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Metabolism of the dual FLT-3/Aurora kinase inhibitor CCT241736 in preclinical and human in vitro models: Implication for the choice of toxicology species.
(ELSEVIER, 2019-11-01)
CCT241736 is a dual fms-like tyrosine kinase 3 (FLT3)/Aurora kinase inhibitor in development for the treatment of acute myeloid leukaemia. The successful development of any new drug relies on adequate safety testing including ...
Suboptimal T-cell Therapy Drives a Tumor Cell Mutator Phenotype That Promotes Escape from First-Line Treatment.
(AMER ASSOC CANCER RESEARCH, 2019-05-01)
Antitumor T-cell responses raised by first-line therapies such as chemotherapy, radiation, tumor cell vaccines, and viroimmunotherapy tend to be weak, both quantitatively (low frequency) and qualitatively (low affinity). ...
Labelled chemical probes for demonstrating direct target engagement in living systems.
(FUTURE SCI LTD, 2019-05-24)
Demonstrating target engagement in living systems can help drive successful drug discovery. Target engagement and occupancy studies in cells confirm direct binding of a ligand to its intended target protein and provide the ...
A critical evaluation of the approaches to targeted protein degradation for drug discovery.
(Elsevier BV, 2019-04-03)
There is a great deal of excitement around the concept of targeting proteins for degradation as an alternative to conventional inhibitory small molecules and antibodies. Protein degradation can be undertaken by bifunctional ...
Cut-and-Run: A Distinct Mechanism by which V(D)J Recombination Causes Genome Instability.
(CELL PRESS, 2019-05-02)
V(D)J recombination is essential to generate antigen receptor diversity but is also a potent cause of genome instability. Many chromosome alterations that result from aberrant V(D)J recombination involve breaks at single ...
Breast cancer risk prediction in women aged 35-50 years: impact of including sex hormone concentrations in the Gail model.
(BMC, 2019-03-19)
BACKGROUND: Models that accurately predict risk of breast cancer are needed to help younger women make decisions about when to begin screening. Premenopausal concentrations of circulating anti-Müllerian hormone (AMH), a ...
3-D Microvascular Imaging Using High Frame Rate Ultrasound and ASAP Without Contrast Agents: Development and Initial In Vivo Evaluation on Nontumor and Tumor Models.
(IEEE-INST ELECTRICAL ELECTRONICS ENGINEERS INC, 2019-05-01)
Three-dimensional imaging is valuable to noninvasively assess angiogenesis given the complex 3-D architecture of vascular networks. The emergence of high frame rate (HFR) ultrasound, which can produce thousands of images ...
Predicting synthetic lethal interactions using conserved patterns in protein interaction networks.
(PUBLIC LIBRARY SCIENCE, 2019-04-17)
In response to a need for improved treatments, a number of promising novel targeted cancer therapies are being developed that exploit human synthetic lethal interactions. This is facilitating personalised medicine strategies ...
Pazopanib in patients with advanced intermediate-grade or high-grade liposarcoma.
(TAYLOR & FRANCIS LTD, 2019-07-03)
Introduction: Liposarcomas (LPS) are a heterogeneous group of adipocytic soft tissue sarcomas with limited treatment options in the advanced/metastatic setting. Pazopanib is a multi-target tyrosine kinase inhibitor (TKI) ...
SHH pathway inhibition is protumourigenic in adamantinomatous craniopharyngioma.
(BIOSCIENTIFICA LTD, 2019-03-01)
Pharmacological inhibition of the sonic hedgehog (SHH) pathway can be beneficial against certain cancers but detrimental in others. Adamantinomatous craniopharyngioma (ACP) is a relevant pituitary tumour, affecting children ...