Results 121 to 130 of about 574,974 (306)

IMPDH inhibition enhances cytarabine efficacy in SAMHD1‐expressing leukaemia cells via guanine nucleotide depletion

open access: yesMolecular Oncology, EarlyView.
Cytarabine is a key therapy for acute myeloid leukaemia (AML), but its efficacy is limited by the dNTPase SAMHD1, which hydrolyses its active metabolite. Screening nucleotide biosynthesis inhibitors revealed that IMPDH inhibitors selectively sensitise SAMHD1‐proficient AML cells to cytarabine.
Miriam Yagüe‐Capilla   +9 more
wiley   +1 more source

Structure/function of the soluble guanylyl cyclase catalytic domain

open access: yesNitric Oxide, 2018
Soluble guanylyl cyclase (GC-1) is the primary receptor of nitric oxide (NO) in smooth muscle cells and maintains vascular function by inducing vasorelaxation in nearby blood vessels. GC-1 converts guanosine 5'-triphosphate (GTP) into cyclic guanosine 3',5'-monophosphate (cGMP), which acts as a second messenger to improve blood flow.
Childers, Kenneth C., Garcin, Elsa D.
openaire   +2 more sources

Loss of IGF‐1R impairs DNA‐PKcs recruitment to chromatin leading to defective end‐joining

open access: yesMolecular Oncology, EarlyView.
IGF‐1R promotes radioresistance by facilitating DNA‐PKcs recruitment to chromatin, enabling non‐homologous end‐joining (NHEJ) repair of double‐strand breaks. Inhibition or loss of IGF‐1R disrupts this recruitment to damage sites, driving compensatory reliance on microhomology‐mediated end‐joining (MMEJ) repair.
Matthew O. Ellis   +3 more
wiley   +1 more source

Structural and Functional Insights Into Lysostaphin–Substrate Interaction

open access: yesFrontiers in Molecular Biosciences, 2018
Lysostaphin from Staphylococcus simulans and its family enzymes rapidly acquire prominence as the next generation agents in treatment of S. aureus infections.
Helena Tossavainen   +8 more
doaj   +1 more source

The telomerase essential N-terminal domain promotes DNA synthesis by stabilizing short RNA-DNA hybrids. [PDF]

open access: yes, 2015
Telomerase is an enzyme that adds repetitive DNA sequences to the ends of chromosomes and consists of two main subunits: the telomerase reverse transcriptase (TERT) protein and an associated telomerase RNA (TER). The telomerase essential N-terminal (TEN)
Akiyama, Benjamin M   +2 more
core   +2 more sources

Exploring alternative catalytic mechanisms of the Cas9 HNH domain

open access: yesProteins: Structure, Function, and Bioinformatics, 2019
AbstractUnderstanding the reaction mechanism of CRISPR‐associated protein 9 (Cas9) is crucial for the application of programmable gene editing. Despite the availability of the structures of Cas9 in apo‐ and substrate‐bound forms, the catalytically active structure is still unclear. Our first attempt to explore the catalytic mechanism of Cas9 HNH domain
Li Na Zhao   +2 more
openaire   +3 more sources

dUTPase is essential in zebrafish development and possesses several single‐nucleotide variants with pronounced structural and functional consequences

open access: yesFEBS Open Bio, EarlyView.
dUTPases are involved in balancing the appropriate nucleotide pools. We showed that dUTPase is essential for normal development in zebrafish. The different zebrafish genomes contain several single‐nucleotide variations (SNPs) of the dut gene. One of the dUTPase variants displayed drastically lower protein stability and catalytic efficiency as compared ...
Viktória Perey‐Simon   +6 more
wiley   +1 more source

Substituting Tyr138 in the active site loop of human phenylalanine hydroxylase affects catalysis and substrate activation

open access: yesFEBS Open Bio, 2017
Mammalian phenylalanine hydroxylase (PAH) is a key enzyme in l‐phenylalanine (l‐Phe) metabolism and is active as a homotetramer. Biochemical and biophysical work has demonstrated that it cycles between two states with a variably low and a high activity ...
João Leandro   +4 more
doaj   +1 more source

Expression and Enzymatic Properties of Domain-Deleted Mutants of Cyclodextrin Glucosyltransferase my20 [PDF]

open access: yesShipin Kexue
In this study, we constructed domain D, E and DE truncated mutants of a marine-derived cyclodextrin glucosyltransferase (CGTase) my20 and heterologously expressed these mutants using the pET-24a vector and E. coli BL21 (DE3) as the host, and purified the
SUN Tengteng, WANG Wei, SUN Jingjing, JIANG Chengcheng, HAO Jianhua
doaj   +1 more source

BMI‐1 modulation and trafficking during M phase in diffuse intrinsic pontine glioma

open access: yesFEBS Open Bio, EarlyView.
The schematic illustrates BMI‐1 phosphorylation during M phase, which triggers its translocation from the nucleus to the cytoplasm. In cycling cells, BMI‐1 functions within the PRC1 complex to mediate H2A K119 monoubiquitination. Following PTC596‐induced M phase arrest, phosphorylated BMI‐1 dissociates from PRC1 and is exported to the cytoplasm via its
Banlanjo Umaru   +6 more
wiley   +1 more source

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