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Article ; Online: Human ACE2 peptide-mimics block SARS-CoV-2 pulmonary cells infection.

Karoyan, Philippe / Vieillard, Vincent / Gómez-Morales, Luis / Odile, Estelle / Guihot, Amélie / Luyt, Charles-Edouard / Denis, Alexis / Grondin, Pascal / Lequin, Olivier

Communications biology

2021 Volume 4, Issue 1, Page(s) 197

Abstract: In light of the recent accumulated knowledge on SARS-CoV-2 and its mode of human cells invasion, the binding of viral spike glycoprotein to human Angiotensin Converting Enzyme 2 (hACE2) receptor plays a central role in cell entry. We designed a series of ...

Abstract	In light of the recent accumulated knowledge on SARS-CoV-2 and its mode of human cells invasion, the binding of viral spike glycoprotein to human Angiotensin Converting Enzyme 2 (hACE2) receptor plays a central role in cell entry. We designed a series of peptides mimicking the N-terminal helix of hACE2 protein which contains most of the contacting residues at the binding site, exhibiting a high helical folding propensity in aqueous solution. Our best peptide-mimics are able to block SARS-CoV-2 human pulmonary cell infection with an inhibitory concentration (IC
MeSH term(s)	Amino Acid Sequence ; Angiotensin-Converting Enzyme 2/chemistry ; COVID-19/virology ; Cell Line ; Circular Dichroism ; Humans ; Peptides/chemical synthesis ; Peptides/chemistry ; Peptides/metabolism ; Peptides/pharmacology ; Protein Binding/drug effects ; Protein Structure, Secondary ; SARS-CoV-2/physiology ; Spike Glycoprotein, Coronavirus/metabolism ; Virus Replication/drug effects
Chemical Substances	Peptides ; Spike Glycoprotein, Coronavirus ; spike protein, SARS-CoV-2 ; ACE2 protein, human (EC 3.4.17.23) ; Angiotensin-Converting Enzyme 2 (EC 3.4.17.23)
Language	English
Publishing date	2021-02-12
Publishing country	England
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ISSN	2399-3642
ISSN (online)	2399-3642
DOI	10.1038/s42003-021-01736-8
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article ; Online: PKHB1, a thrombospondin-1 peptide mimic, induces anti-tumor effect through immunogenic cell death induction in breast cancer cells.

Calvillo-Rodríguez, Kenny Misael / Mendoza-Reveles, Rodolfo / Gómez-Morales, Luis / Uscanga-Palomeque, Ashanti Concepción / Karoyan, Philippe / Martínez-Torres, Ana Carolina / Rodríguez-Padilla, Cristina

Oncoimmunology

2022 Volume 11, Issue 1, Page(s) 2054305

Abstract: Breast cancer is the most commonly diagnosed cancer and the leading cause of cancer death in women worldwide. Recent advances in the field of immuno-oncology demonstrate the beneficial immunostimulatory effects of the induction of immunogenic cell death ( ...

Abstract	Breast cancer is the most commonly diagnosed cancer and the leading cause of cancer death in women worldwide. Recent advances in the field of immuno-oncology demonstrate the beneficial immunostimulatory effects of the induction of immunogenic cell death (ICD). ICD increases tumor infiltration by T cells and is associated with improved prognosis in patients affected by triple negative breast cancer (TNBC) with residual disease. The aim of this study was to evaluate the antitumoral effect of PKHB1, a thrombospondin-1 peptide mimic, against breast cancer cells, and the immunogenicity of the cell death induced by PKHB1 in vitro, ex vivo, and in vivo. Our results showed that PKHB1 induces mitochondrial alterations, ROS production, intracellular Ca
MeSH term(s)	Breast Neoplasms/drug therapy ; Breast Neoplasms/metabolism ; Cell Death ; Cell Line, Tumor ; Female ; Humans ; Immunogenic Cell Death ; Peptides/pharmacology
Chemical Substances	Peptides
Language	English
Publishing date	2022-04-04
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	2645309-5
ISSN	2162-402X ; 2162-4011
ISSN (online)	2162-402X
ISSN	2162-4011
DOI	10.1080/2162402X.2022.2054305
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Article ; Online: Human ACE2 peptide-mimics block SARS-CoV-2 pulmonary cells infection

Philippe Karoyan / Vincent Vieillard / Luis Gómez-Morales / Estelle Odile / Amélie Guihot / Charles-Edouard Luyt / Alexis Denis / Pascal Grondin / Olivier Lequin

Communications Biology, Vol 4, Iss 1, Pp 1-

2021 Volume 9

Abstract: Karoyan et al. present a method to inhibit SARS-CoV-2 by means of a peptide-mimic approach ...

Abstract	Karoyan et al. present a method to inhibit SARS-CoV-2 by means of a peptide-mimic approach. They design a series of peptides mimicking the N-terminal helix of hACE2 protein and their best peptide-mimic blocks SARS-CoV-2 human pulmonary cell infection with an IC50 in nanomolar range.
Keywords	Biology (General) ; QH301-705.5
Language	English
Publishing date	2021-02-01T00:00:00Z
Publisher	Nature Portfolio
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: Methylglyoxal, a potent inducer of AGEs, connects between diabetes and cancer.

Bellier, Justine / Nokin, Marie-Julie / Lardé, Eva / Karoyan, Philippe / Peulen, Olivier / Castronovo, Vincent / Bellahcène, Akeila

Diabetes research and clinical practice

2019 Volume 148, Page(s) 200–211

Abstract: Diabetes is one of the most frequent diseases throughout the world and its incidence is predicted to exponentially progress in the future. This metabolic disorder is associated with major complications such as neuropathy, retinopathy, atherosclerosis, ... ...

Abstract	Diabetes is one of the most frequent diseases throughout the world and its incidence is predicted to exponentially progress in the future. This metabolic disorder is associated with major complications such as neuropathy, retinopathy, atherosclerosis, and diabetic nephropathy, the severity of which correlates with hyperglycemia, suggesting that they are triggered by high glucose condition. Reducing sugars and reactive carbonyl species such as methylglyoxal (MGO) lead to glycation of proteins, lipids and DNA and the gradual accumulation of advanced glycation end products (AGEs) in cells and tissues. While AGEs are clearly implicated in the pathogenesis of diabetes complications, their potential involvement during malignant tumor development, progression and resistance to therapy is an emerging concept. Meta-analysis studies established that patients with diabetes are at higher risk of developing cancer and show a higher mortality rate than cancer patients free of diabetes. In this review, we highlight the potential connection between hyperglycemia-associated AGEs formation on the one hand and the recent evidence of pro-tumoral effects of MGO stress on the other hand. We also discuss the marked interest in anti-glycation compounds in view of their strategic use to treat diabetic complications but also to protect against augmented cancer risk in patients with diabetes.
MeSH term(s)	Animals ; Diabetes Complications/complications ; Diabetes Complications/metabolism ; Diabetes Complications/mortality ; Diabetes Complications/pathology ; Glycation End Products, Advanced/metabolism ; Humans ; Hyperglycemia/complications ; Hyperglycemia/metabolism ; Hyperglycemia/mortality ; Hyperglycemia/pathology ; Meta-Analysis as Topic ; Neoplasms/complications ; Neoplasms/metabolism ; Neoplasms/mortality ; Neoplasms/pathology ; Oxidative Stress/drug effects ; Pyruvaldehyde/metabolism ; Pyruvaldehyde/pharmacology ; Up-Regulation/drug effects
Chemical Substances	Glycation End Products, Advanced ; Pyruvaldehyde (722KLD7415)
Language	English
Publishing date	2019-01-18
Publishing country	Ireland
Document type	Journal Article ; Review
ZDB-ID	632523-3
ISSN	1872-8227 ; 0168-8227
ISSN (online)	1872-8227
ISSN	0168-8227
DOI	10.1016/j.diabres.2019.01.002
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Article ; Online: An hACE2 peptide mimic blocks SARS-CoV-2 Pulmonary Cell Infection

Karoyan, Philippe / Vieillard, Vincent / Odile, Estelle / Denis, Alexis / Gomes-Morales, Luis / Grondin, Pascal / Lequin, Olivier

bioRxiv

Abstract: In the light of the recent accumulated knowledge on SARS-CoV-2 and its mode of human cells invasion, the binding of viral spike glycoprotein to human Angiotensin Converting Enzyme 2 (hACE2) receptor plays a central role in cell entry. We designed a ... ...

Abstract	In the light of the recent accumulated knowledge on SARS-CoV-2 and its mode of human cells invasion, the binding of viral spike glycoprotein to human Angiotensin Converting Enzyme 2 (hACE2) receptor plays a central role in cell entry. We designed a series of peptides mimicking the N-terminal helix of hACE2 protein which contains most of the contacting residues at the binding site and have a high helical folding propensity in aqueous solution. Our best peptide mimics bind to the virus spike protein with high affinity and are able to block SARS-CoV-2 human pulmonary cell infection with an inhibitory concentration (IC50) in the nanomolar range. These first in class blocking peptide mimics represent powerful tools that might be used in prophylactic and therapeutic approaches to fight the coronavirus disease 2019 (COVID-19).
Keywords	covid19
Language	English
Publishing date	2020-08-24
Publisher	Cold Spring Harbor Laboratory
Document type	Article ; Online
DOI	10.1101/2020.08.24.264077
Database	COVID19

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Article ; Online: Human ACE2 peptide mimics block SARS-CoV-2 Pulmonary Cells Infection

Karoyan, Philippe / Vieillard, Vincent / Odile, Estelle / Denis, Alexis / Guihot, Amélie / Luyt, Charles-Edouard / Gómez-Morales, Luis / Grondin, Pascal / Lequin, Olivier

bioRxiv

Abstract	In the light of the recent accumulated knowledge on SARS-CoV-2 and its mode of human cells invasion, the binding of viral spike glycoprotein to human Angiotensin Converting Enzyme 2 (hACE2) receptor plays a central role in cell entry. We designed a series of peptides mimicking the N-terminal helix of hACE2 protein which contains most of the contacting residues at the binding site and have a high helical folding propensity in aqueous solution. Our best peptide mimics bind to the virus spike protein with high affinity and are able to block SARS-CoV-2 human pulmonary cell infection with an inhibitory concentration (IC50) in the nanomolar range. These first in class blocking peptide mimics represent powerful tools that might be used in prophylactic and therapeutic approaches to fight the coronavirus disease 2019 (COVID-19).
Keywords	covid19
Publisher	BioRxiv; WHO
Document type	Article ; Online
DOI	10.1101/2020.08.24.264077
Database	COVID19

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Article ; Online: Synthesis, gallium labelling and characterization of P04087, a functionalized phosphatidylserine-binding peptide.

Ben Azzouna, Rana / Guez, Alexandre / Benali, Khadija / Al-Shoukr, Faisal / Gonzalez, Walter / Karoyan, Philippe / Rouzet, François / Le Guludec, Dominique

EJNMMI radiopharmacy and chemistry

2017 Volume 2, Issue 1, Page(s) 3

Abstract: Background: Radiolabeled phosphatidylserine (PS)-binding peptides represent an innovative strategy for molecular imaging of apoptosis and thrombus. The hexapeptide PGDLSR was described as a selective and high affinity ligand for PS. In this work, we ... ...

Abstract	Background: Radiolabeled phosphatidylserine (PS)-binding peptides represent an innovative strategy for molecular imaging of apoptosis and thrombus. The hexapeptide PGDLSR was described as a selective and high affinity ligand for PS. In this work, we synthesized and evaluated a gallium labelled-PGDLSR peptide as a potential and selective radiopharmaceutical for nuclear imaging. PGDLSR-β-alanine-NODAGA (P04087) was prepared using Fmoc-based synthesis and then chelated with cold gallium, Results: PGDLSR was successfully prepared with a yield of 31%. P04087 was obtained with a yield of 28% and in high chemical purity (>95%). The radiochemical purities of Conclusion: In spite of the preservation of the peptide affinity to the PS after its conjugation to the NODAGA chelator, and of the presence of
Language	English
Publishing date	2017-02-07
Publishing country	England
Document type	Journal Article
ISSN	2365-421X
ISSN (online)	2365-421X
DOI	10.1186/s41181-016-0021-5
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Article ; Online: PSL Chemical Biology Symposia Third Edition: A Branch of Science in its Explosive Phase.

Baron, Leeroy / Hadjerci, Justine / Thoidingjam, Leishemba / Plays, Marina / Bucci, Romain / Morris, Nolwenn / Müller, Sebastian / Sindikubwabo, Fabien / Solier, Stéphanie / Cañeque, Tatiana / Colombeau, Ludovic / Blouin, Cedric M / Lamaze, Christophe / Puisieux, Alain / Bono, Yannick / Gaillet, Christine / Laraia, Luca / Vauzeilles, Boris / Taran, Frédéric /

Papot, Sébastien / Karoyan, Philippe / Duval, Romain / Mahuteau-Betzer, Florence / Arimondo, Paola / Cariou, Kevin / Guichard, Gilles / Micouin, Laurent / Ethève-Quelquejeu, Mélanie / Verga, Daniela / Versini, Antoine / Gasser, Gilles / Tang, Cong / Belmont, Philippe / Linkermann, Andreas / Bonfio, Claudia / Gillingham, Dennis / Poulsen, Thomas / Di Antonio, Marco / Lopez, Marie / Guianvarc'h, Dominique / Thomas, Christophe / Masson, Géraldine / Gautier, Arnaud / Johannes, Ludger / Rodriguez, Raphaël

Chembiochem : a European journal of chemical biology

2023 Volume 24, Issue 8, Page(s) e202300093

Abstract: This symposium is the third PSL (Paris Sciences & Lettres) Chemical Biology meeting (2016, 2019, 2023) held at Institut Curie. This initiative originally started at Institut de Chimie des Substances Naturelles (ICSN) in Gif-sur-Yvette (2013, 2014), under ...

Abstract	This symposium is the third PSL (Paris Sciences & Lettres) Chemical Biology meeting (2016, 2019, 2023) held at Institut Curie. This initiative originally started at Institut de Chimie des Substances Naturelles (ICSN) in Gif-sur-Yvette (2013, 2014), under the directorship of Professor Max Malacria, with a strong focus on chemistry. It was then continued at the Institut Curie (2015) covering a larger scope, before becoming the official PSL Chemical Biology meeting. This latest edition was postponed twice for the reasons that we know. This has given us the opportunity to invite additional speakers of great standing. This year, Institut Curie hosted around 300 participants, including 220 on site and over 80 online. The pandemic has had, at least, the virtue of promoting online meetings, which we came to realize is not perfect but has its own merits. In particular, it enables those with restricted time and resources to take part in events and meetings, which can now accommodate unlimited participants. We apologize to all those who could not attend in person this time due to space limitation at Institut Curie.
MeSH term(s)	Humans ; Paris ; Biology
Language	English
Publishing date	2023-03-21
Publishing country	Germany
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	2020469-3
ISSN	1439-7633 ; 1439-4227
ISSN (online)	1439-7633
ISSN	1439-4227
DOI	10.1002/cbic.202300093
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article: PKHB1 Tumor Cell Lysate Induces Antitumor Immune System Stimulation and Tumor Regression in Syngeneic Mice with Tumoral T Lymphoblasts.

Martínez-Torres, Ana Carolina / Calvillo-Rodríguez, Kenny Misael / Uscanga-Palomeque, Ashanti Concepción / Gómez-Morales, Luis / Mendoza-Reveles, Rodolfo / Caballero-Hernández, Diana / Karoyan, Philippe / Rodríguez-Padilla, Cristina

Journal of oncology

2019 Volume 2019, Page(s) 9852361

Abstract: Acute lymphocytic leukemia (ALL) is the most common pediatric cancer. Currently, treatment options for patients with relapsed and refractory ALL mostly rely on immunotherapies. However, hematological cancers are commonly associated with a low ... ...

Abstract	Acute lymphocytic leukemia (ALL) is the most common pediatric cancer. Currently, treatment options for patients with relapsed and refractory ALL mostly rely on immunotherapies. However, hematological cancers are commonly associated with a low immunogenicity and immune tolerance, which may contribute to leukemia relapse and the difficulties associated with the development of effective immunotherapies against this disease. We recently demonstrated that PKHB1, a TSP1-derived CD47 agonist peptide, induces immunogenic cell death (ICD) in T cell ALL (T-ALL). Cell death induced by PKHB1 on T-ALL cell lines and their homologous murine, L5178Y-R (T-murine tumor lymphoblast cell line), induced damage-associated molecular patterns (DAMPs) exposure and release. Additionally, a prophylactic vaccination with PKHB1-treated L5178Y-R cells prevented tumor establishment
Language	English
Publishing date	2019-06-04
Publishing country	Egypt
Document type	Journal Article
ZDB-ID	2461349-6
ISSN	1687-8469 ; 1687-8450
ISSN (online)	1687-8469
ISSN	1687-8450
DOI	10.1155/2019/9852361
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article ; Online: Small AntiMicrobial Peptide With in Vivo Activity Against Sepsis.

Boullet, Héloise / Bentot, Fayçal / Hequet, Arnaud / Ganem-Elbaz, Carine / Bechara, Chérine / Pacreau, Emeline / Launay, Pierre / Sagan, Sandrine / Jolivalt, Claude / Lacombe, Claire / Moumné, Roba / Karoyan, Philippe

Molecules (Basel, Switzerland)

2019 Volume 24, Issue 9

Abstract: Antimicrobial peptides (AMPs) are considered as potential therapeutic sources of future antibiotics because of their broad-spectrum activities and alternative mechanisms of action compared to conventional antibiotics. Although AMPs present considerable ... ...

Abstract	Antimicrobial peptides (AMPs) are considered as potential therapeutic sources of future antibiotics because of their broad-spectrum activities and alternative mechanisms of action compared to conventional antibiotics. Although AMPs present considerable advantages over conventional antibiotics, their clinical and commercial development still have some limitations, because of their potential toxicity, susceptibility to proteases, and high cost of production. To overcome these drawbacks, the use of peptides mimics is anticipated to avoid the proteolysis, while the identification of minimalist peptide sequences retaining antimicrobial activities could bring a solution for the cost issue. We describe here new polycationic β-amino acids combining these two properties, that we used to design small dipeptides that appeared to be active against Gram-positive and Gram-negative bacteria, selective against prokaryotic versus mammalian cells, and highly stable in human plasma. Moreover, the in vivo data activity obtained in septic mice reveals that the bacterial killing effect allows the control of the infection and increases the survival rate of cecal ligature and puncture (CLP)-treated mice.
MeSH term(s)	Amino Acids/chemistry ; Animals ; Anti-Infective Agents/administration & dosage ; Anti-Infective Agents/chemical synthesis ; Anti-Infective Agents/chemistry ; Anti-Infective Agents/pharmacology ; Antimicrobial Cationic Peptides/administration & dosage ; Antimicrobial Cationic Peptides/chemical synthesis ; Antimicrobial Cationic Peptides/chemistry ; Antimicrobial Cationic Peptides/pharmacology ; Disease Models, Animal ; Drug Design ; Gram-Negative Bacteria/drug effects ; Gram-Positive Bacteria/drug effects ; Humans ; Mice ; Microbial Sensitivity Tests ; Molecular Mimicry ; Proteolysis ; Sepsis/drug therapy ; Sepsis/etiology ; Sepsis/microbiology
Chemical Substances	Amino Acids ; Anti-Infective Agents ; Antimicrobial Cationic Peptides
Language	English
Publishing date	2019-05-01
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	1413402-0
ISSN	1420-3049 ; 1431-5165 ; 1420-3049
ISSN (online)	1420-3049
ISSN	1431-5165 ; 1420-3049
DOI	10.3390/molecules24091702
Database	MEDical Literature Analysis and Retrieval System OnLINE

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