Erika Iervasi
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View article: Targeting Ubiquitin‐Specific Protease 7 with Novel 5‐Amino‐Pyrazole Inhibitors: Design, Synthesis, and Biological Evaluation
Targeting Ubiquitin‐Specific Protease 7 with Novel 5‐Amino‐Pyrazole Inhibitors: Design, Synthesis, and Biological Evaluation Open
To further extend the structure – activity relationships (SARs) of the previously published ubiquitin‐specific protease 7 (USP‐7) inhibitor STIRUR‐41 , a small library of 5‐aminopyrazoles 1a–d and 2a–d is designed and synthesized. The chem…
View article: Antiprotozoal Activity of Highly Substituted Pyrazole and Pyrimidine Derivatives
Antiprotozoal Activity of Highly Substituted Pyrazole and Pyrimidine Derivatives Open
To further extend the structure‐activity relationships of previously reported antimalarial anilino‐pyrazoles VI , trisubstituted pyrazoles 13–15, and pyrimidines 16 and 17 are designed and synthesized. The novel derivatives are prepared th…
View article: A multi-omics approach reveals impaired lipid metabolism and oxidative stress in a zebrafish model of Alexander disease
A multi-omics approach reveals impaired lipid metabolism and oxidative stress in a zebrafish model of Alexander disease Open
Alexander disease (AxD) is a rare leukodystrophy caused by heterozygous mutations in the GFAP gene. To date, several in vitro and in vivo models have been generated in an attempt to unravel the main mechanisms underlying this complex disea…
View article: Novel tetrasubstituted 5-Arylamino pyrazoles able to interfere with angiogenesis and Ca2+ mobilization
Novel tetrasubstituted 5-Arylamino pyrazoles able to interfere with angiogenesis and Ca2+ mobilization Open
In the last years, 5-pyrazolyl ureas and 5-aminopyrazoles have been investigated for their antiangiogenetic properties and their potential interaction with the ubiquitous Ca2+ binding protein Calreticulin. Based on the structure…
View article: A Proteomics Approach Identifies RREB1 as a Crucial Molecular Target of Imidazo–Pyrazole Treatment in SKMEL-28 Melanoma Cells
A Proteomics Approach Identifies RREB1 as a Crucial Molecular Target of Imidazo–Pyrazole Treatment in SKMEL-28 Melanoma Cells Open
Cutaneous melanoma is the most dangerous and deadly form of human skin malignancy. Despite its rarity, it accounts for a staggering 80% of deaths attributed to cutaneous cancers overall. Moreover, its final stages often exhibit resistance …
View article: Anticancer Effects of the Novel Pyrazolyl-Urea GeGe-3
Anticancer Effects of the Novel Pyrazolyl-Urea GeGe-3 Open
In a screen of over 200 novel pyrazole compounds, ethyl 1-(2-hydroxypentyl)-5-(3-(3-(trifluoromethyl) phenyl)ureido)-1H-pyrazole-4-carboxylate (named GeGe-3) has emerged as a potential anticancer compound. GeGe-3 displays potent anti-angio…
View article: Investigations of Antioxidant and Anti-Cancer Activities of 5-Aminopyrazole Derivatives
Investigations of Antioxidant and Anti-Cancer Activities of 5-Aminopyrazole Derivatives Open
To further extend the structure-activity relationships (SARs) of 5-aminopyrazoles (5APs) and identify novel compounds able to interfere with inflammation, oxidative stress, and tumorigenesis, 5APs 1–4 have been designed and prepared. Some …
View article: Structure–Activity Relationship Studies on Highly Functionalized Pyrazole Hydrazones and Amides as Antiproliferative and Antioxidant Agents
Structure–Activity Relationship Studies on Highly Functionalized Pyrazole Hydrazones and Amides as Antiproliferative and Antioxidant Agents Open
Aminopyrazoles represent interesting structures in medicinal chemistry, and several derivatives showed biological activity in different therapeutic areas. Previously reported 5-aminopyrazolyl acylhydrazones and amides showed relevant antio…
View article: Fraisinib: a calixpyrrole derivative reducing A549 cell-derived NSCLC tumor in vivo acts as a ligand of the glycine-tRNA synthase, a new molecular target in oncology
Fraisinib: a calixpyrrole derivative reducing A549 cell-derived NSCLC tumor in vivo acts as a ligand of the glycine-tRNA synthase, a new molecular target in oncology Open
Background and purpose: Lung cancer is the leading cause of death in both men and women, constituting a major public health problem worldwide. Non-small-cell lung cancer accounts for 85%–90% of all lung cancers. We propose a compound that …
View article: A Multi-Omics Approach Reveals Impaired Lipid Metabolism and Oxidative Stress in a Zebrafish Model of Alexander Disease
A Multi-Omics Approach Reveals Impaired Lipid Metabolism and Oxidative Stress in a Zebrafish Model of Alexander Disease Open
View article: Cyclic diacyl thioureas enhance activity of corrector Lumacaftor on F508del‐CFTR
Cyclic diacyl thioureas enhance activity of corrector Lumacaftor on F508del‐CFTR Open
Cystic fibrosis is a genetic disease caused by mutations in the cystic fibrosis transmembrane conductance regulator (CFTR) protein. In the search of novel series of CFTR modulators, a library of mono and diacyl thioureas were prepared by s…
View article: Novel 5-aminopyrazoles endowed with anti-angiogenetic properties: Design, synthesis and biological evaluation
Novel 5-aminopyrazoles endowed with anti-angiogenetic properties: Design, synthesis and biological evaluation Open
View article: Insights into the Pharmacological Activity of the Imidazo−Pyrazole Scaffold
Insights into the Pharmacological Activity of the Imidazo−Pyrazole Scaffold Open
In previous studies, we synthesized different imidazo−pyrazoles 1 and 2 with interesting anticancer, anti‐angiogenic and anti‐inflammatory activities. To further extend the structure‐activity relationships of imidazo−pyrazole scaffold and …
View article: Circulating anti-hypothalamus antibodies in celiac patients: tissue transglutaminase friend or foe?
Circulating anti-hypothalamus antibodies in celiac patients: tissue transglutaminase friend or foe? Open
View article: Lipid Metabolism Reprogramming and Trastuzumab Resistance in Breast Cancer Cell Lines Overexpressing the ERBB2 Membrane Receptor
Lipid Metabolism Reprogramming and Trastuzumab Resistance in Breast Cancer Cell Lines Overexpressing the ERBB2 Membrane Receptor Open
Trastuzumab (Tz), an antibody targeting ERBB2, has significantly improved the prognosis for breast cancer (BCa) patients with overexpression of the ERBB2 receptor. However, Tz resistance poses a challenge to patient outcomes. Numerous mech…
View article: Lipid Metabolism Reprogramming Is Associated with Trastuzumab Resistance in ERBB2+ Breast Cancer Cell Lines
Lipid Metabolism Reprogramming Is Associated with Trastuzumab Resistance in ERBB2+ Breast Cancer Cell Lines Open
The antibody Trastuzumab (Tz) targeting ERBB2 has improved the prognosis of patients with breast cancer (BCa) that overexpress this receptor. Resistance to Tz negatively impacts prognosis. Several mechanisms have been reported to cause Tz …
View article: Lipid Metabolism Reprogramming is Associated with Trastuzumab Resistance in ERBB2 Breast Cancer Cell Lines
Lipid Metabolism Reprogramming is Associated with Trastuzumab Resistance in ERBB2 Breast Cancer Cell Lines Open
View article: Regioselective Synthesis, Structural Characterization, and Antiproliferative Activity of Novel Tetra-Substituted Phenylaminopyrazole Derivatives
Regioselective Synthesis, Structural Characterization, and Antiproliferative Activity of Novel Tetra-Substituted Phenylaminopyrazole Derivatives Open
A small library of highly functionalized phenylaminopyrazoles, bearing different substituents at position 1, 3, and 4 of the pyrazole ring, was prepared by the one-pot condensation of active methylene reagents, phenylisothiocyanate, and su…
View article: Two calix[4]pyrroles as potential therapeutics for castration-resistant prostate cancer
Two calix[4]pyrroles as potential therapeutics for castration-resistant prostate cancer Open
View article: Anti-hypothalamus autoantibodies in anorexia nervosa: a possible new mechanism in neuro-physiological derangement?
Anti-hypothalamus autoantibodies in anorexia nervosa: a possible new mechanism in neuro-physiological derangement? Open
View article: One‐Pot Synthesis and Antiproliferative Activity of Highly Functionalized Pyrazole Derivatives
One‐Pot Synthesis and Antiproliferative Activity of Highly Functionalized Pyrazole Derivatives Open
A series of highly functionalized pyrazole derivatives has been prepared by a one‐pot, versatile and regioselective procedure. Pyrazoles 1 – 29 were tested in cell‐based assay to assess their antiproliferative activity against a panel of t…
View article: JNK3 as Therapeutic Target and Biomarker in Neurodegenerative and Neurodevelopmental Brain Diseases
JNK3 as Therapeutic Target and Biomarker in Neurodegenerative and Neurodevelopmental Brain Diseases Open
The c-Jun N-terminal kinase 3 (JNK3) is the JNK isoform mainly expressed in the brain. It is the most responsive to many stress stimuli in the central nervous system from ischemia to Aβ oligomers toxicity. JNK3 activity is spatial and temp…
View article: FRI0480 CHANGES IN CIRCULATING SCTLA-4 FOLLOWING ZOLEDRONIC ACID INFUSION
FRI0480 CHANGES IN CIRCULATING SCTLA-4 FOLLOWING ZOLEDRONIC ACID INFUSION Open
View article: Hypothalamic expression of PD-L1: does it mediate hypothalamitis?
Hypothalamic expression of PD-L1: does it mediate hypothalamitis? Open