LIVIVO - Search results -

Search results

Result 1 - 10 of total 210

Search options

Article: MBC and ECBL libraries: outstanding tools for drug discovery.

Ginex, Tiziana / Madruga, Enrique / Martinez, Ana / Gil, Carmen

2023 Volume 14, Page(s) 1244317

Abstract: Chemical libraries have become of utmost importance to boost drug discovery processes. It is widely accepted that the quality of a chemical library depends, among others, on its availability and chemical diversity which help in rising the chances of ... ...

Abstract	Chemical libraries have become of utmost importance to boost drug discovery processes. It is widely accepted that the quality of a chemical library depends, among others, on its availability and chemical diversity which help in rising the chances of finding good hits. In this regard, our group has developed a source for useful chemicals named Medicinal and Biological Chemistry (MBC) library. It originates from more than 30 years of experience in drug design and discovery of our research group and has successfully provided effective hits for neurological, neurodegenerative and infectious diseases. Moreover, in the last years, the European research infrastructure for chemical biology EU-OPENSCREEN has generated the European Chemical Biology library (ECBL) to be used as a source of hits for drug discovery. Here we present and discuss the updated version of the MBC library (MBC v.2022), enriched with new scaffolds and containing more than 2,500 compounds together with ECBL that collects about 100,000 small molecules. To properly address the improved potentialities of the new version of our MBC library in drug discovery, up to 44 among physicochemical and pharmaceutical properties have been calculated and compared with those of other well-known publicly available libraries. For comparison, we have used ZINC20, DrugBank, ChEMBL library, ECBL and NuBBE along with an approved drug library. Final results allowed to confirm the competitive chemical space covered by MBC v.2022 and ECBL together with suitable drug-like properties. In all, we can affirm that these two libraries represent an interesting source of new hits for drug discovery.
Language	English
Publishing date	2023-08-11
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2587355-6
ISSN	1663-9812
ISSN	1663-9812
DOI	10.3389/fphar.2023.1244317
Database	MEDical Literature Analysis and Retrieval System OnLINE

Order via subito

This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

Article ; Online: Is drug repurposing really the future of drug discovery or is new innovation truly the way forward?

Gil, Carmen / Martinez, Ana

Expert opinion on drug discovery

2021 Volume 16, Issue 8, Page(s) 829–831

MeSH term(s)	Drug Discovery ; Drug Repositioning ; Humans
Language	English
Publishing date	2021-04-23
Publishing country	England
Document type	Editorial ; Research Support, Non-U.S. Gov't
ZDB-ID	2259618-5
ISSN	1746-045X ; 1746-0441
ISSN (online)	1746-045X
ISSN	1746-0441
DOI	10.1080/17460441.2021.1912733
Database	MEDical Literature Analysis and Retrieval System OnLINE

Full text online

Accessible to users with ZB MED library card

In stock of ZB MED Cologne/Königswinter

Zs.A 6388: Show issues

Location:
Je nach Verfügbarkeit (siehe Angabe bei Bestand)
bis Jg. 2021: Bestellungen von Artikeln über das Online-Bestellformular
ab Jg. 2022: Lesesaal (EG)

Order via subito

Details ▾

Article ; Online: Druggable cavities and allosteric modulators of the cell division cycle 7 (CDC7) kinase.

Rojas-Prats, Elisa / Martinez-Gonzalez, Loreto / Gil, Carmen / Ramírez, David / Martinez, Ana

Journal of enzyme inhibition and medicinal chemistry

2024 Volume 39, Issue 1, Page(s) 2301767

Abstract: Cell division cycle 7 kinase (CDC7) has been found overexpressed in many cancer cell lines being also one of the kinases involved in the nuclear protein TDP-43 ... ...

Abstract	Cell division cycle 7 kinase (CDC7) has been found overexpressed in many cancer cell lines being also one of the kinases involved in the nuclear protein TDP-43 phosphorylation
MeSH term(s)	Humans ; Phosphorylation ; Allosteric Site ; Cell Line ; Nuclear Proteins ; Cell Cycle ; Protein Serine-Threonine Kinases ; Cell Cycle Proteins
Chemical Substances	Nuclear Proteins ; CDC7 protein, human (EC 2.7.1.-) ; Protein Serine-Threonine Kinases (EC 2.7.11.1) ; Cell Cycle Proteins
Language	English
Publishing date	2024-01-11
Publishing country	England
Document type	Journal Article
ZDB-ID	2082578-X
ISSN	1475-6374 ; 1475-6366
ISSN (online)	1475-6374
ISSN	1475-6366
DOI	10.1080/14756366.2024.2301767
Database	MEDical Literature Analysis and Retrieval System OnLINE

In stock of ZB MED Cologne/Königswinter

Zs.A 3004: Show issues

Location:
Je nach Verfügbarkeit (siehe Angabe bei Bestand)
bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
Jg. 1995 - 2021: Lesesall (2.OG)
ab Jg. 2022: Lesesaal (EG)

Order via subito

Details ▾
- See ZB MED holdings
- Order with fees

Article ; Online: The emerging role of mixed lineage kinase 3 (MLK3) and its potential as a target for neurodegenerative diseases therapies.

Moreno, Ricardo / Recio, Javier / Barber, Santiago / Gil, Carmen / Martinez, Ana

European journal of medicinal chemistry

2023 Volume 257, Page(s) 115511

Abstract: Selective and brain-permeable protein kinase inhibitors are in preclinical development for treating neurodegenerative diseases. Among them, MLK3 inhibitors, with a potent neuroprotective biological action have emerged as valuable agents for the treatment ...

Abstract	Selective and brain-permeable protein kinase inhibitors are in preclinical development for treating neurodegenerative diseases. Among them, MLK3 inhibitors, with a potent neuroprotective biological action have emerged as valuable agents for the treatment of pathologies such as Alzheimer's, Parkinson's disease and amyotrophic lateral sclerosis. In fact, one MLK3 inhibitor, CEP-1347, reached clinical trials for Parkinson's disease. Additionally, another compound called prostetin/12k, a potent and rather selective MLK3 inhibitor has started clinical development for ALS based on its motor neuron protection in both in vitro and in vivo models. In this review, we will focus on the role of MLK3 in neuron-related cell death processes, neurodegenerative diseases, and the potential advantages of targeting this kinase through pharmacological modulation for neuroprotective treatment.
MeSH term(s)	Humans ; Neurodegenerative Diseases/drug therapy ; Parkinson Disease/drug therapy ; MAP Kinase Kinase Kinases ; Cell Death ; Mitogen-Activated Protein Kinase Kinase Kinase 11
Chemical Substances	MAP Kinase Kinase Kinases (EC 2.7.11.25)
Language	English
Publishing date	2023-05-24
Publishing country	France
Document type	Journal Article ; Review
ZDB-ID	188597-2
ISSN	1768-3254 ; 0009-4374 ; 0223-5234
ISSN (online)	1768-3254
ISSN	0009-4374 ; 0223-5234
DOI	10.1016/j.ejmech.2023.115511
Database	MEDical Literature Analysis and Retrieval System OnLINE

In stock of ZB MED Cologne/Königswinter

Zs.B 784: Show issues

Location:
Je nach Verfügbarkeit (siehe Angabe bei Bestand)
bis Jg. 2021: Bestellungen von Artikeln über das Online-Bestellformular
ab Jg. 2022: Lesesaal (EG)

Order via subito

Details ▾
- See ZB MED holdings
- Order with fees

Article: Neuroprotective properties of exosomes and chitosan nanoparticles of Tomafran, a bioengineered tomato enriched in crocins.

Etxebeste-Mitxeltorena, Mikel / Niza, Enrique / Fajardo, Cristián Martinez / Gil, Carmen / Gómez-Gómez, Lourdes / Martinez, Ana / Ahrazem, Oussama

Natural products and bioprospecting

2024 Volume 14, Issue 1, Page(s) 9

Abstract: Saffron has many pharmacological properties in addition to being a frequently used food seasoning. Crocin and picrocrocin which accumulate in saffron stigma, are responsible for these pharmacological properties. These natural products have health- ... ...

Abstract	Saffron has many pharmacological properties in addition to being a frequently used food seasoning. Crocin and picrocrocin which accumulate in saffron stigma, are responsible for these pharmacological properties. These natural products have health-promoting effects for the prevention and treatment of numerous diseases, including age-related cognitive and memory disfunction. Currently, crocin and picrocrocin are obtained from saffron, considered as the spice with the highest price in the market. To develop an efficient and low-cost approach to producing these compounds with high bioactivity, biosynthetic genes isolated from saffron can be exploited in the metabolic engineering of heterologous hosts and the production of crocins in productive crop plants. Recently, we engineered tomato fruit producing crocins (Tomafran). In this study, we demonstrated that crocin-rich extract, encapsulated in chitosan or in exosomes may function as a neuroprotective strategy. Crocins contained in the Tomafran extracts and much lower doses in chitosan nanoparticles or exosomes were enough to rescue the neuroblastoma cell line SH-SY5Y after damage caused by okadaic acid. Our results confirm the neuroprotective effect of Tomafran and its exosomes that may be useful for the delay or prevention of neurodegenerative disorders such as Alzheimer's disease.
Language	English
Publishing date	2024-01-12
Publishing country	Germany
Document type	Journal Article
ISSN	2192-2195
ISSN	2192-2195
DOI	10.1007/s13659-023-00425-9
Database	MEDical Literature Analysis and Retrieval System OnLINE

Order via subito

Inter-library loan at ZB MED

Your chosen title can be delivered directly to ZB MED Cologne location if you are registered as a user at ZB MED Cologne.

Article ; Online: Caring for others without neglecting oneself? Grandparent caregivers, gender, and perceived health-related quality of life.

García-Jiménez, María / Torres-Enamorado, Dolores / Sánchez-Sánchez, Elena / García-Gil, Carmen / Casado-Mejía, Rosa

Health care for women international

2024 , Page(s) 1–20

Abstract: In this study, we explored the impact of caregiving on quality of life and health perceptions and outlined the profile of grandparent caregivers in Andalusia (Spain) in terms of a range of sociodemographic variables related to the care of their ... ...

Abstract	In this study, we explored the impact of caregiving on quality of life and health perceptions and outlined the profile of grandparent caregivers in Andalusia (Spain) in terms of a range of sociodemographic variables related to the care of their grandchildren. A sample of 171 participants (21.6% men) completed the Health-Related Quality of Life (HRQoL) questionnaire and another ad hoc one providing sociodemographic and caregiving data. We studied the relationships between these variables and HRQoL using ANOVA, chi-square and Multiple Linear Regression. We found a mainly female profile for the care of grandchildren and interesting relationships for the physical and mental components of HRQoL. Some relationships were marked by gender: caregiving for pleasure was more often the motive for men while by imposition was more common among women. We discuss the impact of caregiving on health according to the Self-Determination Theory and suggest practical implications derived from the main findings.
Language	English
Publishing date	2024-02-26
Publishing country	England
Document type	Journal Article
ZDB-ID	632677-8
ISSN	1096-4665 ; 0739-9332
ISSN (online)	1096-4665
ISSN	0739-9332
DOI	10.1080/07399332.2024.2316142
Database	MEDical Literature Analysis and Retrieval System OnLINE

In stock of ZB MED Cologne/Königswinter

Zs.B 2847: Show issues

Location:
Je nach Verfügbarkeit (siehe Angabe bei Bestand)
bis Jg. 2021: Bestellungen von Artikeln über das Online-Bestellformular
ab Jg. 2022: Lesesaal (EG)

Order via subito

Details ▾
- See ZB MED holdings
- Order with fees

Article ; Online: Optimization of the Extraction of Chitosan and Fish Gelatin from Fishery Waste and Their Antimicrobial Potential as Active Biopolymers.

Rocha-Pimienta, Javier / Navajas-Preciado, Bruno / Barraso-Gil, Carmen / Martillanes, Sara / Delgado-Adámez, Jonathan

Gels (Basel, Switzerland)

2023 Volume 9, Issue 3

Abstract: Fishery residues are abundant raw materials that also provide numerous metabolites with high added value. Their classic valorization includes energy recovery, composting, animal feed, and direct deposits in landfills or oceans along with the ... ...

Abstract	Fishery residues are abundant raw materials that also provide numerous metabolites with high added value. Their classic valorization includes energy recovery, composting, animal feed, and direct deposits in landfills or oceans along with the environmental impacts that this entails. However, through extraction processes, they can be transformed into new compounds with high added value, offering a more sustainable solution. The aim of this study was to optimize the extraction process of chitosan and fish gelatin from fishery waste and their revalorization as active biopolymers. We successfully optimized the chitosan extraction process, achieving a yield of 20.45% and a deacetylation degree of 69.25%. For the fish gelatin extraction process, yields of 11.82% for the skin and 2.31% for the bone residues were achieved. In addition, it was demonstrated that simple purification steps using activated carbon improve the gelatin's quality significantly. Finally, biopolymers based on fish gelatin and chitosan showed excellent bactericidal capabilities against
Language	English
Publishing date	2023-03-22
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2813982-3
ISSN	2310-2861 ; 2310-2861
ISSN (online)	2310-2861
ISSN	2310-2861
DOI	10.3390/gels9030254
Database	MEDical Literature Analysis and Retrieval System OnLINE

Order via subito

Article ; Online: Audiological evaluation (128-20,000Hz) in women with autoimmune thyroiditis: The role of antibodies vs. l-thyroxine deficiency.

Álvarez Montero, Oscar Luis / Rodríguez Valiente, Antonio / Górriz Gil, Carmen / García Berrocal, José Ramón

Acta otorrinolaringologica espanola

2023 Volume 74, Issue 1, Page(s) 50–58

Abstract: Background and aim: Although sensorineural hearing loss may have different aetiologies, we focused on autoimmune hearing loss since it may be reversible with corticosteroid therapy; this entity is sometimes associated with systemic autoimmune diseases. ... ...

Abstract	Background and aim: Although sensorineural hearing loss may have different aetiologies, we focused on autoimmune hearing loss since it may be reversible with corticosteroid therapy; this entity is sometimes associated with systemic autoimmune diseases. Hashimoto's thyroiditis or chronic autoimmune thyroiditis shows antibodies and may be harmful to hearing thresholds regardless of hypothyroidism effect. To date this effect has not been sufficiently studied and never with extended high frequencies. The aim of this work is to study by age groups whether hearing thresholds in the human auditory range (128-20,000Hz) are affected in Hashimoto's disease. Materials and methods: Two groups of 128 patients affected by Hashimoto's thyroiditis were included. First group: patients with pathological antithyroid antibodies who do not need L-thyroxine treatment. Second group: patients controlled with L-thyroxine substitutive treatment. Audiometric threshold study comparing between the groups of patients and a group of 209 controls was performed. All patients underwent complete otorhinolaryngological examination, antithyroid antibodies, TSH, T Results: All patients were women. Both groups showed worst audiometric thresholds than the control group; both study groups showed worse hearing than controls, this difference was statistically significant in all frequencies. In the 8-20kHz frequency range, this difference was more than 10dB, and in the 9-16kHz and 20kHz range this difference was more than 20dB. When separated by age groups, in younger subjects (20-29 years) these differences were found in all frequencies, except for conversational frequencies (500-4,000Hz); between 30 and 49 years the difference is statistically significant in all frequencies; and from 50 to 69 years differences are found, especially in the conversational frequencies. Conclusions: This first work studying the human auditory range in the chronic autoimmune thyroiditis or Hashimoto's thyroiditis confirms that hearing loss related to the autoimmune disorder predominates at extended-high-frequencies initially. But ends up involving all frequencies in pure-tone conventional audiometry, then it may be detected in routine clinical tests. These results support the role of extended-high-frequencies audiometry to diagnose subclinical hearing loss in patients affected by Hashimoto's thyroiditis.
MeSH term(s)	Humans ; Female ; Young Adult ; Adult ; Male ; Thyroiditis, Autoimmune/complications ; Hashimoto Disease/complications ; Thyroxine/therapeutic use ; Hearing Loss/complications ; Audiometry, Pure-Tone
Chemical Substances	Thyroxine (Q51BO43MG4)
Language	English
Publishing date	2023-01-26
Publishing country	Spain
Document type	Journal Article ; Review
ISSN	2173-5735
ISSN (online)	2173-5735
DOI	10.1016/j.otoeng.2021.11.005
Database	MEDical Literature Analysis and Retrieval System OnLINE

Order via subito

Inter-library loan at ZB MED

Your chosen title can be delivered directly to ZB MED Cologne location if you are registered as a user at ZB MED Cologne.

Article: Variation in avian morphology along a short tropical elevational gradient

Lele, Abhimanyu / Garrod, Holly M. / Ferguson, Euan / Azahara Prieto Gil, Carmen / Ellis, Mike

Biotropica. 2022 July, v. 54, no. 4

2022

Abstract: Patterns across species of intraspecific phenotypic variation with environment can shed light on the underlying drivers of adaptive evolution. Phenotypic variation within a species along tropical elevational gradients is of particular interest because ... ...

Abstract	Patterns across species of intraspecific phenotypic variation with environment can shed light on the underlying drivers of adaptive evolution. Phenotypic variation within a species along tropical elevational gradients is of particular interest because species with narrow elevational ranges may still experience considerably varied environmental conditions. Here, we examine morphological variation in 27 tropical bird species, spanning 11 families and 3 orders, across a 675 m elevational gradient in Western Ecuador. We analyzed a data set of six morphological variables in 3263 individual birds using multivariate analyses of variance (MANOVAs) and canonical correlation analyses (CCAs). We found that morphology varies significantly with elevation in 8 species, and that spatial segregation by age or sex was apparently not responsible for this result. The phenotypic traits that varied with elevation varied strongly by species. To the best of our knowledge, morphological variation over equally short elevational and horizontal distances across a diverse suite of vertebrate species has not previously been demonstrated. Abstract in Spanish is available with online material.
Keywords	data collection ; evolutionary adaptation ; multivariate analysis ; phenotype ; phenotypic variation ; tropical birds ; Ecuador
Language	English
Dates of publication	2022-07
Size	p. 869-880.
Publishing place	John Wiley & Sons, Ltd
Document type	Article
Note	JOURNAL ARTICLE
ZDB-ID	2052061-X
ISSN	1744-7429 ; 0006-3606
ISSN (online)	1744-7429
ISSN	0006-3606
DOI	10.1111/btp.13110
Database	NAL-Catalogue (AGRICOLA)

Order via subito

Article ; Online: Kinase Inhibitors as Underexplored Antiviral Agents.

García-Cárceles, Javier / Caballero, Elena / Gil, Carmen / Martínez, Ana

Journal of medicinal chemistry

2021 Volume 65, Issue 2, Page(s) 935–954

Abstract: Viral infections are a major health problem; therefore, there is an urgent need for novel therapeutic strategies. Antivirals used to target proteins encoded by the viral genome usually enhance drug resistance generated by the virus. A potential solution ... ...

Abstract	Viral infections are a major health problem; therefore, there is an urgent need for novel therapeutic strategies. Antivirals used to target proteins encoded by the viral genome usually enhance drug resistance generated by the virus. A potential solution may be drugs acting at host-based targets since viruses are dependent on numerous cellular proteins and phosphorylation events that are crucial during their life cycle. Repurposing existing kinase inhibitors as antiviral agents would help in the cost and effectiveness of the process, but this strategy usually does not provide much improvement, and specific medicinal chemistry programs are needed in the field. Anyway, extensive use of FDA-approved kinase inhibitors has been quite useful in deciphering the role of host kinases in viral infection. The present perspective aims to review the state of the art of kinase inhibitors that target viral infections in different development stages.
MeSH term(s)	Animals ; Antiviral Agents/therapeutic use ; Drug Repositioning/methods ; Humans ; Protein Kinase Inhibitors/therapeutic use ; Virus Diseases/drug therapy ; Virus Diseases/virology ; Viruses/drug effects
Chemical Substances	Antiviral Agents ; Protein Kinase Inhibitors
Language	English
Publishing date	2021-05-10
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't ; Review
ZDB-ID	218133-2
ISSN	1520-4804 ; 0022-2623
ISSN (online)	1520-4804
ISSN	0022-2623
DOI	10.1021/acs.jmedchem.1c00302
Database	MEDical Literature Analysis and Retrieval System OnLINE

In stock of ZB MED Cologne/Königswinter

Zs.B 151: Show issues			Location: Je nach Verfügbarkeit (siehe Angabe bei Bestand) bis Jg. 2021: Bestellungen von Artikeln über das Online-Bestellformular ab Jg. 2022: Lesesaal (EG)
Zs.MB 1: Show issues

Order via subito

Details ▾
- See ZB MED holdings
- Order with fees

To top

More links

Kategorien

Order via subito

Full text online

More links

Kategorien

In stock of ZB MED Cologne/Königswinter

Order via subito

More links

Kategorien

In stock of ZB MED Cologne/Königswinter

Order via subito

More links

Kategorien

In stock of ZB MED Cologne/Königswinter

Order via subito

More links

Kategorien

Order via subito

Inter-library loan at ZB MED

More links

Kategorien

In stock of ZB MED Cologne/Königswinter

Order via subito

More links

Kategorien

Order via subito

More links

Kategorien

Order via subito

Inter-library loan at ZB MED

More links

Kategorien

Order via subito

More links

Kategorien

In stock of ZB MED Cologne/Königswinter

Order via subito