Results 231 to 240 of about 317,261 (329)

Covalent drug discovery: Progress against key targets, emerging strategies and lessons learnt

open access: yesBritish Journal of Pharmacology, EarlyView.
Abstract Covalent drug discovery is currently experiencing a boom in industrial and academic interest. To date, at least 75 covalent drugs have received regulatory approval, targeting both traditional target classes and more challenging proteins for which other approaches failed. In many cases, unique aspects of covalent targeting are essential for the
Charles P. Brown   +2 more
wiley   +1 more source

Altered X-chromosome inactivation of the TLR7/8 locus and heterogeneity of pDCs in systemic sclerosis. [PDF]

open access: yesJ Exp Med
Du Y   +11 more
europepmc   +1 more source

Enhancing antitumour response to proteasome inhibitors with inhibitors of insulin‐degrading enzyme, a new molecular vulnerability in multiple myeloma

open access: yesBritish Journal of Pharmacology, EarlyView.
Inhibitors of insulin‐degrading enzyme boost PI cytotoxicity through an increased sensitivity of proteasome to PI inhibitors, induction of ISR, DNA damage and Myc down‐regulation. They overcome PI resistance in vitro and induce tumour regression in vivo.
Laetitia Lesire   +28 more
wiley   +1 more source

Gene reactivation upon erosion of X chromosome inactivation in female hiPSCs is predictable yet variable and persists through differentiation. [PDF]

open access: yesStem Cell Reports
Raposo AC   +13 more
europepmc   +1 more source

Molecular and Cell Biological Characterization of Patient‐Derived Head and Neck Squamous Carcinoma Cell Lines

open access: yesCancer Science, EarlyView.
Patient‐derived head and neck squamous cell carcinoma (HNSCC) cells were genomically and cytogenetically characterized, revealing actionable alterations and chromosomal instability. Targeted therapies suppressed growth according to EGFR amplification or PIK3CA mutation status.
Kazue Ito   +17 more
wiley   +1 more source

The role of genetic testing in accurate diagnosis of X-linked sideroblastic anemia: novel ALAS2 mutations and the impact of X-chromosome inactivation. [PDF]

open access: yesSci Rep
Jové-Solavera D   +12 more
europepmc   +1 more source

RNF12 is an X-Encoded dose-dependent activator of X chromosome inactivation.

open access: yesCell, 2009
I. Jonkers   +8 more
semanticscholar   +1 more source

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