Neratinib: First Global Approval

Deeks, Emma D.

doi:10.1007/s40265-017-0811-4

Cited by 102 publications

(71 citation statements)

References 42 publications

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“…Furthermore, different quinoline small molecules, acting as protein kinases inhibitors, have been approved by the Food and Drug Administration (FDA) for clinical uses [ 4 , 5 ]. In this contest, bosutinib, a potent inhibitor of Abl, was approved in 2012 for the treatment of Philadelphia chromosome-positive chronic myelogenous leukaemia (CML) [ 6 ]; lenvatinib, an inhibitor of RET and VEGFR has been employed, since 2015, for the treatment of differentiated thyroid cancers [ 7 ]; and neratinib and cabozantinib were authorized for the clinical treatment respectively in 2017 and 2012 [ 8 , 9 ].…”

Section: Introductionmentioning

confidence: 99%

Quinoline-Based Molecules Targeting c-Met, EGF, and VEGF Receptors and the Proteins Involved in Related Carcinogenic Pathways

2020

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The quinoline ring system has long been known as a versatile nucleus in the design and synthesis of biologically active compounds. Currently, more than one hundred quinoline compounds have been approved in therapy as antimicrobial, local anaesthetic, antipsychotic, and anticancer drugs. In drug discovery, indeed, over the last few years, an increase in the publication of papers and patents about quinoline derivatives possessing antiproliferative properties has been observed. This trend can be justified by the versatility and accessibility of the quinoline scaffold, from which new derivatives can be easily designed and synthesized. Within the numerous quinoline small molecules developed as antiproliferative drugs, this review is focused on compounds effective on c-Met, VEGF (vascular endothelial growth factor), and EGF (epidermal growth factor) receptors, pivotal targets for the activation of important carcinogenic pathways (Ras/Raf/MEK and PI3K/AkT/mTOR). These signalling cascades are closely connected and regulate the survival processes in the cell, such as proliferation, apoptosis, differentiation, and angiogenesis. The antiproliferative biological data of remarkable quinoline compounds have been analysed, confirming the pivotal importance of this ring system in the efficacy of several approved drugs. Furthermore, in view of an SAR (structure-activity relationship) study, the most recurrent ligand–protein interactions of the reviewed molecules are summarized.

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Section: Introductionmentioning

confidence: 99%

Quinoline-Based Molecules Targeting c-Met, EGF, and VEGF Receptors and the Proteins Involved in Related Carcinogenic Pathways

2020

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“…Two murine humanized antibodies are currently used in HER2-positive cancer therapy: trastuzumab (Herceptin, Roche-Genentech) binding to subdomain IV of HER2 and pertuzumab (Perjeta, Roche-Genentech), which binds to subdomain II of the receptor [32]. In addition, trastuzumab conjugated with the microtubule assembly inhibitor (trastuzumab-emtazine, Kadcyla, Roche) [33] and two chemical tyrosine kinase domain inhibitors are used: lapatinib (Tykerb or Tyverb, GlaxoSmithKlein) [34] and neratinib (Nerlynx, Pfizer) [35]. These drugs have been approved for HER2-positive breast cancer, gastric cancer, and gastroesophageal cancer [36].…”

Section: Applications Of Darpins In Cancer Diagnosis and Therapymentioning

confidence: 99%

DARPins: Promising Scaffolds for Theranostics

Shilova

Deyev

2019

Acta Naturae

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Monoclonal antibodies are the classical basis for targeted therapy, but the development of alternative binding proteins has made it possible to use non-immunoglobulin proteins as targeting modules. The advantages of DARPins, scaffold proteins based on ankyrin repeats, over antibodies are as follows: small size, stability over a wide range of temperatures and pH values, low aggregation tendency, and ease of production in heterologous expression systems. The differences in the structure of the paratope of DARPin and antibodies broaden the spectrum of target molecules, while the ease of creating hybrid fusion proteins allows one to obtain bispecific and multivalent constructs. In this article, we summarize recent data on the development of therapeutic and imaging compounds based on DARPins.

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“…Cytokines of the IL-1 family are synthesized as precursor molecules containing a pro-peptide domain. It has been established that caspase-1 is the main enzyme necessary for the processing of precursor molecules into mature cytokine forms and their subsequent secretion [35]. IL-37b is also synthesized as a precursor protein and processed into mature form after cell stimulation (for example, with LPS) [36].…”

Section: Il-37 Genementioning

confidence: 99%

The Role of Interleukin-37 in the Pathogenesis of Allergic Diseases

Shilovskiy¹,

Dyneva²,

Курбачева³

et al. 2019

Acta Naturae

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Cytokines of the interleukin-1 (IL-1) family play an important role in the realization of the protective functions of innate immunity and are the key mediators involved in the pathogenesis of a wide range of diseases, including various manifestations of allergy. The IL-1 family includes more than 11 members. However, the functions of many of them remain to be elucidated. Recently, new members of the IL-1 family have been discovered. In 2000, several independent research groups reported the discovery of a new interleukin of this family, which was named IL-37, or IL-1F7 (according to the new nomenclature). IL-37 was assigned to the IL-1 family based on its structural similarity with other members of this family. The study of its biological properties showed that its activity changes in inflammatory diseases, such as rheumatoid arthritis, psoriasis, as well as allergic diseases (allergic rhinitis, bronchial asthma, and atopic dermatitis). However, unlike most members of the IL-1 family, IL-37 acts as a negative regulator of inflammation. Activation of IL-37 suppresses inflammation, resulting in the suppression of inflammatory cytokines and chemokines, which in turn prevents infiltration of pro-inflammatory cells, mainly eosinophils and neutrophils. The exact molecular and cellular mechanisms of the anti-inflammatory effect of IL-37 in the development of allergic diseases (AD) have not been fully studied. This review summarizes and analyzes the accumulated experimental data on the role of IL-37 in the pathogenesis of AD, such as allergic rhinitis, bronchial asthma, and atopic dermatitis.

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Neratinib: First Global Approval

Cited by 102 publications

References 42 publications

Quinoline-Based Molecules Targeting c-Met, EGF, and VEGF Receptors and the Proteins Involved in Related Carcinogenic Pathways

Quinoline-Based Molecules Targeting c-Met, EGF, and VEGF Receptors and the Proteins Involved in Related Carcinogenic Pathways

DARPins: Promising Scaffolds for Theranostics

The Role of Interleukin-37 in the Pathogenesis of Allergic Diseases

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