Duration of receptor antagonism, measured as the recovery of agonist responsiveness, is gaining attention as a method to evaluate the ‘effective’ target-residence for antagonists. These functional assays might be a good alternative for ki...
In this review, we describe the attributes of histone H3 mutants identified in cancer. H3 mutants were first identified in genes encoding H3.3, in pediatric high-grade glioma, and subsequently in chondrosarcomas and giant cell tumors of bone (GCTB) i...
The histamine H1 receptor (H1R) is a G protein-coupled receptor (GPCR) and plays a key role in allergic reactions upon activation by histamine which is locally released from mast cells and basophils. Consequently, H1R is a well-established therapeuti...
Pediatric high-grade gliomas (pHGGs) are a deadly and heterogenous subgroup of gliomas for which the development of innovative treatments is urgent. Advances in high-throughput molecular techniques have shed light on key epigenetic components of thes...
An exceptional gut-colonizing ability may underlie the dramatic epidemiological success of the multidrug-resistant H30R subclone of Escherichia coli sequence type 131 (O25b:K+:H4). In order to inform the development of colonization-preventing measure...
Isocitrate dehydrogenase (IDH) catalyzes the conversion of NAD(P)+ and isocitrate to NAD(P)H and α-ketoglutarate (αKG). The cytoplasmic enzyme IDH1 is important for producing NADPH for biosynthesis and for protecting against oxidative str...
Tryptophan hydroxylase 2 (TPH2) is the key and rate-limiting enzyme of serotonin (5-HT) synthesis in the mammalian brain. The 1473G mutation in the Tph2 gene decreases TPH2 activity in the mouse brain by twofold. (R)-2-amino-6-(1R, 2S)-1,2-dihydroxyp...
Herein we report the synthesis of 6-(7,8-dimethyl-2,4-dioxo-3,4-dihydrobenzo[g]pteridin-10(2H)-yl)hexyl 5-((3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl)pentanoate. The compound was fully characterized by melting point, 1H-, 13C-NMR spect...
Human wild type (wt) cardiac α-actin and its mutants p.A295S or p.R312H and p.E361G correlated with hypertrophic or dilated cardiomyopathy, respectively, were expressed by using the baculovirus/Sf21 insect cell system. The c-actin variants inhi...
Primary central nervous system tumors are the most frequent solid tumors in children, accounting for over 40% of all childhood brain tumor deaths, specifically high-grade gliomas. Compared with pediatric low-grade gliomas (pLGGs), pediatric high-grad...
We investigated the mechanism of signal transduction using inactivating (R476H) and activating (D576G) mutants of luteinizing hormone receptor (LHR) of eel at the conserved regions of intracellular loops II and III, respectively, naturally occurring...
Influenza A viruses (IAV) modulate host antiviral responses to promote growth and pathogenicity. Here, we examined the multifunctional IAV nonstructural protein 1 (NS1) of influenza A virus to better understand factors that contribute to viral replic...
After we identified pGlu-βGlu-Pro-NH2 as the first functional antagonist of the cholinergic central actions of the thyrotropin-releasing hormone (TRH, pGlu-His-Pro-NH2), we became interested in finding the receptor-associated mechanism responsible fo...
Recurrent pregnancy loss (RPL) is defined as the loss of two or more pregnancies, affecting approximately 1 to 3% of women worldwide. Scientific data highlight a possible correlation between thrombophilic genetic variants and RPL. H1299R variant in t...
Despite numerous studies investigating histamine and its receptors, the impact of histamine protonation states on binding to the histamine H1-receptor (H1R) has remained elusive. Therefore, we assessed the influence of different histamine tautomers (...
The human mutant cardiac α-actins p.A295S or p.R312H and p.E361G, correlated with hypertrophic or dilated cardiomyopathy, respectively, were expressed by the baculovirus/Sf21 insect cell system and purified to homogeneity. The purified cardiac actins...
Lauridia tetragona (L.f) R.H. Archer is routinely used in traditional medicine; however, its hepatoprotective property is yet to be scientifically proven. To this effect, the hepatoprotective activity of the polyphenolic-rich fractions (PPRFs) was in...
Enterotoxigenic Escherichia coli (ETEC) strains are a major cause of diarrhea in humans and animals. Heat-stable (STa) and heat-labile (LT) enterotoxins produced by ETEC disrupt fluid homeostasis in host small intestinal epithelial cells and cause fl...
Background and Objectives: To assess the association between the single nucleotide polymorphisms (SNPs) in the genes encoding complement factors CFH, C2, and C3 (Y402H rs1061170, R102G rs2230199, and E318D rs9332739, respectively) and response to int...
A hypergraph H = ( V , ε ) is a pair consisting of a vertex set V , and a set ε of subsets (the hyperedges of H ) of V . A hypergraph H is r -uniform if all the hyperedges of H have the...
G protein-coupled receptors (GPCRs) are targets of extracellular stimuli and hence occupy a key position in drug discovery. By specific and not yet fully elucidated coupling profiles with α subunits of distinct G protein families, they regulate cellu...
Caseous lymphadenitis is a chronic contagious disease that causes economic losses worldwide. Treatments are ineffective, thus demonstrating the importance of vaccination. In this study, rNanH and rPknG proteins from Corynebacterium pseudotuberculosis...
Let D=(V(D),A(D)) be a digraph of order n and let r∈S⊆V(D) with 2≤|S|≤n. A directed (S,r)-Steiner path (or an (S,r)-path for short) is a directed path P beginning at r such that S⊆V(P). Arc-disjoint between two (S,r)-paths is cha...
In the paper we prove for the first time an analogue of the Wiman inequality in the class of analytic functions f∈A0p(G) in an arbitrary complete Reinhard domain G⊂Cp, p∈N represented by the power series of the form f(z)=f(z1,⋯,zp)=∑‖n‖=0+∞anzn with...
Let G be a connected, simple, and finite graph. For an ordered set W={w1,w2,…,wk}⊆V(G) and a vertex v of G, the representation of v with respect to W is the k-vector r(v|W)=(dG(v,w1),…,dG(v,wk)). The set W is called a resolving set...
In drug discovery, assays with proximal readout are of great importance to study target-specific effects of potential drug candidates. In the field of G protein-coupled receptors (GPCRs), the determination of GPCR-G protein interactions and G protein...
Background: The variability of prion protein gene (PRNP) codons and the frequency of alleles (K222, D146, and S146) that appear to confer genetic resistance to classical scrapie are still unknown in several goat populations/breeds prevalent in Romani...
Given a graph G without isolated vertices, a total Roman dominating function for G is a function f:V(G)→{0,1,2} such that every vertex u with f(u)=0 is adjacent to a vertex v with f(v)=2, and the set of vertices with positive labels induces a gr...
African swine fever (ASF) is a highly contagious disease that affects wild and domestic swine. Currently, the disease is present as a pandemic affecting pork production in Eurasia and the Caribbean region. The etiological agent of ASF is a large, hig...
The destructionof clouds by strong shocks and hot winds is the key process responsible for the transporting of metals and dust from the ISM to the ICM/IGM, and establishing the multiphase structure in and around galaxies. In this work, we perform a d...
Theis’ theory (1935), later improved by Hantush & Jacob (1955) and Moench (1971), is a technique designed to study the water level in aquifers. The key formula in this theory is a certain integral transform H[g](r,t) of the pumping function...
Lots of symmetric properties are well-explored and analyzed in extremal graph theory, such as the well-known symmetrization operation in the Turán problem and the high symmetric in the extremal graphs. This paper is devoted to studying the Lag...
In this paper, first, we state an operator LR on an ordered semihyperring R. We show that if φ:R⟶T is a monomorphism and K⊆R, then LT(φ(K))=φ(LR(K)). Afterward, hyperatom elements in ordered semihyperrings are defined and some...
Proton relay between interfacial water molecules allows rapid two-dimensional diffusion. An energy barrier, ΔGr‡, opposes proton-surface-to-bulk release. The ΔGr‡-regulating mechanism thus far has remained unknown. Here, we...
Because of the complex mechanisms mediating cancer onset, prognosis, and metastatic behavior, different therapeutic approaches targeting these mechanisms have been investigated. Recent advancements in nanocarrier-based drug and gene delivery methods...
Let R be an associative ring with unity, X be a finite group, H be a subgroup of X, and G be a set of left coset representatives for the left action of H on X. In this article, we introduce two different ways to put R into a non-trivial G-weak graded...
Background: Dolutegravir (DTG)-based antiretroviral therapy (ART) rarely leads to virological failure (VF) and drug resistance in integrase strand transfer inhibitor (INSTI)-naïve persons living with HIV (PLWH). As a result, limited data are ava...
The purified active fraction of Albizia julibrissin saponin (AJSAF) is an ideal adjuvant candidate that improves antigen-specific both cellular and humoral immune responses and elicits mixed Th1/Th2 responses, but its mechanisms remain unclear. The k...
Motivated by the observation that most companies are more likely to consider job applicants referred by their employees than those who applied on their own, Arcaute and Vassilvitskii modeled a job market that integrates social networks into stable ma...
A facile, one-pot hydrothermal method was used to synthesize Nickel selenide (NiSe) nanoparticles decorated with reduced graphene oxide nanosheets (rGO), denoted as NiSe/rGO. The NiSe/rGO exhibits good electrochemical performance when tested as anode...
Rhodamine 6G (R6G) and 4-nitro-2,1,3-benzoxadiazole (NBD) linked through a spacer molecule spermidine (spd), R6G-spd-NBD, produces a fluorescent probe with pH-sensitive FRET (Förster (fluorescence) resonance energy transfer) effect that can be u...
Let (X,G,ω1,ω2,{ηt}) be a manifold with a bi-Poisson structure {ηt} generated by a pair of G-invariant symplectic structures ω1 and ω2, where a Lie group G acts properly on X. We prove that there exists two canonically defined manifolds (RLi,Gi,ω1i,ω...
Analytical spherically symmetric static solution to the set of Einstein and Klein-Gordon equations in a synchronous reference frame is considered. In a synchronous reference frame, a static solution exists in the ultrarelativistic limit p=−&eps...
Influenza A(H1N1)pdm09 viruses carrying a dual neuraminidase (NA) substitution were isolated from immunocompromised patients after administration of one or more NA inhibitors. These mutant viruses possessed an H275Y/I223R, H275Y/I223K, or H275Y/G147R...
For S⊆V(G),κG(S) denotes the maximum number k of edge disjoint trees T1,T2,…,Tk in G, such that V(Ti)∩V(Tj)=S for any i,j∈{1,2,…,k} and i≠j. For an integer 2≤r≤|V(G)|, the generalized r-connectivity of G is...
A subgraph H of an edge-colored graph G is called rainbow if all of its edges have different colors. Let ar(G,H) denote the maximum positive integer t, such that there is a t-edge-colored graph G without any rainbow subgraph H. We denote by kK2 a mat...
Photocatalysts lead vitally to water purifications and decarbonise environment each by wastewater treatment and hydrogen (H2) production as a renewable energy source from water-photolysis. This work deals with the photocatalytic degradation of ciprof...
The histamine H4 receptor (H4R) is a G protein-coupled receptor that is predominantly expressed on immune cells and considered to be an important drug target for various inflammatory disorders. Like most GPCRs, the H4R activates G proteins and recrui...
For G∈Rm×n and g∈Rm, the minimization min∥Gψ−g∥2, with ψ∈Rn, is known as the Tykhonov regularization. We transport the Tykhonov regularization to an infinite-dimensional setting, that is min∥T(h)&m...
The success of many computer vision and pattern recognition applications depends on matching local features on two or more images. Because the initial correspondence set—i.e., the set of the initial feature pairs—is often contaminated by...
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