Francesca Carlomagno
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View article: Discovery of a Proteolysis Targeting Chimera for TRKA and RET-derived oncoproteins
Discovery of a Proteolysis Targeting Chimera for TRKA and RET-derived oncoproteins Open
We designed Proteolysis Targeting Chimeras (PROTACs) to target Tropomyosin Receptor Kinase A (TRKA) and Rearranged during Transfection (RET) oncogenic proteins. We analyzed a series of 22 PROTACs, based on the RET and TRKA small molecule i…
View article: Targeting the Liver Serine Protease <scp>TMPRSS6</scp> Ameliorates Steatosis and Attenuates Fibrosis in Experimental <scp>MASLD</scp>
Targeting the Liver Serine Protease <span>TMPRSS6</span> Ameliorates Steatosis and Attenuates Fibrosis in Experimental <span>MASLD</span> Open
Background and Aims Metabolic dysfunction–associated steatotic liver disease (MASLD) is the most common cause of liver disease and a leading contributor to liver‐related morbidity and mortality. Currently, no pharmacological approach has d…
View article: Ultrasound-induced mechanical damage of cancer cell cytoskeleton causes disruption of nuclear envelope and activation of cGAS-STING
Ultrasound-induced mechanical damage of cancer cell cytoskeleton causes disruption of nuclear envelope and activation of cGAS-STING Open
Neoplastic transformation is accompanied by critical changes in cell mechanical properties, including reduced cell elasticity. By leveraging such mechanical flaw, exposure to low intensity therapeutic ultrasounds (LITUS) has been proposed …
View article: D898_E901 <i>RET</i> Deletion Is Oncogenic, Responds to Selpercatinib, and Treatment Resistance Can Arise Via RET-Independent Mechanisms
D898_E901 <i>RET</i> Deletion Is Oncogenic, Responds to Selpercatinib, and Treatment Resistance Can Arise Via RET-Independent Mechanisms Open
PURPOSE We analyzed the oncogenic potential of RET Δ898-901 mutant and its response to selpercatinib, vandetanib, and cabozantinib in vitro and in a clinical case. MATERIALS AND METHODS A 35-year-old man with a medullary thyroid cancer (MT…
View article: Supplementary Methods from Identification of Polo-like Kinase 1 as a Potential Therapeutic Target in Anaplastic Thyroid Carcinoma
Supplementary Methods from Identification of Polo-like Kinase 1 as a Potential Therapeutic Target in Anaplastic Thyroid Carcinoma Open
Supplementary Methods from Identification of Polo-like Kinase 1 as a Potential Therapeutic Target in Anaplastic Thyroid Carcinoma
View article: Data from Identification of Polo-like Kinase 1 as a Potential Therapeutic Target in Anaplastic Thyroid Carcinoma
Data from Identification of Polo-like Kinase 1 as a Potential Therapeutic Target in Anaplastic Thyroid Carcinoma Open
Anaplastic thyroid carcinoma (ATC) is one of the most aggressive and chemoresistant cancers. The serine/threonine kinase Polo-like kinase 1 (PLK1), a key regulator of multiple steps during mitotic progression, is highly expressed in ATC. H…
View article: Supplementary Figure 1 from Identification of Polo-like Kinase 1 as a Potential Therapeutic Target in Anaplastic Thyroid Carcinoma
Supplementary Figure 1 from Identification of Polo-like Kinase 1 as a Potential Therapeutic Target in Anaplastic Thyroid Carcinoma Open
Supplementary Figure 1 from Identification of Polo-like Kinase 1 as a Potential Therapeutic Target in Anaplastic Thyroid Carcinoma
View article: Supplementary Figure 1 from Identification of Polo-like Kinase 1 as a Potential Therapeutic Target in Anaplastic Thyroid Carcinoma
Supplementary Figure 1 from Identification of Polo-like Kinase 1 as a Potential Therapeutic Target in Anaplastic Thyroid Carcinoma Open
Supplementary Figure 1 from Identification of Polo-like Kinase 1 as a Potential Therapeutic Target in Anaplastic Thyroid Carcinoma
View article: Supplementary Methods from Identification of Polo-like Kinase 1 as a Potential Therapeutic Target in Anaplastic Thyroid Carcinoma
Supplementary Methods from Identification of Polo-like Kinase 1 as a Potential Therapeutic Target in Anaplastic Thyroid Carcinoma Open
Supplementary Methods from Identification of Polo-like Kinase 1 as a Potential Therapeutic Target in Anaplastic Thyroid Carcinoma
View article: Data from Identification of Polo-like Kinase 1 as a Potential Therapeutic Target in Anaplastic Thyroid Carcinoma
Data from Identification of Polo-like Kinase 1 as a Potential Therapeutic Target in Anaplastic Thyroid Carcinoma Open
Anaplastic thyroid carcinoma (ATC) is one of the most aggressive and chemoresistant cancers. The serine/threonine kinase Polo-like kinase 1 (PLK1), a key regulator of multiple steps during mitotic progression, is highly expressed in ATC. H…
View article: NCOA4 links iron bioavailability to DNA metabolism
NCOA4 links iron bioavailability to DNA metabolism Open
Iron is essential for deoxyribonucleotides production and for enzymes containing an Fe-S cluster involved in DNA replication and repair. How iron bioavailability and DNA metabolism are coordinated remains poorly understood. NCOA4 protein m…
View article: Prioritization of driver genes in cancer-associated copy number alterations identifies B4GALT5 as a glycooncogene
Prioritization of driver genes in cancer-associated copy number alterations identifies B4GALT5 as a glycooncogene Open
Cancer is a disease resulting from aberrant communication between cells of a multicellular organism. The glycan coat that surrounds the cells is an important player in cellular communication. While altered cell surface glycans are known bi…
View article: Discovery of N-Trisubstituted Pyrimidine Derivatives as Type I RET and RET Gatekeeper Mutant Inhibitors with a Novel Kinase Binding Pose
Discovery of N-Trisubstituted Pyrimidine Derivatives as Type I RET and RET Gatekeeper Mutant Inhibitors with a Novel Kinase Binding Pose Open
Mutations of the rearranged during transfection (RET) kinase are frequently reported in cancer, which make it as an attractive therapeutic target. Herein, we discovered a series of N-trisubstituted pyrimidine derivatives as potent inhibito…
View article: Targeted activity of the small molecule kinase inhibitor Pz-1 towards RET and TRK kinases
Targeted activity of the small molecule kinase inhibitor Pz-1 towards RET and TRK kinases Open
View article: The pyruvate kinase activator mitapivat reduces hemolysis and improves anemia in a β-thalassemia mouse model
The pyruvate kinase activator mitapivat reduces hemolysis and improves anemia in a β-thalassemia mouse model Open
Anemia in β-thalassemia is related to ineffective erythropoiesis and reduced red cell survival. Excess free heme and accumulation of unpaired α-globin chains impose substantial oxidative stress on β-thalassemic erythroblasts and erythrocyt…
View article: Discovery of pyrazolo-thieno[3,2-d]pyrimidinylamino-phenyl acetamides as type-II pan-tropomyosin receptor kinase (TRK) inhibitors: Design, synthesis, and biological evaluation
Discovery of pyrazolo-thieno[3,2-d]pyrimidinylamino-phenyl acetamides as type-II pan-tropomyosin receptor kinase (TRK) inhibitors: Design, synthesis, and biological evaluation Open
View article: Bioisosteric Discovery of NPA101.3, a Second-Generation RET/VEGFR2 Inhibitor Optimized for Single-Agent Polypharmacology
Bioisosteric Discovery of NPA101.3, a Second-Generation RET/VEGFR2 Inhibitor Optimized for Single-Agent Polypharmacology Open
RET receptor tyrosine kinase is a driver oncogene in human cancer. We recently identified the clinical drug candidate Pz-1, which targets RET and VEGFR2. A key in vivo metabolite of Pz-1 is its less active demethylated pyrazole anal…
View article: RET Gene Fusions in Malignancies of the Thyroid and Other Tissues
RET Gene Fusions in Malignancies of the Thyroid and Other Tissues Open
Following the identification of the BCR-ABL1 (Breakpoint Cluster Region-ABelson murine Leukemia) fusion in chronic myelogenous leukemia, gene fusions generating chimeric oncoproteins have been recognized as common genomic structural variat…
View article: NCOA4-mediated ferritinophagy in macrophages is crucial to sustain erythropoiesis in mice
NCOA4-mediated ferritinophagy in macrophages is crucial to sustain erythropoiesis in mice Open
The Nuclear Receptor Coactivator 4 (NCOA4) promotes ferritin degradation and Ncoa4-ko mice in C57BL/6 background show microcytosis and mild anemia, aggravated by iron deficiency. To understand tissue specific contribution of NCOA4-mediated…
View article: Tamoxifen erythroid toxicity revealed by studying the role of nuclear receptor co-activator 4 in erythropoiesis
Tamoxifen erythroid toxicity revealed by studying the role of nuclear receptor co-activator 4 in erythropoiesis Open
View article: Iron and Ferritin Modulate MHC Class I Expression and NK Cell Recognition
Iron and Ferritin Modulate MHC Class I Expression and NK Cell Recognition Open
The ability of pathogens to sequester iron from their host cells and proteins affects their virulence. Moreover, iron is required for various innate host defense mechanisms as well as for acquired immune responses. Therefore, intracellular…
View article: Association between DNA methylation profile and malignancy in follicular-patterned thyroid neoplasms
Association between DNA methylation profile and malignancy in follicular-patterned thyroid neoplasms Open
Molecular differentiation between benign (follicular thyroid adenoma (FTA)) and malignant (follicular thyroid carcinoma (FTC)) thyroid neoplasms is challenging. Here, we explored the genome-wide DNA methylation profile of FTA (n.10) and FT…
View article: Insights into Current Tropomyosin Receptor Kinase (TRK) Inhibitors: Development and Clinical Application
Insights into Current Tropomyosin Receptor Kinase (TRK) Inhibitors: Development and Clinical Application Open
The use of kinase-directed precision medicine has been heavily pursued since the discovery and development of imatinib. Annually, it is estimated that around ∼20 000 new cases of tropomyosin receptor kinase (TRK) cancers are diagnosed, wit…
View article: NCOA4 Deficiency Impairs Systemic Iron Homeostasis
NCOA4 Deficiency Impairs Systemic Iron Homeostasis Open
View article: Inside Back Cover: Fragment‐Based Discovery of a Dual pan‐RET/VEGFR2 Kinase Inhibitor Optimized for Single‐Agent Polypharmacology (Angew. Chem. Int. Ed. 30/2015)
Inside Back Cover: Fragment‐Based Discovery of a Dual pan‐RET/VEGFR2 Kinase Inhibitor Optimized for Single‐Agent Polypharmacology (Angew. Chem. Int. Ed. 30/2015) Open
The inhibitory powers of a next-generation inhibitor were carefully balanced so that it is equally potent on the RET kinase and VEGFR2. In their Communication on page 8717 ff., H.-y. Li, M. Santoro, et al. report the optimization of a dual…
View article: Innenrücktitelbild: Fragment‐Based Discovery of a Dual pan‐RET/VEGFR2 Kinase Inhibitor Optimized for Single‐Agent Polypharmacology (Angew. Chem. 30/2015)
Innenrücktitelbild: Fragment‐Based Discovery of a Dual pan‐RET/VEGFR2 Kinase Inhibitor Optimized for Single‐Agent Polypharmacology (Angew. Chem. 30/2015) Open
Die hemmendenen Wirkung eines neuen Inhibitors wurden sorgsam ausgewogen, damit er gegenüber der RET-Kinase und VEGFR2 gleichermaßen aktiv ist. In der Zuschrift auf S. 8841 ff. beschreiben H.-y. Li, M. Santoro et al. die Optimierung des du…
View article: Fragment‐Based Discovery of a Dual pan‐RET/VEGFR2 Kinase Inhibitor Optimized for Single‐Agent Polypharmacology
Fragment‐Based Discovery of a Dual pan‐RET/VEGFR2 Kinase Inhibitor Optimized for Single‐Agent Polypharmacology Open
Oncogenic conversion of the RET (rearranged during transfection) tyrosine kinase is associated with several cancers. A fragment‐based chemical screen led to the identification of a novel RET inhibitor, Pz‐1. Modeling and kinetic analysis i…
View article: Identification of Novel Small Molecule Inhibitors of Oncogenic RET Kinase
Identification of Novel Small Molecule Inhibitors of Oncogenic RET Kinase Open
Oncogenic mutation of the RET receptor tyrosine kinase is observed in several human malignancies. Here, we describe three novel type II RET tyrosine kinase inhibitors (TKI), ALW-II-41-27, XMD15-44 and HG-6-63-01, that inhibit the cellular …