Browsing ICR Divisions by title
Now showing items 3948-3967 of 4595
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Synthesis and pre-clinical evaluation of a [F-18] fluoromethyl-tanaproget derivative for imaging of progesterone receptor expression
(ROYAL SOC CHEMISTRY, 2016-01-01)<p>This work features the synthesis and biological evaluation of a novel fluorinated derivative of tanaproget and a carbon-11 labelled analogue, a high affinity non-steroidal PR ligand, as a possible candidate for imaging ... -
Synthesis and profiling of a 3-aminopyridin-2-one-based kinase targeted fragment library: Identification of 3-amino-5-(pyridin-4-yl)pyridin-2(1H)-one scaffold for monopolar spindle 1 (MPS1) and Aurora kinases inhibition.
(PERGAMON-ELSEVIER SCIENCE LTD, 2018-07-15)Screening a 3-aminopyridin-2-one based fragment library against a 26-kinase panel representative of the human kinome identified 3-amino-5-(1-methyl-1H-pyrazol-4-yl)pyridin-2(1H)-one (2) and 3-amino-5-(pyridin-4-yl)pyridi ... -
Synthesis of a benzoxazinthione derivative of tanaproget and pharmacological evaluation for PET imaging of PR expression.
(SPRINGERNATURE, 2019-12-01)BACKGROUND: The histological evaluation of estrogen receptor (ER) and progesterone receptor (PR) expression in breast cancer lesions from biopsy tissue can stratify patients to receive endocrine therapy. Furthermore, PR ... -
Synthesis of a Ribose-Incorporating Medium Ring Scaffold via a Challenging Ring-Closing Metathesis Reaction.
(WILEY-V C H VERLAG GMBH, 2016-09-01)A practical synthesis of a novel oxabicyclo[6.2.1]undecenetriol useful as a medicinal chemistry scaffold has been developed starting from l-ribose. The sequence involves an oxidation/Grignard addition sequence and a ... -
Synthesis of trisubstituted pyrimidines by regioselective S<sub>N</sub>Ar and Suzuki reactions of polyhalopyrimidines
(GEORG THIEME VERLAG KG, 2006-04-04)An efficient, regioselective approach to the synthesis of trisubstituted pyrimidines was developed. Sequential functionalization of com. available polyhalopyrimidines provided the target compds. in moderate to good overall ... -
Synthetic 4D-CT of the thorax for treatment plan adaptation on MR-guided radiotherapy systems.
(IOP PUBLISHING LTD, 2019-05-23)MR-guided radiotherapy treatment planning utilises the high soft-tissue contrast of MRI to reduce uncertainty in delineation of the target and organs at risk. Replacing 4D-CT with MRI-derived synthetic 4D-CT would support ... -
Synthetic Lethal Screen Demonstrates That a JAK2 Inhibitor Suppresses a BCL6-dependent IL10RA/JAK2/STAT3 Pathway in High Grade B-cell Lymphoma.
(AMER SOC BIOCHEMISTRY MOLECULAR BIOLOGY INC, 2016-08-05)We demonstrate the usefulness of synthetic lethal screening of a conditionally BCL6-deficient Burkitt lymphoma cell line, DG75-AB7, with a library of small molecules to determine survival pathways suppressed by BCL6 and ... -
Synthetic Lethal Targeting of ARID1A-Mutant Ovarian Clear Cell Tumors with Dasatinib.
(AMER ASSOC CANCER RESEARCH, 2016-07-01)New targeted approaches to ovarian clear cell carcinomas (OCCC) are needed, given the limited treatment options in this disease and the poor response to standard chemotherapy. Using a series of high-throughput cell-based ... -
Synthetic lethal therapies for cancer: what's next after PARP inhibitors?
(NATURE PUBLISHING GROUP, 2018-06-28)The genetic concept of synthetic lethality has now been validated clinically through the demonstrated efficacy of poly(ADP-ribose) polymerase (PARP) inhibitors for the treatment of cancers in individuals with germline ... -
Synthetic Lethality and Cancer - Penetrance as the Major Barrier.
(CELL PRESS, 2018-10-01)Synthetic lethality has long been proposed as an approach for targeting genetic defects in tumours. Despite a decade of screening efforts, relatively few robust synthetic lethal targets have been identified. Improved genetic ... -
Synthetic lethality: the road to novel therapies for breast cancer.
(BIOSCIENTIFICA LTD, 2016-10-01)When the BRCA1 and BRCA2 tumour suppressor genes were identified in the early 1990s, the immediate implications of mapping, cloning and delineating the sequence of these genes were that individuals in families with a BRCA ... -
Systematic analysis of tumour cell-extracellular matrix adhesion identifies independent prognostic factors in breast cancer.
(IMPACT JOURNALS LLC, 2016-08-17)Tumour cell-extracellular matrix (ECM) interactions are fundamental for discrete steps in breast cancer progression. In particular, cancer cell adhesion to ECM proteins present in the microenvironment is critical for ... -
Systematic Discovery of Short Linear Motifs Decodes Calcineurin Phosphatase Signaling.
(CELL PRESS, 2020-07-16)Short linear motifs (SLiMs) drive dynamic protein-protein interactions essential for signaling, but sequence degeneracy and low binding affinities make them difficult to identify. We harnessed unbiased systematic approaches ... -
Systematic evaluation of PAXgene® tissue fixation for the histopathological and molecular study of lung cancer.
(WILEY, 2019-11-11)Whilst adequate for most existing pathological tests, formalin is generally considered a poor DNA preservative and use of alternative fixatives may prove advantageous for molecular testing of tumour material; an increasingly ... -
Systematic evaluation of quantotypic peptides for targeted analysis of the human kinome.
(NATURE PUBLISHING GROUP, 2014-10-01)In targeted proteomics it is critical that peptides are not only proteotypic but also accurately represent the level of the protein (quantotypic). Numerous approaches are used to identify proteotypic peptides, but quantotypic ... -
Systematic evaluation of the prognostic impact and intratumour heterogeneity of clear cell renal cell carcinoma biomarkers.
(ELSEVIER, 2014-07-19)BACKGROUND: Candidate biomarkers have been identified for clear cell renal cell carcinoma (ccRCC) patients, but most have not been validated. OBJECTIVE: To validate published ccRCC prognostic biomarkers in an independent ... -
Systematic literature review for the association of biomarkers with efficacy of anti-PD-1 inhibitors in advanced melanoma.
(FUTURE MEDICINE LTD, 2021-03-30)Aim: Summarize the literature assessing biomarkers in predicting efficacy of anti-PD-1 therapy for patients with high-risk unresectable or metastatic melanoma. Materials & methods: Relevant studies were identified via a ... -
Systematic review of methodology used in clinical studies evaluating the benefits of proton beam therapy.
(ELSEVIER IRELAND LTD, 2019-11-01)BACKGROUND: Proton beam therapy (PBT) delivers high-energy radiation to target tumours while sparing surrounding normal tissues. The dosimetric advantages of PBT over traditional photon radiotherapy may be clear but the ...
