Results 201 to 210 of about 6,021,091 (244)

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

British 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, Alan Armstrong, David J. Mann   +2 more
wiley   +1 more source

Imprinted X chromosome inactivation at the gamete-to-embryo transition. [PDF]

Mol Cell
Wei C, Kesner B, Yin H, Lee JT.
europepmc   +1 more source

Targeting KRAS for cancer therapy

British Journal of Pharmacology, EarlyView.
In recent years, therapeutics targeted against KRAS proto‐oncogene GTPase (KRAS)‐mutant cancers have seen significant progress. Herein we outline the biology and epidemiology of KRAS alterations at the lineage and allele levels, reviewing the clinical evidence for KRASG12C inhibition from the discovery of the recessive switch pocket to sotorasib ...
Jianlong Jia, Ruonan Liu, Tonia A. Adamide, Isis E. Fernandez, Georgios T. Stathopoulos   +4 more
wiley   +1 more source

Breaking rules: the complex relationship between DNA methylation and X-chromosome inactivation in the human placenta. [PDF]

Biol Sex Differ
Inkster AM, Matthews AM, Phung TN, Plaisier SB, Wilson MA, Brown CJ, Robinson WP.   +6 more
europepmc   +1 more source

Long non‐coding RNAs at the crossroads of inflammation, cancer and angiogenesis: Molecular mechanisms and their potential as therapeutic targets

British Journal of Pharmacology, EarlyView.
Long non‐coding RNAs (lncRNAs), a broad class of non‐protein‐coding RNAs, are characterized as new regulators of gene expression at the epigenetic, transcriptional, and post‐transcriptional level. Thus, lncRNAs are involved in the regulation of physiological processes and the development of human diseases and cancer by modulating proinflammatory ...
Charlie Leboff, Pamela Calle‐Mendoza, Maria Hatziapostolou, Christos Polytarchou   +3 more
wiley   +1 more source

Altered X-chromosome inactivation predisposes to autoimmunity. [PDF]

Sci Adv
Huret C, Ferrayé L, David A, Mohamed M, Valentin N, Charlotte F, Savignac M, Goodhardt M, Guéry JC, Rougeulle C, Morey C.   +10 more
europepmc   +1 more source

Ezh2 Inhibits the Differentiation of Short‐Lived Effector CD8+ T Cells and Promotes T Cell‐Dependent Antitumor Immunity

Cancer Science, EarlyView.
The antitumor immune response is attenuated in T cell‐specific Ezh2 knockout mice. ABSTRACT Appropriate regulation of the differentiation balance between effector CD8+ T cells and memory CD8+ T cells is crucial for an appropriate immune response. We previously reported that the tumor suppressor menin suppresses the differentiation of CD8+ T cells into ...
Kenji Takagi, Junpei Suzuki, Yuko Matsuoka, Makoto Kuwahara, Taro Oshikiri, Masakatsu Yamashita   +5 more
wiley   +1 more source

Measuring X-Chromosome inactivation skew for X-linked diseases with adaptive nanopore sequencing. [PDF]

Genome Res
Gocuk SA, Lancaster J, Su S, Jolly JK, Edwards TL, Hickey DG, Ritchie ME, Blewitt ME, Ayton LN, Gouil Q.   +9 more
europepmc   +1 more source

A Three‐Dimensional Culture–Drug Sensitivity Test Predicts MDM2 Inhibitor–Sensitivity in SMARCB1/INI1‐Deficient Tumors

Cancer Science, EarlyView.
This study aimed to determine whether personalized selection of effective drugs for SMARCB1/INI1‐deficient tumors is feasible using in vitro drug sensitivity profiling. Drug sensitivity was assessed using a short‐term collagen gel–embedded three‐dimensional drug sensitivity test (3D‐DST) in tumors derived from SMARCB1/INI1‐deficient tumor cell line ...
Hiroaki Goto, Chiyoko Nishime, Takashi Ohtsu, Mieko Ito, Maiko Sagisaka, Takuya Naruto, Norihiko Kitagawa, Mio Tanaka, Masakatsu Yanagimachi, Yukihiko Hiroshima, Junko Takita, Yasuhide Hayashi, Yohei Miyagi   +12 more
wiley   +1 more source

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

J Exp Med
Du Y, Faz-Lopez B, Ah Kioon MD, Cenac C, Pierides M, Lakin KS, Spiera RF, Chaumeil J, Truchetet ME, Gordon JK, Guéry JC, Barrat FJ.   +11 more
europepmc   +1 more source