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Article ; Online: A Biomimetic Multiparametric Assay to Characterise Anti-Amyloid Drugs.

Smeralda, Willy / Since, Marc / Corvaisier, Sophie / Fayolle, Dimitri / Cardin, Julien / Duprey, Sylvain / Jourdan, Jean-Pierre / Cullin, Christophe / Malzert-Freon, Aurélie

International journal of molecular sciences

2023 Volume 24, Issue 23

Abstract: Alzheimer's disease (AD) is the most widespread form of senile dementia worldwide and represents a leading socioeconomic problem in healthcare. Although it is widely debated, the aggregation of the amyloid β peptide (Aβ) is linked to the onset and ... ...

Abstract	Alzheimer's disease (AD) is the most widespread form of senile dementia worldwide and represents a leading socioeconomic problem in healthcare. Although it is widely debated, the aggregation of the amyloid β peptide (Aβ) is linked to the onset and progression of this neurodegenerative disease. Molecules capable of interfering with specific steps in the fibrillation process remain of pharmacological interest. To identify such compounds, we have set up a small molecule screening process combining multiple experimental methods (UV and florescence spectrometry, ITC, and ATR-FTIR) to identify and characterise potential modulators of Aβ
MeSH term(s)	Humans ; Alzheimer Disease/drug therapy ; Alzheimer Disease/metabolism ; Amyloid beta-Peptides/metabolism ; Neurodegenerative Diseases ; Biomimetics ; Amyloid
Chemical Substances	Amyloid beta-Peptides ; Amyloid
Language	English
Publishing date	2023-11-30
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2019364-6
ISSN	1422-0067 ; 1422-0067 ; 1661-6596
ISSN (online)	1422-0067
ISSN	1422-0067 ; 1661-6596
DOI	10.3390/ijms242316982
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Article ; Online: A Biomimetic Multiparametric Assay to Characterise Anti-Amyloid Drugs

Willy Smeralda / Marc Since / Sophie Corvaisier / Dimitri Fayolle / Julien Cardin / Sylvain Duprey / Jean-Pierre Jourdan / Christophe Cullin / Aurélie Malzert-Freon

International Journal of Molecular Sciences, Vol 24, Iss 23, p

2023 Volume 16982

Abstract: Alzheimer’s disease (AD) is the most widespread form of senile dementia worldwide and represents a leading socioeconomic problem in healthcare. Although it is widely debated, the aggregation of the amyloid β peptide (Aβ) is linked to the onset and ... ...

Abstract	Alzheimer’s disease (AD) is the most widespread form of senile dementia worldwide and represents a leading socioeconomic problem in healthcare. Although it is widely debated, the aggregation of the amyloid β peptide (Aβ) is linked to the onset and progression of this neurodegenerative disease. Molecules capable of interfering with specific steps in the fibrillation process remain of pharmacological interest. To identify such compounds, we have set up a small molecule screening process combining multiple experimental methods (UV and florescence spectrometry, ITC, and ATR-FTIR) to identify and characterise potential modulators of Aβ 1-42 fibrillation through the description of the biochemical interactions (molecule–membrane Aβ peptide). Three known modulators, namely bexarotene, Chicago sky blue and indomethacin, have been evaluated through this process, and their modulation mechanism in the presence of a biomembrane has been described. Such a well-adapted physico-chemical approach to drug discovery proves to be an undeniable asset for the rapid characterisation of compounds of therapeutic interest for Alzheimer’s disease. This strategy could be adapted and transposed to search for modulators of other amyloids such as tau protein.
Keywords	Alzheimer’s disease ; liposomes ; β-amyloïd ; drug discovery ; bexarotene ; indomethacin ; Biology (General) ; QH301-705.5 ; Chemistry ; QD1-999
Subject code	540
Language	English
Publishing date	2023-11-01T00:00:00Z
Publisher	MDPI AG
Document type	Article ; Online
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Article: Thermal Behavior of Ti-64 Primary Material in Electron Beam Melting Process.

Bellot, Jean-Pierre / Jourdan, Julien / Kroll-Rabotin, Jean-Sébastien / Quatravaux, Thibault / Jardy, Alain

Materials (Basel, Switzerland)

2021 Volume 14, Issue 11

Abstract: The Electron Beam Melting (EBM) process has emerged as either an alternative or a complement to vacuum arc remelting of titanium alloys, since it is capable of enhancing the removal of exogenous inclusions by dissolution or sedimentation. The melting of ... ...

Abstract	The Electron Beam Melting (EBM) process has emerged as either an alternative or a complement to vacuum arc remelting of titanium alloys, since it is capable of enhancing the removal of exogenous inclusions by dissolution or sedimentation. The melting of the primary material is a first step of this continuous process, which has not been studied so far and is investigated experimentally and numerically in the present study. Experiments have been set up in a 100 kW laboratory furnace with the aim of analyzing the effect of melting rate on surface temperature of Ti-64 bars. It was found that melting rate is nearly proportional to the EB power while the overheating temperature remains roughly independent of the melting rate and equal to about 100 °C. The emissivity of molten Ti-64 was found to be 0.22 at an average temperature of about 1760 °C at the tip of the bar. In parallel, a mathematical model of the thermal behavior of the material during melting has been developed. The simulations revealed valuable results about the melting rate, global heat balance and thermal gradient throughout the bar, which agreed with the experimental values to a good extent. The modeling confirms that the overheating temperature of the tip of the material is nearly independent of the melting rate.
Language	English
Publishing date	2021-05-26
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2487261-1
ISSN	1996-1944
ISSN	1996-1944
DOI	10.3390/ma14112853
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Article ; Online: Drug repositioning: a brief overview.

Jourdan, Jean-Pierre / Bureau, Ronan / Rochais, Christophe / Dallemagne, Patrick

The Journal of pharmacy and pharmacology

2020 Volume 72, Issue 9, Page(s) 1145–1151

Abstract: Objectives: Drug repositioning, that is, the use of a drug in an indication other than the one for which it was initially marketed, is a growing trend. Its origins lie mainly in the attrition experienced in recent years in the field of new drug ... ...

Abstract	Objectives: Drug repositioning, that is, the use of a drug in an indication other than the one for which it was initially marketed, is a growing trend. Its origins lie mainly in the attrition experienced in recent years in the field of new drug discovery. Key findings: Despite some regulatory and economic challenges, drug repositioning offers many advantages, and a number of recent successes have confirmed both its public health benefits and its commercial value. The first examples of successful drug repositioning mainly came about through serendipity like acetylsalicylic acid, thalidomide, sildenafil or dimethylfumarate. Conclusion: The history of great-repositioned drugs has given some solutions to various pathologies. Serendipity is not yet useful to find repositioning drugs. Drug repositioning is of growing interest. Nowadays, a more rational approach to the identification of drug candidates for repositioning is possible, especially using data mining.
MeSH term(s)	Data Mining ; Drug Discovery/methods ; Drug Repositioning/economics ; Drug Repositioning/history ; Drug Repositioning/methods ; History, 19th Century ; History, 20th Century ; History, 21st Century ; Humans
Keywords	covid19
Language	English
Publishing date	2020-04-17
Publishing country	England
Document type	Historical Article ; Journal Article ; Review
ZDB-ID	3107-0
ISSN	2042-7158 ; 0022-3573 ; 0373-1022
ISSN (online)	2042-7158
ISSN	0022-3573 ; 0373-1022
DOI	10.1111/jphp.13273
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Article ; Online: Implementation of clinical medication review in a geriatric ward to reduce potentially inappropriate prescriptions among older adults.

Meurant, Alexandre / Lescure, Pascale / Lafont, Claire / Pommier, Wilhelm / Delmas, Claire / Descatoire, Pablo / Baudon, Marie / Muzard, Alexandra / Villain, Cédric / Jourdan, Jean-Pierre

European journal of clinical pharmacology

2023 Volume 79, Issue 10, Page(s) 1391–1400

Abstract: Purpose: The impact of several pharmaceutical interventions to reduce the use of potentially inappropriate medications (PIMs) and potentially omitted medications (POMs) has been recently studied. We aimed to determine whether clinical medication review ( ...

Abstract	Purpose: The impact of several pharmaceutical interventions to reduce the use of potentially inappropriate medications (PIMs) and potentially omitted medications (POMs) has been recently studied. We aimed to determine whether clinical medication review (CMR) (i.e. a systematic and patient-centred clinical assessment of all medicines currently taken by a patient) performed by a geriatrician and a pharmacist added to standard pharmaceutical care (SPC) (i.e. medication reconciliation and regular prescription review by the pharmacist) resulted in more appropriate prescribing compared to SPC among older inpatients. Methods: A retrospective observational single-centre study was conducted in a French geriatric ward. Six criteria for appropriate prescribing were chosen: the number of PIMs and POMs as defined by the STOPP/STARTv2 list, the total number of drugs prescribed, the number of administrations per day and the number of psychotropic and anticholinergic drugs. These criteria were compared between CMR and SPC group using linear and logistic regression models weighted on propensity scores. Results: There were 137 patients included, 66 in the CMR group and 71 in the SPC group. The mean age was 87 years, the sex ratio was 0.65, the mean number of drugs prescribed was 9, the mean MMSE was 21 and at admission 242 POMs, and 363 PIMs were prescribed. Clinical medication review did not reduce the number of PIMs at discharge compared to SPC (beta = - 0.13 [- 0.84; 0.57], p = 0.71) nor did it reduce the number of drugs prescribed (p = 0.10), the number of psychotropic drugs (p = 0.17) or the anticholinergic load (p = 0.87). Clinical medication review resulted in more POMs being prescribed than in standard pharmaceutical care (beta = - 0.39 [- 0.72; - 0.06], p = 0.02). Cardiology POMs were more implemented in the medication review group (p = 0.03). Conclusion: Clinical medication review did not reduce the number of PIMs but helped clinicians introduce underused drugs, especially cardiovascular drugs, which are known to be associated with morbidity and mortality risk reduction.
MeSH term(s)	Aged, 80 and over ; Humans ; Cholinergic Antagonists ; Inappropriate Prescribing/prevention & control ; Medication Review ; Potentially Inappropriate Medication List ; Retrospective Studies
Chemical Substances	Cholinergic Antagonists
Language	English
Publishing date	2023-08-19
Publishing country	Germany
Document type	Journal Article ; Observational Study
ZDB-ID	121960-1
ISSN	1432-1041 ; 0031-6970
ISSN (online)	1432-1041
ISSN	0031-6970
DOI	10.1007/s00228-023-03551-y
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Article ; Online: Desirable drug-drug interactions or when a matter of concern becomes a renewed therapeutic strategy.

Guieu, Benjamin / Jourdan, Jean-Pierre / Dreneau, Aurore / Willand, Nicolas / Rochais, Christophe / Dallemagne, Patrick

Drug discovery today

2020 Volume 26, Issue 2, Page(s) 315–328

Abstract: Drug-drug interactions are sometimes considered to be detrimental and responsible for adverse effects. In some cases, however, some are stakeholders of the efficiency of the treatment and this combinatorial strategy is exploited by some drug associations, ...

Abstract	Drug-drug interactions are sometimes considered to be detrimental and responsible for adverse effects. In some cases, however, some are stakeholders of the efficiency of the treatment and this combinatorial strategy is exploited by some drug associations, including levodopa (L-Dopa) and dopadecarboxylase inhibitors, β-lactam antibiotics and clavulanic acid, 5-fluorouracil (5-FU) and folinic acid, and penicillin and probenecid. More recently, some drug-drug combinations have been integrated in modern drug design strategies, aiming to enhance the efficiency of already marketed drugs with new compounds acting not only as synergistic associations, but also as real boosters of activity. In this review, we provide an update of examples of such strategies, with a special focus on microbiology and oncology.
MeSH term(s)	Animals ; Anti-Infective Agents/administration & dosage ; Anti-Infective Agents/pharmacology ; Antineoplastic Agents/administration & dosage ; Antineoplastic Agents/pharmacology ; Drug Design ; Drug Interactions ; Drug Synergism ; Drug Therapy, Combination ; Humans
Chemical Substances	Anti-Infective Agents ; Antineoplastic Agents
Language	English
Publishing date	2020-11-27
Publishing country	England
Document type	Journal Article ; Review
ZDB-ID	1324988-5
ISSN	1878-5832 ; 1359-6446
ISSN (online)	1878-5832
ISSN	1359-6446
DOI	10.1016/j.drudis.2020.11.026
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Article: Drug repositioning: a brief overview

Jourdan, Jean-Pierre / Bureau, Ronan / Rochais, Christophe / Dallemagne, Patrick

J Pharm Pharmacol

Abstract: OBJECTIVES: Drug repositioning, that is, the use of a drug in an indication other than the one for which it was initially marketed, is a growing trend. Its origins lie mainly in the attrition experienced in recent years in the field of new drug discovery. ...

Abstract	OBJECTIVES: Drug repositioning, that is, the use of a drug in an indication other than the one for which it was initially marketed, is a growing trend. Its origins lie mainly in the attrition experienced in recent years in the field of new drug discovery. KEY FINDINGS: Despite some regulatory and economic challenges, drug repositioning offers many advantages, and a number of recent successes have confirmed both its public health benefits and its commercial value. The first examples of successful drug repositioning mainly came about through serendipity like acetylsalicylic acid, thalidomide, sildenafil or dimethylfumarate. CONCLUSION: The history of great-repositioned drugs has given some solutions to various pathologies. Serendipity is not yet useful to find repositioning drugs. Drug repositioning is of growing interest. Nowadays, a more rational approach to the identification of drug candidates for repositioning is possible, especially using data mining.
Keywords	covid19
Publisher	WHO
Document type	Article
Note	WHO #Covidence: #72101
Database	COVID19

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Article ; Online: Characteristics and clinical outcomes of SARS-CoV-2 infection in adult patients with acute leukemia in France.

Dumas, Pierre-Yves / Bertoli, Sarah / Bonmati, Caroline / Carre, Martin / Lambert, Juliette / Ojeda-Uribe, Mario / Chantepie, Sylvain / Paul, Franciane / Jourdan, Eric / Haiat, Stéphanie / Tavernier, Emmanuelle / Peterlin, Pierre / Marolleau, Jean-Pierre / Laribi, Kamel / Orvain, Corentin / Cabrera, Quentin / Turlure, Pascal / Girault, Stéphane / Balsat, Marie /

Bernard, Marc / Bene, Marie-Christine / Pigneux, Arnaud / Dombret, Hervé / Récher, Christian

Leukemia research

2022 Volume 120, Page(s) 106901

MeSH term(s)	Acute Disease ; Adult ; COVID-19/epidemiology ; France/epidemiology ; Humans ; Leukemia, Myeloid, Acute ; SARS-CoV-2
Language	English
Publishing date	2022-06-20
Publishing country	England
Document type	Letter ; Comment
ZDB-ID	752396-8
ISSN	1873-5835 ; 0145-2126
ISSN (online)	1873-5835
ISSN	0145-2126
DOI	10.1016/j.leukres.2022.106901
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Article ; Online: Hypomethylating agent monotherapy in core binding factor acute myeloid leukemia: a French multicentric retrospective study.

Gabellier, Ludovic / Peterlin, Pierre / Thepot, Sylvain / Hicheri, Yosr / Paul, Franciane / Gallego-Hernanz, Maria Pilar / Bertoli, Sarah / Turlure, Pascal / Pigneux, Arnaud / Guieze, Romain / Ochmann, Marlène / Malfuson, Jean-Valère / Cluzeau, Thomas / Thomas, Xavier / Tavernier, Emmanuelle / Jourdan, Eric / Bonnet, Sarah / Tudesq, Jean-Jacques / Raffoux, Emmanuel

Annals of hematology

2024 Volume 103, Issue 3, Page(s) 759–769

Abstract: Very few data are available about hypomethylating agent (HMA) efficiency in core binding factor acute myeloid leukemias (CBF-AML). Our main objective was to evaluate the efficacy and safety of HMA in the specific subset of CBF-AML. Here, we report the ... ...

Abstract	Very few data are available about hypomethylating agent (HMA) efficiency in core binding factor acute myeloid leukemias (CBF-AML). Our main objective was to evaluate the efficacy and safety of HMA in the specific subset of CBF-AML. Here, we report the results of a multicenter retrospective French study about efficacy of HMA monotherapy, used frontline or for R/R CBF-AML. Forty-nine patients were included, and received a median of 5 courses of azacitidine (n = 46) or decitabine (n = 3). ORR was 49% for the whole cohort with a median time to response of 112 days. After a median follow-up of 72.3 months, median OS for the total cohort was 10.6 months. In multivariate analysis, hematological relapse of CBF-AML at HMA initiation was significantly associated with a poorer OS (HR: 2.13; 95%CI: 1.04-4.36; p = 0.038). Responders had a significantly improved OS (1-year OS: 75%) compared to non-responders (1-year OS: 15.3%; p < 0.0001). Hematological improvement occurred for respectively 28%, 33% and 48% for patients who were red blood cell or platelet transfusion-dependent, or who experienced grade 3/4 neutropenia at HMA initiation. Adverse events were consistent with the known safety profile of HMA. Our study highlights that HMA is a well-tolerated therapeutic option with moderate clinical activity for R/R CBF-AML and for patients who cannot handle intensive chemotherapy.
MeSH term(s)	Humans ; Retrospective Studies ; Decitabine/therapeutic use ; Azacitidine/adverse effects ; Leukemia, Myeloid, Acute/drug therapy ; Core Binding Factors ; Antineoplastic Combined Chemotherapy Protocols/therapeutic use ; Treatment Outcome
Chemical Substances	Decitabine (776B62CQ27) ; Azacitidine (M801H13NRU) ; Core Binding Factors
Language	English
Publishing date	2024-01-26
Publishing country	Germany
Document type	Multicenter Study ; Journal Article
ZDB-ID	1064950-5
ISSN	1432-0584 ; 0939-5555 ; 0945-8077
ISSN (online)	1432-0584
ISSN	0939-5555 ; 0945-8077
DOI	10.1007/s00277-024-05623-0
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Article ; Online: Urban flood susceptibility modelling using AHP and GIS approach

Daouda Nsangou / Amidou Kpoumié / Zakari Mfonka / Abdou Nasser Ngouh / Donald Hermann Fossi / Camille Jourdan / Henri Zobo Mbele / Oumar Farikou Mouncherou / Jean-Pierre Vandervaere / Jules Remy Ndam Ngoupayou

Scientific African, Vol 15, Iss , Pp e01043- (2022)

case of the Mfoundi watershed at Yaoundé in the South-Cameroon plateau

2022

Abstract: Floods are considered as the natural hazards that affect the world's major metropolises the most. Thus, the present study aimed at evaluating the sensitivity to flood risks of the Mfoundi watershed (96.5 km2) located in the heart of the Cameroonian ... ...

Abstract	Floods are considered as the natural hazards that affect the world's major metropolises the most. Thus, the present study aimed at evaluating the sensitivity to flood risks of the Mfoundi watershed (96.5 km2) located in the heart of the Cameroonian political capital in a tropical humid forest zone, more precisely in the South Cameroon plateau. The methodological approach adopted was to identify the factors that most favor the risk of flooding in the area from intense literature review and field investigations; the analysis of these factors and the calculation of the Flood Harzard Index (FHI) using the Analytical Hierarchy Process (AHP) approach coupled with the Geographical Information System (GIS) environment. The results reveal that among the ten parameters of the natural environment (elevation, drainage density, rainfall, slope, distance from the river, topographic humidity, hydraulic conductivity, groundwater level, geology and land cover) selected, the land cover, elevation and the geology are the factors that most influences the flooding phenomenon in the area. The value of Flood Hazard Index (FHI) varied from 4.16 to 9.16, the higher the value, the more sensitive the area is to the risk of flooding. Five main classes of flood susceptibility are highlighted: very low, low, moderate, high and very high, representing 9.50, 26, 23, 22 and 19.5%, respectively of the study area. To validate the efficiency of the obtained flood susceptibility map, the adopted Area Under the Curve (AUC) method shows a very good accuracy (0.84 or 84%). The results of this study constitute a basic tool for decision-making for environmental management by public authorities and decentralised territorial authorities with territorial jurisdiction.
Keywords	Yaoundé-Cameroon ; Multi-criteria decision analysis ; Mapping ; Flood hazard ; Validation ; Science ; Q
Subject code	910
Language	English
Publishing date	2022-03-01T00:00:00Z
Publisher	Elsevier
Document type	Article ; Online
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