Results 111 to 120 of about 90,710 (248)

Rgnef regulates bone mass through the activation of RhoA and Rac1

open access: yesExperimental and Molecular Medicine
Rho guanine nucleotide exchange factor (Rgnef/p190RhoGEF), a RhoA-specific guanine nucleotide exchange factor, has been implicated in cancer and amyotrophic lateral sclerosis, but little is known about its role in bone.
Jiae Lee   +7 more
doaj   +1 more source

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

Thermodynamic and kinetic insights into stop codon recognition by release factor 1. [PDF]

open access: yes, 2014
Stop codon recognition is a crucial event during translation termination and is performed by class I release factors (RF1 and RF2 in bacterial cells). Recent crystal structures showed that stop codon recognition is achieved mainly through a network of ...
Joseph, Simpson   +2 more
core  

The RasGrf family of mammalian guanine nucleotide exchange factors

open access: yesBiochimica et Biophysica Acta (BBA) - Reviews on Cancer, 2011
RasGrf1 and RasGrf2 are highly homologous mammalian guanine nucleotide exchange factors which are able to activate specific Ras or Rho GTPases. The RasGrf genes are preferentially expressed in the central nervous system, although specific expression of either locus may also occur elsewhere.
Fernández-Medarde, Alberto   +1 more
openaire   +4 more sources

Cardiotoxicity of BRAF/MEK inhibitors

open access: yesBritish Journal of Pharmacology, EarlyView.
Abstract Rapidly accelerated fibrosarcoma type B/B‐Raf proto‐oncogene, serine/threonine kinase (BRAF) and mitogen‐activated protein kinase (MEK) inhibitors have transformed outcomes in cancer therapy, particularly in melanoma. However, cardiovascular toxicities are increasingly recognized in real‐world clinical practice.
Katharina Seuthe   +4 more
wiley   +1 more source

Targeting the Menin–KMT2A Axis in Acute Leukemia: From Epigenetic Dependency to Clinical Translation

open access: yesEuropean Journal of Haematology, EarlyView.
ABSTRACT Acute leukemias characterized by a shared epigenetic dependency on the menin–KMT2A axis rely on aberrant HOX‐driven transcriptional programs that sustain leukemic self‐renewal and impair differentiation. This dependency is most evident in KMT2A‐rearranged and NPM1‐mutated acute myeloid leukemia (AML), but also extends to other HOX‐dependent ...
Antonella Bruzzese   +12 more
wiley   +1 more source

GCN2 in proteostasis: structural logic, signalling networks and disease

open access: yesThe FEBS Journal, EarlyView.
Threats to protein synthesis activate the kinase GCN2, initiating the integrated stress response (ISR). GCN2 is triggered by stalled ribosomes and uncharged tRNAs, which accumulate when amino acids are scarce. The ISR adjusts cellular physiology by promoting redox balance, protein quality control, and mitochondrial optimisation.
JiaYi Zhu, Stefan J. Marciniak
wiley   +1 more source

Targeting dermatophyte Cdc42 and Rac GTPase signaling to hinder hyphal elongation and virulence

open access: yesiScience
Summary: The development of antifungal drugs requires novel molecular targets due to limited treatment options and drug resistance. Through chemical screening and establishment of a novel genetic technique to repress gene expression in Trichophyton ...
Masaki Ishii   +5 more
doaj   +1 more source

Structural basis of guanine nucleotide exchange for Rab11 by SH3BP5

open access: yesLife Science Alliance, 2019
The structure of the SH3BP5–Rab11a complex and structure-based mutational analyses reveal structural basis of nucleotide exchange for Rab11 by its specific guanine nucleotide exchange factor. The Rab GTPase family is a major regulator of membrane traffic
Sakurako Goto-Ito   +5 more
doaj   +1 more source

First Tetraploa Genome and Multi‐Omics Analysis Reveal Key Plant‐Microbe‐Soil Interactions for Salt Tolerance and Yield Improvement of Wheat

open access: yesPlant Biotechnology Journal, EarlyView.
ABSTRACT Salinity is a major threat to global agricultural productivity of staple crops such as wheat. Although microbial‐based solutions hold promise for alleviating salinity stress, practical implementation is hindered by insufficient mechanistic characterization of bioinoculants and their interactions with plants.
Cheng‐Wei Qiu   +6 more
wiley   +1 more source

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