Results 151 to 160 of about 13,155 (273)
Prospects and advances of PROTAC in the treatment of hematologic malignancies
Experimental Hematology & OncologyOver the past years, target protein degradation (TPD) has emerged as a hot topic in treating hematologic malignancies out of its strong ability to eliminate pathological proteins precisely.
Xinyang Wang, Ming Zhang, Heng Mei
doaj +1 more source
Allergy, EarlyView.ABSTRACT In the last decades, critical advancements in research technology and knowledge on disease mechanisms steered therapeutic approaches for chronic inflammatory diseases towards unprecedented target specificity. For allergic and chronic lung diseases, biologic drugs pioneered this goal, acquiring on the way—through the clinical use of monoclonal ...
F. Roth‐Walter +20 more
wiley +1 more source
Shining a Light on Proteolysis Targeting Chimeras [PDF]
ACS Central Science, 2019 Ellen Teichmann, Stefan Hecht
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Biochemical bone biomarkers in plasma cell dyscrasias
British Journal of Haematology, EarlyView.Visual abstract depicting that bone turnover markers reflect dynamic alterations in bone remodelling across the spectrum of plasma cell dyscrasias but remain limited by assay variability, biological confounding and incomplete integration with imaging and risk stratification.
Guido Nador +4 more
wiley +1 more source
Acta Materia MedicaEndocrine therapy that blocks estrogen receptor signaling has been effective for decades as a primary treatment choice for breast cancer patients expressing the estrogen receptor.
Jian Min +5 more
doaj +1 more source
Malignant craniopharyngiomas: Institutional experience and literature review
Brain Pathology, EarlyView.We report the second case of malignant craniopharyngioma with BAP1 and TP53 mutations. A literature review identified 44 cases of malignant craniopharyngiomas with a median overall survival of 6 months. Eighteen (41%) occurred in patients without any history of radiation, suggesting that mechanisms other than radiation have contributed to their ...
Thomas J. Auen +10 more
wiley +1 more source
Evaluation of Anti-cancer Activity of Stilbene and Methoxydibenzo[b,f] oxepin Derivatives [PDF]
, 2017 Background: Stilbenes, 1,2-diphenylethen derivatives, including resveratrol and combretastatins, show anticancer features especially against tumor angiogenesis. Fosbretabulin, CA-4, in combination with carboplatin, is in the last stages of clinical tests
Dębski, Janusz +10 more
core
Targeting protein–protein interactions with reversible covalent modalities: Non‐cysteine chemistries
British Journal of Pharmacology, EarlyView.Abstract Protein–protein interactions (PPIs) are central to diverse cellular functions, and represent a rapidly expanding class of therapeutic targets. Advancements in covalent drug design have enabled small‐molecule drugs to overcome challenges associated with engaging these targets, such as limited durations of action and difficult‐to‐drug (expansive,
Ruchira Basu, Steven Fletcher
wiley +1 more source
Lock, relax, load, and shoot: a molecular perspective on Nedd4 regulation
The FEBS Journal, EarlyView.Structural basis of inactive and active states of the Nedd4 HECT E3 ligase subfamily, following a ‘lock, relax, load, and shoot’ mechanism. In the locked, autoinhibited state, intramolecular domain interactions restrain the HECT domain. Relaxation releases these restraints, allowing loading of ubiquitin onto the catalytic cysteine, followed by the ...
Masa Janosev +2 more
wiley +1 more source
Metabolism-driven in vitro/in vivo disconnect of an oral ERɑ VHL-PROTAC
Communications BiologyTargeting the estrogen receptor alpha (ERα) pathway is validated in the clinic as an effective means to treat ER+ breast cancers. Here we present the development of a VHL-targeting and orally bioavailable proteolysis-targeting chimera (PROTAC) degrader ...
Thomas G. Hayhow +35 more
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