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From triazolophthalazines to triazoloquinazolines: A bioisosterism-guided approach toward the identification of novel PCAF inhibitors with potential anticancer activity.

Bioorg Med Chem 2021 Jun 5;42:116266. Epub 2021 Jun 5.

Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy (Boys), Al-Azhar University, Nasr City 11884, Cairo, Egypt; Pharmaceutical Chemistry Department, Faculty of Pharmacy, Horus University - Egypt, International Coastal Road, 34518 New Damietta, Egypt. Electronic address:

Inhibition of PCAF bromodomain has been validated as a promising strategy for the treatment of cancer. In this study, we report the bioisosteric modification of the first reported potent PCAF bromodomain inhibitor, L-45 to its triazoloquinazoline bioisosteres. Accordingly, three new series of triazoloquinazoline derivatives were designed, synthesized, and assessed for their anticancer activity against a panel of four human cancer cells. Read More

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Antiproliferative and antibacterial activity of extracts of strains grown in vitro.

Food Sci Biotechnol 2021 May 5;30(5):711-721. Epub 2021 May 5.

Centro de Investigación en Micología Aplicada, Universidad Veracruzana, Calle Médicos 5, Col. Unidad del Bosque, 91010 Xalapa, Veracruz, Mexico.

In this bioprospecting study the biological activities of extracts of the in vitro culture of Mexican strains were evaluated. The extracts were tested by the Sulforhodamine B staining method for antiproliferative activity and the plate microdilution method for antibacterial activity. Extracts that proved bioactive in these two activities, the antioxidant activity (Galvinoxyl, ABTS, and DPPH) and total phenolic contents (Folin-Ciocalteu) were additionally determined, as well as acute toxicity (). Read More

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Chemical constituents, anti-inflammatory, antioxidant and hemostatic activities of the -butanol extract of (Poir.) Rothm.

Nat Prod Res 2021 Jun 14:1-5. Epub 2021 Jun 14.

Laboratory of Biology and Environment, Faculty of Nature and Life Sciences, University of Mentouri Brothers, Constantine, Algeria.

The phytochemical profile obtained from LC-ESI-MS/MS analysis of the -butanol extract (BEHL) from the North African endemic plant (Poir.) Rothm. brought about the identification of ten glycosylated derivatives of apigenin and luteolin flavones. Read More

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A new underdetermined NMF based anti-collision algorithm for RFID systems.

ISA Trans 2021 Jun 2. Epub 2021 Jun 2.

School of Automation and Information Engineering, Sichuan University of Science and Engineering, Yibin 644000, China; Artificial Intelligence Key Laboratory of Sichuan Province, Sichuan University of Science and Engineering, Yibin 644000, China.

Radio Frequency Identification (RFID) has been one of the critical technologies of the Internet of Things (IoT). With the rapid development of the IoT, the RFID systems are required to be more efficient and with high throughput capacity. In the widespread IoT application scenes, the collision problem of the RFID tags has become the increasingly remarkable problem in RFID systems. Read More

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Potent and Subtype-Selective Dopamine D Receptor Biased Partial Agonists Discovered via an Ugi-Based Approach.

J Med Chem 2021 Jun 10. Epub 2021 Jun 10.

Centro Singular de Investigación en Química Biolóxica e Materiais Moleculares (CIQUS), Universidade de Santiago de Compostela, 15782 Santiago de Compostela, Spain.

Using a previously unexplored, efficient, and versatile multicomponent method, we herein report the rapid generation of novel potent and subtype-selective DRD biased partial agonists. This strategy exemplifies the search for diverse and previously unexplored moieties for the secondary/allosteric pharmacophore of the common phenyl-piperazine scaffold. The pharmacological characterization of the new compound series led to the identification of several ligands with excellent DRD affinity and subtype selectivity and remarkable functional selectivity for either the cAMP ( and ) or the β-arrestin ( and ) signaling pathways. Read More

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Internal Mammary Artery and Its Resilience to Atherogenesis: Shifting From Risk to Resistance to Address Unmet Needs.

Arterioscler Thromb Vasc Biol 2021 Jun 10:ATVBAHA121316256. Epub 2021 Jun 10.

Center for Molecular Cardiology, University of Zürich, Switzerland (S.K., A.A., G.G.C., T.F.L.).

Fueled by the global surge in aging, atherosclerotic cardiovascular disease reached pandemic dimensions putting affected individuals at enhanced risk of myocardial infarction, stroke, and premature death. Atherosclerosis is a systemic disease driven by a wide spectrum of factors, including cholesterol, pressure, and disturbed flow. Although all arterial beds encounter a similar atherogenic milieu, the development of atheromatous lesions occurs discontinuously across the vascular system. Read More

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Challenges in the Management of an Echis coloratus Adult Snakebite Victim at a Tertiary Care Hospital: A Case Report.

Am J Case Rep 2021 Jun 9;22:e931532. Epub 2021 Jun 9.

King Abdullah International Medical Research Center, Jeddah, Saudi Arabia.

BACKGROUND The World Health Organization has set clear guidelines for the management of snakebite envenomation. However, challenges have been reported in the clinical application of guidelines, such as identification of the biting snake, hypersensitivity reactions to the antivenom, and influence of repeated antivenom administration during hospital stay. This report aims to discuss how these challenges can affect patient management and to highlight improvement opportunities. Read More

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A Family With Novel X-Linked Recessive Homozygous Mutation in (c.628_629 del, p.1210fs∗) in Kallmann Syndrome Associated Unilateral Ptosis: Case Report and Literature Review.

AACE Clin Case Rep 2021 May-Jun;7(3):216-219. Epub 2021 Feb 17.

Student Research Committee, Alborz University of Medical Sciences, Karaj, Alborz, Iran.

Objective: Kallmann syndrome (KS) may be accompanied by anosmia or hyposmia and midline defects. We present an overweight 16-year-old boy with a lack of puberty, anosmia, congenital right eye ptosis, and normal intellectual function.

Methods: Testicular ultrasonography was performed. Read More

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February 2021

Serum Metabolite Biomarkers Predictive of Response to PD-1 Blockade Therapy in Non-Small Cell Lung Cancer.

Front Mol Biosci 2021 21;8:678753. Epub 2021 May 21.

CAS-Key Laboratory of Synthetic Biology, CAS Center for Excellence in Molecular Plant Sciences, Chinese Academy of Sciences, Shanghai, China.

Despite remarkable success of immunotherapies with checkpoint blockade antibodies targeting programmed cell death protein 1 (PD-1), the majority of patients with non-small-cell lung cancer (NSCLC) have yet to receive durable benefits. We used the metabolomic profiling of early on-treatment serum to explore predictors of clinical outcomes of anti-PD-1 treatment in patients with advanced NSCLC. We recruited 74 Chinese patients who had stage IIIB/IV NSCLC-proven tumor progression and were treated with PD-1 inhibitor. Read More

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Identification of Docetaxel as a Potential Drug to Promote HDL Biogenesis.

Front Pharmacol 2021 21;12:679456. Epub 2021 May 21.

Cardiovascular Research Laboratories, Research Institute of the McGill University Health Center, Montreal, QC, Canada.

Our recent studies showed that desmocollin 1 (DSC1) binds to apoA-I in order to inhibit apoA-I-mediated high density lipoprotein (HDL) biogenesis in atherosclerotic plaques. To promote HDL biogenesis in the plaque, here we search for small molecules that block apoA-I-DSC1 interactions. We combined mutational and computational mapping methods to show that amino acid residues 442-539 in the mature DSC1 protein form an apoA-I binding site (AIBS). Read More

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Functional identification of ergothioneine transporter in rainbow trout (Oncorhynchus mykiss).

Comp Biochem Physiol B Biochem Mol Biol 2021 Jun 2;256:110631. Epub 2021 Jun 2.

Department of Food Science and Technology, Tokyo University of Marine Science and Technology, 4-5-7 Konan, Minato-ku, Tokyo 108-8477, Japan. Electronic address:

(2S)-3-(2-sulfanylidene-1,3-dihydroimidazol-4-yl)-2-(trimethylazaniumyl)propanoate (ergothioneine, ET) is hydrophilic antioxidant produced only by certain low-level organisms, but has been reported in the organs of some animals upon dietary intake, facilitated by the ergothioneine transporter (ETT). In this study, it was hypothesised that ETT is involved in the uptake of ET from diet in salmonids. The mechanism of ET uptake was evaluated through knockdown of candidate gene encoding ETT in a cell line (RTG-2) from rainbow trout (Oncorhynchus mykiss). Read More

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[Advances in the development of constraint-based genome-scale metabolic network models].

Sheng Wu Gong Cheng Xue Bao 2021 May;37(5):1526-1540

State Key Laboratory of Bioreactor Engineering, East China University of Science and Technology, Shanghai 200237, China.

Genome-scale metabolic network model (GSMM) is becoming an important tool for studying cellular metabolic characteristics, and remarkable advances in relevant theories and methods have been made. Recently, various constraint-based GSMMs that integrated genomic, transcriptomic, proteomic, and thermodynamic data have been developed. These developments, together with the theoretical breakthroughs, have greatly contributed to identification of target genes, systems metabolic engineering, drug discovery, understanding disease mechanism, and many others. Read More

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Insights into the Organization of the Poxvirus Multi-Component Entry-Fusion Complex from Proximity Analyses in Living Infected Cells.

J Virol 2021 Jun 2:JVI0085221. Epub 2021 Jun 2.

Laboratory of Viral Diseases, National Institute of Allergy and Infectious Diseases, National Institutes of Health, Bethesda, MD 20892, USA.

Poxviruses are exceptional in having a complex entry-fusion complex (EFC) that is comprised of eleven conserved proteins embedded in the membrane of mature virions. However, the detailed architecture is unknown and only a few bimolecular protein interactions have been demonstrated by co-immunoprecipitation from detergent-treated lysates and by cross-linking. Here, we adapted the tripartite split green fluorescent protein (GFP) complementation system in order to analyze EFC protein contacts within living cells. Read More

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Review of Venetoclax in CLL, AML and Multiple Myeloma.

J Pers Med 2021 May 24;11(6). Epub 2021 May 24.

Department of Haematology, Peter MacCallum Cancer Centre, Melbourne 3000, Australia.

Venetoclax is a highly selective and effective B-cell lymphoma-2 (BCL-2) inhibitor, which is able to reinstate the apoptotic potential of cancer cells. With its full repertoire yet to be explored, it has changed the therapeutic landscape in haematological malignancies, and most particularly chronic lymphocytic leukaemia (CLL), acute myeloid leukaemia (AML) and multiple myeloma (MM). In CLL, it has shown remarkable efficacy both as monotherapy and in combination therapy. Read More

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Bioactive Compounds in Waste By-Products from Olive Oil Production: Applications and Structural Characterization by Mass Spectrometry Techniques.

Foods 2021 May 29;10(6). Epub 2021 May 29.

Chemistry Department, University of Bari Aldo Moro, via Orabona 4, 70126 Bari, Italy.

In recent years, a remarkable increase in olive oil consumption has occurred worldwide, favoured by its organoleptic properties and the growing awareness of its health benefits. Currently, olive oil production represents an important economic income for Mediterranean countries, where roughly 98% of the world production is located. Both the cultivation of olive trees and the production of industrial and table olive oil generate huge amounts of solid wastes and dark liquid effluents, including olive leaves and pomace and olive oil mill wastewaters. Read More

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NMR Profiling of Identifies Cytotoxic Compounds against Cetuximab-Resistant Colon Cancer Cell Lines.

Molecules 2021 May 28;26(11). Epub 2021 May 28.

Dipartimento di Scienze e Tecnologie Ambientali, Biologiche e Farmaceutiche, Università degli Studi della Campania "Luigi Vanvitelli", Via Vivaldi 43, 81100 Caserta, Italy.

In the search of new natural products to be explored as possible anticancer drugs, two plant species, namely and , were screened against colorectal cancer cell lines. The cytotoxic activity of the crude extracts was tested on a panel of colon cancer cell models including cetuximab-sensitive (Caco-2, GEO, SW48), intrinsic (HT-29 and HCT-116), and acquired (GEO-CR, SW48-CR) cetuximab-resistant cell lines. showed remarkable cytotoxic activity, especially on the cetuximab-resistant cell lines. Read More

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The Insulin Receptor: A Potential Target of Amarogentin Isolated from Franch That Induces Neurogenesis in PC12 Cells.

Biomedicines 2021 May 20;9(5). Epub 2021 May 20.

College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China.

Amarogentin (AMA) is a secoiridoid glycoside isolated from the traditional Chinese medicine, Franch. AMA exhibits nerve growth factor (NGF)-mimicking and NGF-enhancing activities in PC12 cells and in primary cortical neuron cells. In this study, a possible mechanism was found showing the remarkable induction of phosphorylation of the insulin receptor (INSR) and protein kinase B (AKT). Read More

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Reprogramming cellular identity during intestinal regeneration.

Curr Opin Genet Dev 2021 May 29;70:40-47. Epub 2021 May 29.

BRIC - Biotech Research and Innovation Centre, Faculty of Health and Medical Sciences, University of Copenhagen, DK-2200 Copenhagen N, Denmark; Novo Nordisk Foundation Center for Stem Cell Biology, Faculty of Health and Medical Sciences, University of Copenhagen, DK-2200 Copenhagen N, Denmark. Electronic address:

The intestine is a vital organ mediating absorption of nutrients and water. Following tissue damage, the intestine mounts a remarkable regenerative response by reprogramming cellular identity to facilitate reinstatement of homeostasis. Here we review recent advances within intestinal regenerative biology and the emerging concept of fetal-like reprogramming, in which the adult intestinal epithelium transiently enters a repair-associated state reminiscent of ontologically pre-existing stages. Read More

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Development and application of novel electrophilic warheads in target identification and drug discovery.

Biochem Pharmacol 2021 May 29;190:114636. Epub 2021 May 29.

School of Pharmacy, Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, China; MOE Key Laboratory of Tumor Molecular Biology, Jinan University, Guangzhou, China. Electronic address:

Nucleophilic amino acids play important roles in maintenance of protein structure and function, covalent modification of such amino acid residues by therapeutic agents is an efficient way to treat human diseases. Most of current clinical drugs are structurally limited to α,β-unsaturated amide as an electrophilic warhead. To alleviate this issue, many novel electrophiles have been developed in recent years that can covalently bind to different amino acid residues and provides a unique way to interrogate proteins, including "undruggable" targets. Read More

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Attention-Based Neural Architecture Search for Person Re-Identification.

IEEE Trans Neural Netw Learn Syst 2021 May 31;PP. Epub 2021 May 31.

Recent years have witnessed significant progress of person reidentification (reID) driven by expert-designed deep neural network architectures. Despite the remarkable success, such architectures often suffer from high model complexity and time-consuming pretraining process, as well as the mismatches between the image classification-driven backbones and the reID task. To address these issues, we introduce neural architecture search (NAS) into automatically designing person reID backbones, i. Read More

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Identification of Subgenomic DNAs Associated with Infection in Iran.

Iran J Biotechnol 2020 Oct 1;18(4):e2472. Epub 2020 Oct 1.

Department of Agriculture and Natural Resources, Higher Education Center of Eghlid, Eghlid, Iran.

Background: (WDV) is a leafhopper-transmitted DNA virus which causes yellowing and stunting in wheat and barley fields leading to considerable crop loss around the world. Mainly, two host-specific forms of WDV have been characterized in wheat and barley (WDV-Wheat and WDV-Barley, respectively).

Objectives: This study was aimed to amplify, sequence and describe subgenomic DNAs (sgDNAs) associated with WDV infection among wheat and barley plants. Read More

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October 2020

Identification of a Novel Variant in Causing MELAS.

Front Genet 2021 12;12:638749. Epub 2021 May 12.

Department of Neurology, Beijing Children's Hospital, Capital Medical University, National Center for Children's Health, Beijing, China.

Mitochondrial encephalomyopathy, lactic acidosis, and stroke-like episodes (MELAS) is a maternally inherited mitochondrial disease. Most cases of MELAS are caused by the m.3243A > G variant in the gene encoding tRNALeu. Read More

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Reproducible, shelf-stable, and bioaffinity SERS nanotags inspired by multivariate polyphenolic chemistry for bacterial identification.

Anal Chim Acta 2021 Jul 28;1167:338570. Epub 2021 Apr 28.

School of Food Science and Engineering, South China University of Technology, Guangzhou 510641, China; Academy of Contemporary Food Engineering, South China University of Technology, Guangzhou Higher Education Mega Center, Guangzhou 510006, China; Engineering and Technological Research Centre of Guangdong Province on Intelligent Sensing and Process Control of Cold Chain Foods, & Guangdong Province Engineering Laboratory for Intelligent Cold Chain Logistics Equipment for Agricultural Products, Guangzhou Higher Education Mega Centre, Guangzhou 510006, China.

Efficient identification of pathogenic bacteria is greatly concerned with microbial food safety and foodborne diseases diagnosis. Surface-enhanced Raman scattering (SERS) tags are among the cutting-edge tools for bioanalysis, but facing troubles in either SERS sensitivity, durability, interfering signals, or universal recognition agents for target bacteria. This work proposed a multivariate scheme enabled by polyphenolic chemistry for the green synthesis, facile stabilization (functionalization), protective encapsulation, and bio-affinitive design of metal-phenolic networks (MPNs)-encapsulated silver SERS nanotags ([email protected]@MPNs). Read More

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The development and neuronal complexity of bipinnaria larvae of the sea star Asterias rubens.

Integr Comp Biol 2021 May 27. Epub 2021 May 27.

Department of Genetics, Evolution and Environment, University College London, Darwin Building, Gower Street, London, WC1E 6BT, United Kingdom.

Free-swimming planktonic larvae are a key stage in the development of many marine phyla, and studies of these organisms have contributed to our understanding of major genetic and evolutionary processes. Although transitory, these larvae often attain a remarkable degree of tissue complexity, with well-defined musculature and nervous systems. Amongst the best studied are larvae belonging to the phylum Echinodermata, but with work largely focused on the pleuteus larvae of sea urchins (class Echinoidea). Read More

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Signal-piloted processing and machine learning based efficient power quality disturbances recognition.

PLoS One 2021 28;16(5):e0252104. Epub 2021 May 28.

Electrical and Computer Engineering Department, Effat University, Jeddah, Saudi Arabia.

Significant losses can occur for various smart grid stake holders due to the Power Quality Disturbances (PQDs). Therefore, it is necessary to correctly recognize and timely mitigate the PQDs. In this context, an emerging trend is the development of machine learning assisted PQDs management. Read More

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Identification of Novel and Potent Modulators Involved in Neonatal Cardiac Regeneration.

Pediatr Cardiol 2021 May 27. Epub 2021 May 27.

Regenerative Biology Research Laboratory, Department of Genetics and Bioengineering, Faculty of Engineering, Yeditepe University, Istanbul, Turkey.

Neonatal mammalian heart has been shown to possess the capacity to regenerate substantially after an injury. This remarkable regenerative capacity is lost in a week. This transition has been marked with cardiomyocyte cell cycle arrest and induction of fibrotic response similar to what occurs after myocardial infarction in adult hearts. Read More

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Quinoline and Quinazoline Derivatives Inhibit Viral RNA Synthesis by SARS-CoV-2 RdRp.

ACS Infect Dis 2021 06 26;7(6):1535-1544. Epub 2021 May 26.

Institute of Medicinal Biotechnology, Chinese Academy of Medical Science, Beijing 100050, China.

Coronavirus disease 2019 (COVID-19) is a fatal respiratory illness caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). The identification of potential drugs is urgently needed to control the pandemic. RNA dependent RNA polymerase (RdRp) is a conserved protein within RNA viruses and plays a crucial role in the viral life cycle, thus making it an attractive target for development of antiviral drugs. Read More

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Molecular characterization and genetic diversity of cutaneous leishmaniasis from North Eastern Pakistan.

Acta Trop 2021 May 20:105964. Epub 2021 May 20.

Department of Zoology, Faculty of Biological Science, Quaid-i-Azam University Islamabad 45320, Pakistan.. Electronic address:

The genetic diversity of Leishmania spp. in North Eastern Pakistan remains undetermined despite increased cases of cutaneous leishmaniasis (CL). This study was designed to decipher the molecular characterization and genetic diversity of Leishmania spp. Read More

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Description of novel resistance islands harbouring bla in IncC type 2 plasmids.

J Glob Antimicrob Resist 2021 May 18;26:37-41. Epub 2021 May 18.

Departamento de Bacteriología y Virología, Instituto de Higiene, Facultad de Medicina, Universidad de la República, Montevideo, Uruguay.

Objectives: We sequenced two IncA/C plasmids harbouring bla in Klebsiella pneumoniae clinical isolates and compared their antibiotic resistance islands.

Methods: Transconjugants were obtained from two clinical K. pneumoniae isolates harbouring bla. Read More

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Identifying Gaps in Community Pharmacists' Competence in Medication Risk Management in Routine Dispensing.

Innov Pharm 2021 11;12(1). Epub 2021 Feb 11.

Clinical Pharmacy Group, Division of Pharmacology and Pharmacotherapy, Faculty of Pharmacy, University of Helsinki, Finland.

Background: Community pharmacists increasingly contribute to medication risk management while dispensing medicines to outpatients. Their risk management actions are shifting from medication counselling towards reviewing medications and following-up their therapeutic effects and outcomes. Acquiring these more clinical tasks require more patient care-oriented competences. Read More

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February 2021