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The cytoplasmic tail (CT) of the HIV-2 envelope glycoprotein (Env) includes amino acid (aa) sequences that are similar to lentiviral lytic peptides (LLP) described in other lentiviruses. Within the putative LLP-2 region, we previously observed insertions of 3 or 7 aa in sequences deduced from plasma viral RNA of symptomatic HIV-2-infected individuals. Based on these observations, we reproduced the insertions in a molecular clone to assess their impact on replicative fitness and cell death in vitro. Using a molecular clone of the HIV-2 reference strain, site-directed mutagenesis experiments allowed the generation of plasmids with the insertion LTAI or LQRALTAI in the Env protein. The clone with 7 aa insertion enhanced viral release 8 to 11 times in infected T cells and cell viability was impaired by more than 20%, compared with the wild-type HIV-2 virus. The effect of the 3 aa insertion was milder, with a nonsignificant trend to enhance viral replication and cell death compared with the wild-type virus. Interestingly, the insertions in the Env proteins did not induce a significant increase of viral infectivity, as revealed by the infectivity assay using TZM-bl cells. The insertions in the Env CT observed in vivo from disease progressors may, therefore, be involved in the higher viral load observed in these individuals. This study may open the way to the development of a prognostic marker related to the HIV-2 infection progression.

The Human Immunodeficiency Virus type 2 (HIV-2) is the second etiologic agent causing AIDS (acquired immune deficiency syndrome) in the human host. However, this retrovirus may be considered as an attenuated model of retroviral infection since the HIV-2-infected individuals show a longer asymptomatic phase, lower plasmatic viral loads without antiviral therapy, and do not experience AIDS-like symptoms in 60-70% of cases, in striking contrast with HIV-1-infected patients. HIV-2-positive individuals appear to control the virus replication and the main hypothesis that could explain this phenotype is a strong T cell-mediated immunity and a robust early innate immune response against HIV-2. In this thesis research project, we focus on a host restriction factor involved in the antiviral immune response: BST-2/Tetherin. This interferon (IFN)-inducible protein is able to retain the budding virions at the plasma membrane of the infected cells, and promotes the endocytosis and degradation of the “tethered” viral particle. HIVs have evolved means to counteract BST-2/Tetherin in order to ensure the viral dissemination in the human host. HIV-1 uses the accessory Vpu protein to bind and degrade BST-2/Tetherin, whereas HIV-2 - that lacks Vpu - relies on its envelope (Env) glycoprotein. It has been reported that the HIV-2 envelope glycoproteins bind and remove BST-2 from the cell membrane, but this countermeasure does not result in the degradation of BST-2. HIV-2 Env and BST-2 interact mainly through their ectodomain. However, little was known concerning the domain in the Env protein that can exert this function. During this research project, we first revealed the precise motif within the ectodomain of HIV-2 Env protein involved in the anti-tetherin function. Indeed, we demonstrated that the N659 residue is clearly involved in the antagonism of BST-2/Tetherin. We also showed that the cytoplasmic tail (CT) of the HIV-2 Env protein cooperates in this anti-tetherin function. BST-2/Tet, (BIFA - Sciences biomédicales et pharmaceutiques) -- UCL, 2019

[This corrects the article DOI: 10.1371/journal.pone.0209561.].

Group IV cytosolic phospholipase A2 (cPLA2α) plays a critical role in inflammatory processes. It produces arachidonic acid which is the main source of the pro-inflammatory eicosanoids mediators that are important in innate immune system. In some cases, these pro-inflammatory mediators cause damages to the host tissues and therefore promote autoimmune diseases. Consequently, development of potent inhibitors against cPLA2α could improve the therapy of inflammatory diseases. In the last two decades, intense efforts have been done to find potent cPLA2α inhibitors. Several scaffolds have been developed with the use of structure-activity relationship (SAR) studies, and potent inhibitors have been obtained. The poor absorption of these compounds from intestine was the main challenge for clinical application. This review illustrates the search for cPLA2α inhibitors, their SAR studies and biological effects., SCOPUS: re.j, info:eu-repo/semantics/published

INTRODUCTION: The WHO urges action against the threat posed by HIV drug resistance. It is well known that the sensitivity of Next-Generation Sequencing (NGS) is greater than that of Sanger Sequencing (SS). The objective of this study was to evaluate the performance of the novel NGS HIV-1 drug resistance monitoring system. MATERIALS & METHODS: NGS analyses were performed on 67 plasma samples from HIV-1 infected patients using the Sentosa SQ HIV Genotyping Assay from Vela-Dx. This kit was used on a semi-automated Ion Torrent-based platform. Sequences were compared to those obtained by SS. Samples were analysed in the same and in separate runs. Quality controls (QC) were added to control sequencing processes of protease (PRO), reverse transcriptase (RT) and integrase (INT) regions. RESULTS: Of the 41 analysed samples, 33 (80.5%) had identical drug resistance interpretation reports. Discrepant results were observed for eight samples. Five of them were only detected by NGS and had drug resistance mutations (DRMs) with an allelic frequency below the limit of detection of the SS method (between 6.3 to 20.5%). Two DRMs were only identified using the SS method. The sequences were similar in 98.2% of cases (counting variants as mismatches) and homologous in 99.9% if missed variants. Duplicated samples in a single run were similar in 95.7% (99.9%) of cases. Duplicated samples in two different runs were 98% (100%) homologous. QC results were manually assessed with a score of 340/340 for detection of DRMs in PRO and RT and 100% for INT sequencing. CONCLUSIONS: This is the first preliminary evaluation in Belgium employing the Sentosa SQ HIV Genotyping Assay. The NGS appears to be a promising tool for the detection of DRMs in HIV-1 patients and showed a higher sensitivity compared to SS. Large studies assessing the clinical relevance of low frequency DRMs are needed.

With the emergence of novel and more effective drug therapies, increased importance is being placed upon the methods by which these drugs are being delivered to the body. In conventional drug delivery systems, there is very little control over the release of drug. The effective concentration at the target site can be achieved by intermittent administration of grossly excessive doses, which, often results in constantly, unpredictable variations in plasma concentrations, with the risk of reaching levels below or above the therapeutic range leading to marked side effects. A plethora of formulation strategies mainly based on polymeric/lipid nanoparticles, are described in literature. Even though these systems are therapeutically advantageous in comparison to conventional systems, they remain insensitive to the changing metabolic states of the body although the symptoms of most metabolic diseases follow a rhythmic pattern.A more appropriate and effective approach of managing some of these conditions lies in the chronotherapy. This approach allows for pulsed or self-regulated drug delivery which is adjusted to the staging of biological rhythms, since the onset of certain diseases exhibits strong circadian temporal dependence. In order to reach the objective of mimicking the biophysical and biochemical processes of pathological states, many innovations in material design for drug delivery systems (DDS) that are able to release the therapeutic payload-on-demand were done to release the therapeutic agent only when it is required, according to the physiological need. The development of multidisciplinary research teams has brought huge advantages in the design, fabrication and utilization of such smart systems, especially in the pharmaceutical field. Interestingly, numerous smart polymeric materials exhibit a response to a specific stimulus. A step further, the elaboration of purpose-built monomers can give rise to compounds with tunable sensitivities or multi-stimuli responsi, Doctorat en Sciences biomédicales et pharmaceutiques (Pharmacie), info:eu-repo/semantics/nonPublished

The heme enzyme myeloperoxidase (MPO) participates in innate immune defense mechanism through formation of microbicidal reactive oxidants. However, evidence has emerged that MPO-derived oxidants contribute to propagation of inflammatory diseases. Because of the deleterious effects of circulating MPO, there is a great interest in the development of new efficient and specific inhibitors. Here, we have performed a novel virtual screening procedure, depending on ligand-based pharmacophore modeling followed by structure-based virtual screening. Starting from a set of 727842 compounds, 28 molecules were selected by this virtual method and tested on MPO in vitro. Twelve out of 28 compounds were found to have an IC50 less than 5 μM. The best inhibitors were 2-(7-methoxy-4-methylquinazolin-2-yl)guanidine (28) and (R)-2-(1-((2,3-dihydro-1H-imidazol-2-yl)methyl)pyrrolidin-3-yl)-5-fluoro-1H-benzo[d]imidazole (42) with IC50 values of 44 and 50 nM, respectively. Studies on the mechanism of inhibition suggest that 28 is the first potent mechanism-based inhibitor and inhibits irreversibly MPO at nanomolar concentration., SCOPUS: ar.j, info:eu-repo/semantics/published

The “Journées Franco-Belges de Pharmacochimie” is a recognized two-day annual meeting on Medicinal Chemistry that is renowned for the advanced science presented, conviviality, and outstanding opportunities for senior and young scientists to exchange knowledge. Abstracts of plenary lectures, oral communications, and posters presented during the meeting are collected in this report., SCOPUS: ar.j, info:eu-repo/semantics/published

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Lung cancer is the deadliest cancer in the world, with a global 5-year survival rate of about 15%. Despite a notable impact of the latest improvements in prevention, screening, detection and staging, the efficacy of conventional treatments is not sufficient and has reached a therapeutic plateau. These conventional treatments involve a combination of surgery, radiotherapy (RT) and chemotherapy (CT). CT is used in almost all stages: in operable and inoperable stages to limit tumour cell invasion and in latest stages as a palliative treatment. Cisplatin is one of the most frequently used and most potent drugs available. It is administered by parenteral route at doses limited by its high and cumulative nephrotoxicity but also by other systemic toxicities (e.g. ototoxicity). Its administration therefore requires many precautions (long hydration procedure, surveillance of the renal function), which mobilize medical personnel. A major limitation of parental CT is the low concentration of drug that successfully reaches the tumour or the metastases. A potential additional modality could be aerosolized CT to localize lung cancer treatment. It has shown a relative local tolerance for cisplatin through preclinical and clinical studies in humans by means of nebulized solutions or liposomal formulations. As a local treatment, aerosolized CT has a clear pharmacokinetic (PK) advantage, as it can increase local exposure while decreasing systemic exposure. However, because CT drugs, such as cisplatin, are active at rather high doses (in the mg range), the duration of administration from nebulizers is very long as it depends on the drug solubility or on drug encapsulation into liposomes. They also pose a high risk of environmental contamination and require HEPA-filtrated hoods during the nebulization procedure. Of all the inhalation devices available to deliver high drug doses, dry powder inhalers (DPIs) were chosen in this work. These were chosen to circumvent the above issues by pro, Doctorat en Sciences biomédicales et pharmaceutiques (Pharmacie), info:eu-repo/semantics/nonPublished

The implementation of dynamic combinatorial libraries allowed the determination of highly active reversible and irreversible inhibitors of myeloperoxidase (MPO) at the nanomolar level. Docking experiments highlighted the interaction between the most active ligands and MPO, and further kinetic studies defined the mode of inhibition of these compounds. Finally, in vivo evaluation showed that one dose of irreversible inhibitors is able to suppress the activity of MPO after inducing inflammation., SCOPUS: ar.j, info:eu-repo/semantics/published

Le laboratoire de Chimie Organique et Photochimie de l’ULB s’est intensivement impliqué dans la recherche portant sur le développement et l’étude de complexes polyazaaromatiques de ruthéniumII. En utilisant des ligands π-déficients tels que le 1,4,5,8-tétraazaphénanthrène (TAP) chélatés au centre métallique de RuII, des propriétés d’oxydo-réduction particulières à l’état excité du complexe peuvent être obtenues. Cette recherche s’est principalement focalisée sur l’étude de complexes de RuII photoréactifs dans un cadre biologique puisque ces complexes sont capables de photoréagir avec le matériel génétique ou les protéines par l’intermédiaire d’un transfert d’électron photo-induit (PET). Cependant, il existe un obstacle majeur à l’utilisation thérapeutique des complexes polyazaaromatiques de RuII, à savoir leur incapacité à traverser d’eux-mêmes la membrane des cellules vivantes. Ce projet vise à développer une stratégie ciblée de vectorisation de ces complexes, ce qui pourrait permet d’administrer l’agent thérapeutique uniquement aux cellules « malades ». Le ciblage de récepteurs surexprimés par les cellules endothéliales néo-formées, tels que l’intégrine αvβ3, a été envisagé dans le cadre de ce travail grâce à un ligand peptidique c(RGDfK). Ce ciblage associé à l’utilisation d’un complexe photoréactif de RuII permettrait un contrôle du type cellulaire, par la reconnaissance des intégrines αvβ3, ainsi qu’un contrôle temporel de l’activité thérapeutique du complexe, par l’illumination. De manière à combiner ces agents de ciblage et l’agent thérapeutique (complexe de RuII), des plateformes moléculaires de deux types ont été utilisées et comparées entre elles, à savoir le cyclodécapeptide RAFT et un calix[4]arène. La synthèse des conjugués RuII-RAFT-[c-(RGDfK)]4 et le RuII-calix[4]arène-[c-(RGDfK)]4 a donc été réalisée avec succès et leurs propriétés photophysiques et photochimiques ont été étudiées de manière à vérifier que la présence de la plateforme ne modifie pas, Doctorat en Sciences, info:eu-repo/semantics/nonPublished

BST-2 or tetherin is a host cell restriction factor that prevents the budding of enveloped viruses at the cell surface, thus impairing the viral spread. Several countermeasures to evade this antiviral factor have been positively selected in retroviruses: the human immunodeficiency virus type 2 (HIV-2) relies on the envelope glycoprotein (Env) to overcome BST-2 restriction. The Env gp36 ectodomain seems involved in this anti-tetherin activity, however residues and regions interacting with BST-2 are not clearly defined. Among 32 HIV-2 ROD Env mutants tested, we demonstrated that the asparagine residue at position 659 located in the gp36 ectodomain is mandatory to exert the anti-tetherin function. Viral release assays in cell lines expressing BST-2 showed a loss of viral release ability for the HIV-2 N659D mutant virus compared to the HIV-2 wild type virus. In bst-2 inactivated H9 cells, those differences were lost. Subtilisin treatment of infected cells demonstrated that the N659D mutant was more tethered at the cell surface. Förster resonance energy transfer (FRET) experiments confirmed a direct molecular link between Env and BST-2 and highlighted an inability of the mutant to bind BST-2. We also tested a virus presenting a truncation of 109 amino acids at the C-terminal part of Env, a cytoplasmic tail partial deletion that is spontaneously selected in vitro. Interestingly, viral release assays and FRET experiments indicated that a full Env cytoplasmic tail was essential in BST-2 antagonism. In HIV-2 infected cells, an efficient Env-mediated antagonism of BST-2 is operated through an intermolecular link involving the asparagine 659 residue as well as the C-terminal part of the cytoplasmic tail.

Le cancer du poumon est l’un des cancers les plus fréquents dans le monde et reste le plus meurtrier actuellement en terme d’incidence absolue. Les traitements employés chez les patients atteints d’un cancer du poumon consistent en une combinaison de chirurgie, de radiothérapie et de chimiothérapie. Alors qu’il y a quelques années, les guidelines de traitement étaient principalement basées sur le stade clinique de la maladie, le développement de nouvelles thérapies a mené à une classification plus appropriée des cancers du poumon. Cette nouvelle classification se base, en plus du stade clinique de la maladie, sur l’expression de différents biomarqueurs exprimés chez des sous-populations bien définies de patients. Ces biomarqueurs sont par exemple la mutation d’un gène ou l’expression d’une protéine. Au cours de ces dix dernières années, la recherche a été très active dans ce domaine avec l’arrivée de nouveaux traitements plus spécifiques pour ces sous-populations de patients. Des exemples concrets de ces nouvelles thérapies sont les chimiothérapies dites ciblées et l’immunothérapie. L’arrivée de tels traitements a parmi d’augmenter significativement le pronostic de la maladie et également de réduire considérablement les graves effets secondaires des chimiothérapies conventionnelles. Toutefois, le bénéfice en termes de survie reste modéré. Le taux de survie des patients à cinq ans est actuellement de 15%. Il y a donc toujours un besoin urgent de mettre au point de nouvelles stratégie de traitement.La chimiothérapie inhalée constitue une perspective de traitement adjuvant du cancer du poumon très intéressante, comparée à la chimiothérapie conventionnelle. En effet, elle permettrait d’administrer des doses d’anticancéreux plus importantes directement au niveau du site tumoral tout en limitant l’exposition systémique du médicament dans l’organisme, et donc, les toxicités importantes s’y rapportant. Toutefois, aucun médicament suivant cette approche n’est actuellement di, Lung cancer is one of the most frequent cancers in the world, and remains the most deadly. Lung cancer therapy involves the combination of surgery, radiotherapy and chemotherapy. Whereas the treatment guidelines used to be related mainly to the stage of the disease, more recent treatments have introduced the concept of treating lung cancers according not only to the stage, but also to the specific characteristics of the tumors, i.e. a gene mutation, expression of a protein, etc. In the last decade, scientific and clinical research has been very active in this field, with recurrent introduction of new treatments, including new chemotherapies (e.g. targeted chemotherapies and immunotherapies). Many of these new treatments certainly induce better therapeutic responses and a sharp reduction in the adverse effects of conventional chemotherapies for well-defined subpopulations of patients. However, the benefit in terms of survival rates is only moderate. The five-year survival rate is currently ~15%. There is therefore no doubt that new treatment approaches and strategies are needed. One interesting approach is aerosolized chemotherapy. The pulmonary delivery of anti-cancer drugs could potentially be an interesting alternative to conventional adjuvant chemotherapy in lung cancer treatment, for many reasons. Among them, it could enhance the therapeutic ratio significantly by decreasing systemic severe toxicities and increasing anti-tumour efficacy. However, despite interesting clinical trial reports, all the strategies describing an aerosolized anti-cancer treatment have failed to bring new medicine on the market so far. The failures have been related mainly to (i) the inability to deliver proper and efficient drug doses in the lungs with the inhalation devices used in clinical trials (i.e. nebulizers), (ii) concerns about potential increase in lung toxicities engendered by these anti-cancer drug-based aerosols, and (iii) the requirement for adapted facilities to perform t, Doctorat en Sciences biomédicales et pharmaceutiques (Pharmacie), info:eu-repo/semantics/nonPublished

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Metal complexes have been the subject of numerous investigations in oncology but, despite the plethora of newly synthesized compounds, their precise mechanisms of action remain generally unknown or, for the best, incompletely determined. The continuous development of efficient and sensitive techniques in analytical chemistry and molecular biology gives scientists new tools to gather information on how metal complexes can be effective toward cancer. This review focuses on recent findings about the anticancer mechanism of action of metal complexes and how the ligands can be used to tune their pharmacological and physicochemical properties., SCOPUS: re.j, info:eu-repo/semantics/published

Inflammation is the initial response of the body to the harmful stimuli and it is achieved by the increased movement of leukocytes (especially granulocytes) from blood into injured tissues. It is required for healing wounds and infections. Despite their indispensable role in microbial killing, the inflammation reactions may also cause diseases to a host such as hay fever, atherosclerosis, and rheumatoid arthritis. The enzymes and oxidizing species released during the inflammatory process can cause damages to the host tissues which lead to inflammatory syndromes. The role of myeloperoxidase (MPO) in the inflammatory reactions is well documented. It contributes in killing the pathogens but it is also implicated in several inflammatory syndromes such as Parkinson's disease, Alzheimer's disease and atherosclerosis. Thus, this enzyme attracted more and more attention of the scientists and it became a target for drug designing. In the last decade, several reversible and irreversible MPO inhibitors were identified as very high potent inhibitors such as fluoroalkylindole, aromatic hydroxamic acid, thioxanthine and benzoic acid hydrazide derivatives. In this review, we tried to illustrate the MPO inhibitors and highlight their structure activity relationship (SAR). In this paper we also discussed the mechanism of the inhibitory effect of the most potent compounds., SCOPUS: re.j, info:eu-repo/semantics/published

Despite its important role in the immune system, myeloperoxidase (MPO) is implicated in a wide range of inflammatory syndromes due to its oxidative product HOCl. The oxidative damages caused by MPO make it a new target for developing promising anti-inflammatory agents. In this paper, we tried to understand the mechanism of MPO inhibition in order to facilitate the drug design, to develop more accurate virtual tests and to understand the structure-activity relationship., info:eu-repo/semantics/published

Les pathologies infectieuses, maladies causées par certains micro-organismes pathogènes parmi les bactéries, les virus, les champignons et les protozoaires, sont à l’origine des taux de mortalité et de morbidité élevés enregistrés surtout dans les pays en voie de développement où la majorité de la population n’a pas les moyens d'accéder aux soins de santé. Les résistances des micro-organismes aux antimicrobiens, observées actuellement dans la pratique médicale moderne, constituent un autre grand problème lié au traitement de ces maladies. Elles constituent l’une des menaces de santé les plus sérieuses et peuvent frapper n’importe qui dans le monde. Face à ces fléaux, il est urgent de découvrir de nouveaux agents antimicrobiens qui pourraient, éventuellement, présenter de nouveaux mécanismes d'action. Une bonne part des plantes utilisées en médecines traditionnelles contiennent des composants antimicrobiens utiles contre les infections et qui peuvent aider dans la lutte contre les maladies infectieuses liées à l’antibiorésistance. C’est dans cette optique que nous avons mené une enquête ethnobotanique sur les plantes médicinales utilisées contre les infections microbiennes en médecine traditionnelle Burundaise. Nous en avons inventorié 155 et sélectionné 5 d'entre elles (Justicia subsessilis Oliv. (Acanthaceae); Platostoma rotundifolium (Briq.) A. J. Paton (Lamiaceae), Virectaria major (Schum.) Verdc. (Rubiaceae), Pavetta ternifolia (Oliv.) Hiern (Rubiaceae), et Stomatanthes africanus (Oliv. & Hiern) R. M. King & H. Rob. (Asteraceae)) pour en étudier la composition phytochimique et les propriétés biologiques. Les extraits de ces plantes ont été évalués notamment pour leurs effets antibactériens direct (bactéricide ou bactériostatique) et indirect (modulation des mécanismes de résistance qui augmente ou restaure l’activité des antibiotiques sur des souches résistantes). Les cinq plantes retenues ont montré une activité antibactérienne, justifiant ainsi leur usage cont, Infectious pathologies are diseases caused by the transmission of some pathogenic microorganisms among bacteria, viruses, fungi and protozoa. They drive the high mortality and morbidity rates recorded especially in developing countries, where the majority of the population cannot afford to access health care. The antimicrobial resistances currently observed in modern medical practice represent another major problem in the treatment of these diseases. These resistances are one of the most serious population health threats and can strike anyone in the world. It has thus become urgent to discover new antimicrobial agents that could possibly have novel mechanisms of action.Many plants used in traditional medicines against infections harbor useful antimicrobial components that can help in the fight against infectious diseases and antibiotic resistances. In this context, we conducted an ethnobotanical survey of medicinal plants used in Burundian traditional medicine to treat microbial infections. We inventoried 155 herbs from which 5 (Justicia subsessilis Oliv. (Acanthaceae); Platostoma rotundifolium (Briq.) A. J. Paton (Lamiaceae), Virectaria major (Schum.) Verdc. (Rubiaceae), Pavetta ternifolia (Oliv.) Hiern (Rubiaceae), and Stomatanthes africanus (Oliv. & Hiern) R. M. King & H. Rob. (Asteraceae) were selected for phytochemical screening and biological assays. The extracts of these plants were evaluated for their antibacterial effects, direct (bacteriostatic or bactericidal) and indirect (inhibition of resistance mechanisms by increasing or restoring the activity of antibiotics against resistant strains). All the selected plants species have shown antibacterial activity, justifying their use against microbial infections in Burundian traditional medicine, and more particularly Platostoma rotundifolium, whose extracts showed direct and indirect antibacterial effects on susceptible and resistant (MRSA) strains. The extracts from Platostoma rotundifolium also presented inhi, Doctorat en Sciences biomédicales et pharmaceutiques (Pharmacie), info:eu-repo/semantics/nonPublished

Platinum-based drugs are commonly used in cancer treatment. The biological activity of a metallodrug is obviously closely related to its chemical and stereochemical characteristics. An overlooked aspect is the effect of the ligand to the electronic structure of the metal atom (coordinated atom). We report herein a Resonant X-ray Emission Spectroscopy (RXES) study on the chemical speciation of chiral platinum complexes in which diastereomers are distinguished on the basis of their metal electronic configuration. This demonstrates RXES high chemical speciation capabilities, a necessary property to further investigate the reactivity of the Pt atom towards nucleophiles or bionucleophiles, and an important complement the previously reported RXES abilities, namely that it can be employed for in situ studies at physiological concentrations., SCOPUS: ar.j, info:eu-repo/semantics/published

Low estradiol level in postmenopausal women is implicated in osteoporosis, which occurs because of the high bone resorption rate. Estrogen formation is controlled by 17-β hydroxysteroid dehydrogenase 17-β HSD enzymes, where 17-β HSD type 1 contributes in the formation of estradiol, while type 2 catalyzes its catabolism. Inhibiting 17-β HSD2 can help in increasing estradiol concentration. Several promising 17-β HSD2 inhibitors that can act at low nanomolar range have been identified. However, there are some specific challenges associated with the application of these compounds. Our review provides an up-to-date summary of the current status and recent progress in the production of 17-β HSD2 inhibitors as well as the future challenges in their clinical application., SCOPUS: re.j, info:eu-repo/semantics/published

The “Journées Franco-Belges de Pharmacochimie” is a recognized two-day annual meeting on Medicinal Chemistry that is renowned for the advanced science presented, conviviality, and outstanding opportunities for senior and young scientists to exchange knowledge. Abstracts of plenary lectures, oral communications, and posters presented during the meeting are collected in this report.

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