Browsing Cancer Therapeutics by title
Now showing items 495-514 of 647
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Preclinical Evidence That Trametinib Enhances the Response to Antiangiogenic Tyrosine Kinase Inhibitors in Renal Cell Carcinoma.
(AMER ASSOC CANCER RESEARCH, 2016-01-01)Sunitinib and pazopanib are antiangiogenic tyrosine kinase inhibitors (TKI) used to treat metastatic renal cell carcinoma (RCC). However, the ability of these drugs to extend progression-free and overall survival in this ... -
Preclinical transgenic and patient-derived xenograft models recapitulate the radiological features of human adamantinomatous craniopharyngioma.
(WILEY, 2018-07-01)To assess the clinical relevance of transgenic and patient-derived xenograft models of adamantinomatous craniopharyngioma (ACP) using serial magnetic resonance imaging (MRI) and high resolution post-mortem microcomputed ... -
Preclinical trial of a MAP4K4 inhibitor to reduce infarct size in the pig: does cardioprotection in human stem cell-derived myocytes predict success in large mammals?
(SPRINGER HEIDELBERG, 2021-05-20)Reducing infarct size (IS) by interfering with mechanisms for cardiomyocyte death remains an elusive goal. DMX-5804, a selective inhibitor of the stress-activated kinase MAP4K4, suppresses cell death in mouse myocardial ... -
Prediction of outcome in newly diagnosed myeloma: a meta-analysis of the molecular profiles of 1905 trial patients.
(NATURE PUBLISHING GROUP, 2018-01-01)Robust establishment of survival in multiple myeloma (MM) and its relationship to recurrent genetic aberrations is required as outcomes are variable despite apparent similar staging. We assayed copy number alterations (CNA) ... -
Preparation of tyrosine amide derivatives as Rho-kinase inhibitors
(2018-08-02)The invention relates to compds. of formula I and pharmaceutically acceptable salts and solvates thereof (wherein X1 and X2 are independently CH and N; p = 1 - 3; each R when present is halo; R0 and R1 are independently ... -
Presence of human breast cancer xenograft changes the diurnal profile of amino acids in mice.
(NATURE PORTFOLIO, 2022-01-19)Human xenografts are extremely useful models to study the biology of human cancers and the effects of novel potential therapies. Deregulation of metabolism, including changes in amino acids (AAs), is a common characteristic ... -
The prevalence and outcomes of frail older adults in clinical trials in multiple myeloma: A systematic review.
(SPRINGERNATURE, 2023-01-05)Multiple myeloma (MM) is an incurable blood cancer that primarily affects older adults. Several frailty tools have been developed to address the heterogeneity of aging in this population. Uptake of these measures has been ... -
Privileged Structures and Polypharmacology within and between Protein Families.
(AMER CHEMICAL SOC, 2018-12-13)Polypharmacology is often a key contributor to the efficacy of a drug, but is also a potential risk. We investigated two hits discovered via a cell-based phenotypic screen, the CDK9 inhibitor CCT250006 (1) and the pirin ... -
Prognostic role of the LCS6 KRAS variant in locally advanced rectal cancer: results of the EXPERT-C trial.
(OXFORD UNIV PRESS, 2015-09-01)BACKGROUND: Lethal-7 (let-7) is a tumour suppressor miRNA which acts by down-regulating several oncogenes including KRAS. A single-nucleotide polymorphism (rs61764370, T > G base substitution) in the let-7 complementary ... -
Prospective Evaluation of Whole-Body MRI versus FDG PET/CT for Lesion Detection in Participants with Myeloma.
(RADIOLOGICAL SOC NORTH AMERICA (RSNA), 2021-09-01)Purpose To compare disease detection of myeloma using contemporary whole-body (WB) MRI and fluorine 18 (18F) fluorodeoxyglucose (FDG) PET/CT protocols and to correlate imaging with laboratory estimates of disease burden, ... -
Prostate specific membrane antigen and DNA damage repair in advanced prostate cancer
(Institute of Cancer Research (University Of London), 2022-03-31)Identification and implementation of novel therapeutic strategies for advanced prostate cancer (PCa) remains an urgent, unmet clinical need. Prostate Specific Membrane Antigen (PSMA), a PCa biomarker, is currently being ... -
Prostate-specific Antigen Decline After 4 Weeks of Treatment with Abiraterone Acetate and Overall Survival in Patients with Metastatic Castration-resistant Prostate Cancer.
(ELSEVIER SCIENCE BV, 2016-11-01)BACKGROUND: The availability of multiple new treatments for metastatic castration-resistant prostate cancer (mCRPC) mandates earlier treatment switches in the absence of a response. A decline in prostate-specific antigen ... -
Prostate-Specific Membrane Antigen Expression and Response to DNA Damaging Agents in Prostate Cancer.
(AMER ASSOC CANCER RESEARCH, 2022-07-15)PURPOSE: Prostate-specific membrane antigen (PSMA) targeting therapies such as Lutetium-177 (177Lu)-PSMA-617 are affecting outcomes from metastatic castration-resistant prostate cancer (mCRPC). However, a significant subset ... -
Prostate-specific Membrane Antigen Heterogeneity and DNA Repair Defects in Prostate Cancer.
(ELSEVIER, 2019-10-01)BACKGROUND: Prostate-specific membrane antigen (PSMA; folate hydrolase) prostate cancer (PC) expression has theranostic utility. OBJECTIVE: To elucidate PC PSMA expression and associate this with defective DNA damage repair ... -
Protein coalitions in a core mammalian biochemical network linked by rapidly evolving proteins
(Springer Science and Business Media LLC, 2011-05-25)<jats:title>Abstract</jats:title> <jats:sec> <jats:title>Background</jats:title> <jats:p>Cellular ATP levels are generated by glucose-stimulated mitochondrial metabolism and determine ... -
Public resources for chemical probes: the journey so far and the road ahead.
(Future Science Ltd, 2019-11-28)High-quality small molecule chemical probes are extremely valuable for biological research and target validation. However, frequent use of flawed small-molecule inhibitors produces misleading results and diminishes the ... -
Pyrido[3,4-d]pyrimidin-4(3H)-one metabolism mediated by aldehyde oxidase is blocked by C2-substitution.
(TAYLOR & FRANCIS LTD, 2017-09-01)1. We have previously described C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-one derivatives as cell permeable inhibitors of the KDM4 and KDM5 subfamilies of JmjC histone lysine demethylases. 2. Although exemplar compound ... -
PYRIMIDINE COMPOUNDS AS INHIBITORS OF PROTEIN KINASES IKK EPSILON AND/OR TBK-1, PROCESSES FOR THEIR PREPARATION, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
(2012-01-26)Compounds of the general formula (I) and salts thereof are useful in the treatment of diseases associated with aberrant activity of the protein kinases IKKe and/or TBK-1 : in which: R1 represents an aliphatic heterocyclyl ... -
PYRIMIDINE COMPOUNDS USEFUL IN THE TREATMENT OF DISEASES MEDIATED BY IKKE AND/OR TBK1 MECHANISMS
(2014-08-28)Compounds of the general formula (I) and salts thereof are useful in the treatment of diseases associated with aberrant activity of the protein kinases &Igr;&Kgr;&Kgr;&egr; and/or TBK-1 in which one of V and W is N, and ... -
PYRUVAMIDE COMPOUNDS AS INHIBITORS OF DUST MITE GROUP 1 PEPTIDASE ALLERGEN AND THEIR USE
(2011-07-28)The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain pyruvamide compounds of the formula (X) (for convenience, collectively referred to herein as "PVA compounds"), ...