chemistry research (01-07-2023)“…We report here the discovery and structure-guided optimization of a novel series of AKT kinase inhibitors. Based on docking studies for the predicted active…”
Get full text
Journal Article -
14
Discovery of Mammalian Target of Rapamycin (mTOR) Kinase Inhibitor CC-223
Published in Journal of medicinal chemistry (09-07-2015)“…We report here the synthesis and structure–activity relationship (SAR) of a novel series of mammalian target of rapamycin (mTOR) kinase inhibitors. A series of…”
Get full text
Journal Article -
15
The synthetic compound CC-5079 is a potent inhibitor of tubulin polymerization and tumor necrosis factor-α production with antitumor activity
Published in Cancer research (Chicago, Ill.) (15-01-2006)“…We have found that the synthetic compound CC-5079 potently inhibits cancer cell growth in vitro and in vivo by a novel combination of molecular mechanisms…”
Get full text
Journal Article -
16
Emerging treatments for asthma
Published in Expert opinion on emerging drugs (01-05-2003)“…Despite the availability of a great number of medications, the asthma epidemic is continuing to increase. It is obvious that a high, unmet medical need remains…”
Get more information
Journal Article -
17
Small molecule inhibitors of cell signaling: novel future therapeutics for asthma and chronic obstructive pulmonary diseases
Published in Current opinion in investigational drugs (London, England : 2000) (01-05-2003)“…The respiratory diseases asthma and chronic obstructive pulmonary disease (COPD) exhibit common, key pathological features, including the development of…”
Get more information
Journal Article -
18
Immortalized Human Dorsal Root Ganglion Cells Differentiate into Neurons with Nociceptive Properties
Published in The Journal of neuroscience (01-07-1999)“…A renewable source of human sensory neurons would greatly facilitate basic research and drug development. We had established previously conditionally…”
Get full text
Journal Article -
19
Abstract 4517: Evaluation of the TOR kinase inhibitor CC214-2 in a mouse model of hormone-refractory prostate cancer
Published in Cancer research (Chicago, Ill.) (01-10-2014)“…Abstract Prostate cancer is one of the most common malignancy diagnosed in men. Although androgen deprivation therapy is effective at the beginning of…”
Get full text
Journal Article -
20
Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115
Published in Journal of medicinal chemistry (23-07-2015)“…We report here the synthesis and structure–activity relationship (SAR) of a novel series of triazole containing mammalian target of rapamycin (mTOR) kinase…”
Get full text
Journal Article