Search results for "anti-p"
showing 10 items of 65 documents
Biological Evaluation of the Antiproliferative and Anti-migratory Activity of a Series of 3-(6-Phenylimidazo[2,1-b][1,3,4]thiadiazol-2-yl)-1H-indole …
2019
Heterocyclic rings are recognized as key components of many natural, semi-synthetic and synthetic molecules with a broad spectrum of biological activities. Among these molecules, the indole and imidazo[2,1-b][1,3,4]thiadiazole systems have recently been described as useful scaffolds for the design of anticancer agents. Herein the antitumor activity of a series of 3-(6-phenylimidazo[2,1-b][1,3,4]thiadiazol-2-yl)-1H-indoles, designed as hybrid structures, was assessed. Seven out of 10 compounds (1a-g) were submitted to National Cancer Institute (NCI). Remarkably, compound 1g showed antiproliferative activity against the full panel of sixty human cancer lines, with half-maximal inhibitory conc…
Management of Patients with Asymptomatic and Symptomatic Carotid Artery Disease: Update on Anti-Thrombotic Therapy
2019
AbstractThe most common causes of ischaemic stroke are represented by carotid artery atherosclerotic disease (CAAD) and atrial fibrillation. While oral anticoagulants substantially reduce the incidence of thromboembolic stroke (< 1%/year), the rate of ischaemic stroke and other cardiovascular disease events in patients with CAAD remains high, ranging from 8.4 to 18.1 events per 100 patient-years. Similar to any other atherosclerotic disease, anti-thrombotic therapies are proposed for CAAD to reduce stroke and other cardiovascular events. The 2017 European Society of Cardiology (ESC)/European Society for Vascular Surgery (ESVS) guidelines recommend for patients with asymptomatic CAAD ≥60%…
Synthesis of N-acyl Derivatives of Aminocombretastatin A-4 and Study of their Interaction with Tubulin and Downregulation of c-Myc.
2021
11 p.-9 fig.-4 tab.
Tevatron Run II combination of the effective leptonic electroweak mixing angle
2018
The Ministry of Science and Innovation and the Consolider-Ingenio 2010 Program and the European Union community Marie Curie Fellowship Contract No. 302103.
SF3B1 modulators affect key genes in metastasis and drug influx: a new approach to fight pancreatic cancer chemoresistance.
2021
Aim: Because mutations of splicing factor 3B subunit-1 (SF3B1) have been identified in 4% of pancreatic ductal adenocarcinoma (PDAC) patients, we investigated the activity of new potential inhibitors of SF3B1 in combination with gemcitabine, one of the standard drugs, in PDAC cell lines. Methods: One imidazo[2,1-b][1,3,4]thiadiazole derivative (IS1) and three indole derivatives (IS2, IS3 and IS4), selected by virtual screening from an in-house library, were evaluated by the sulforhodamine-B and wound healing assay for their cytotoxic and antimigratory activity in the PDAC cells SUIT-2, Hs766t and Panc05.04, the latter harbouring the SF3B1 mutations. The effects on the splicing pattern of pr…
Insight into the Evolving Role of PCSK9
2022
Proprotein convertase subtilisin/kexin type 9 (PCSK9) is the last discovered member of the family of proprotein convertases (PCs), mainly synthetized in hepatic cells. This serine protease plays a pivotal role in the reduction of the number of low-density lipoprotein receptors (LDLRs) on the surface of hepatocytes, which leads to an increase in the level of cholesterol in the blood. This mechanism and the fact that gain of function (GOF) mutations in PCSK9 are responsible for causing familial hypercholesterolemia whereas loss-of-function (LOF) mutations are associated with hypocholesterolemia, prompted the invention of drugs that block PCSK9 action. The high efficiency of PCSK9 inhibitors (…
Algorithms for Anti-Powers in Strings
2018
Abstract A string S [ 1 , n ] is a power (or tandem repeat) of order k and period n / k if it can be decomposed into k consecutive equal-length blocks of letters. Powers and periods are fundamental to string processing, and algorithms for their efficient computation have wide application and are heavily studied. Recently, Fici et al. (Proc. ICALP 2016) defined an anti-power of order k to be a string composed of k pairwise-distinct blocks of the same length ( n / k , called anti-period). Anti-powers are a natural converse to powers, and are objects of combinatorial interest in their own right. In this paper we initiate the algorithmic study of anti-powers. Given a string S, we describe an op…
Anti-powers in infinite words
2018
In combinatorics of words, a concatenation of $k$ consecutive equal blocks is called a power of order $k$. In this paper we take a different point of view and define an anti-power of order $k$ as a concatenation of $k$ consecutive pairwise distinct blocks of the same length. As a main result, we show that every infinite word contains powers of any order or anti-powers of any order. That is, the existence of powers or anti-powers is an unavoidable regularity. Indeed, we prove a stronger result, which relates the density of anti-powers to the existence of a factor that occurs with arbitrary exponent. As a consequence, we show that in every aperiodic uniformly recurrent word, anti-powers of ev…
Combination of the novel farnesyltransferase inhibitor RPR130401 and the geranylgeranyltransferase-1 inhibitor GGTI-298 disrupts MAP kinase activatio…
1999
To test the Kirsten-Ras (Ki-Ras) alternative prenylation hypothesis in malignant transformation, we used a novel farnesyltransferase inhibitor competitive to farnesyl-pyrophosphate, RPR130401, and a CaaX peptidomimetic geranylgeranyltransferase-1 inhibitor GGTI-298. In Ki-Ras-overexpressing transformed adrenocortical cells, RPR130401 at 1-10 microM inhibited very efficiently the [(3)H]farnesyl but not [(3)H]geranylgeranyl transfer to Ras. However, proliferation of these cells was only slightly sensitive to RPR130401 (IC(50)=30 microM). GGTI-298 inhibited the growth of these cells with an IC(50) of 11 microM but cell lysis was observed at 15 microM. The combination of 10 microM RPR130401 and…
Spectral analysis of the Neumann-Poincaré operator and characterization of the stress concentration in anti-plane elasticity
2012
When holes or hard elastic inclusions are closely located, stress which is the gradient of the solution to the anti-plane elasticity equation can be arbitrarily large as the distance between two inclusions tends to zero. It is important to precisely characterize the blow-up of the gradient of such an equation. In this paper we show that the blow-up of the gradient can be characterized by a singular function defined by the single layer potential of an eigenfunction corresponding to the eigenvalue 1/2 of a Neumann–Poincare type operator defined on the boundaries of the inclusions. By comparing the singular function with the one corresponding to two disks osculating to the inclusions, we quant…