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The metabolomics approach, defined as the study of all endogenously-produced low-molecular-weight compounds, appeared as a promising strategy to define new cancer biomarkers. Information obtained from metabolomic data can help to highlight disrupted cellular pathways and, consequently, contribute to the development of new-targeted therapies and the optimization of therapeutics. Therefore, metabolomic research may be more clinically translatable than other omics approaches, since metabolites are closely related to the phenotype and the metabolome is sensitive to many factors. Metabolomics seems promising to identify key metabolic pathways characterizing features of pathological and physiological states. Thus, knowing that tumor metabolism markedly differs from the metabolism of normal cells, the use of metabolomics is ideally suited for biomarker research. Some works have already focused on the application of metabolomic approaches to different cancers, namely lung, breast and liver, using urine, exhaled breath and blood. In this Special Issue we contribute to a more complete understanding of cancer disease using metabolomics approaches.

cell transporters --- pharmacodynamics --- cell growth --- in vitro study --- metabolomic signatures --- endometabolome --- lung cancer --- metabolomics --- chemometric methods --- bladder cancer --- mTOR --- metabolite profiling --- metabolic pathways --- hepatocellular carcinoma --- glutamate --- senescence MCF7 --- breath analysis --- bio actives --- biomarker --- gas chromatography–mass spectrometry (GC–MS) --- GC-MS --- lung --- omics --- nutraceuticals --- glutaminase --- metabolism --- acylcarnitines --- Erwinaze --- Kidrolase --- glutathione --- targeted metabolomics --- apoptosis --- SLC1A5 --- essential amino acids --- cancer progression --- ASCT2 --- HR MAS --- alanine --- analytical platforms --- volatile organic compound --- glutaminolysis --- isotope tracing analysis --- asparaginase --- vitamin E --- breast cancer --- prognosis --- early diagnosis --- tocotrienols --- NMR --- prostate cancer --- in vitro --- cancer --- MDA-MB-231

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The Special Issue "Anticancer Drugs 2021" of Pharmaceuticals is focused on recent significant advances in the design, synthesis, molecular mechanism of action and therapeutic applications of anticancer drugs. This collection of preclinical research papers and reviews includes designed chemotherapeutic agents, targeted therapies and biological agents. The rationalization for the biological activity of these drugs is presented, which helps to guide the design of more effective agents. Structure–activity relationships, together with the biological context in which targets are selected for oncology drug development, are also considered.

Research & information: general --- Chemistry --- thymidylate synthase --- cytotoxicity --- 1,2,3-triazole --- 1,3,4-oxadiazole --- 5-fluoruracil --- pemetrexed --- docking --- 3,4'-bis-guanidino --- 3-amino-4'-guanidino --- diphenyl ether --- phenyl pyridyl ether --- intramolecular hydrogen bond --- cancer cell viability --- HL-60 --- BRAF --- apoptosis --- thieno[2,3-d][1,2,3]triazine --- acetamide --- H1299 --- HER2 --- EGFR --- Bcl-2 inhibitors --- Indole-based analogues --- benzimidazole --- MTT cytotoxic assay --- cell cycle analysis --- DNA fragmentation --- ELISA --- solid/lipid nanoparticles --- phenstatin --- letrozole --- tubulin polymerisation inhibitor --- aromatase inhibitor --- breast cancer --- hybrid molecule --- dual-targeting molecule --- designed multiple ligand --- NaMSA --- cyclophosphamide --- histopathology --- testis --- urinary bladder --- anticancer agents --- enantioselective synthesis --- gastric adenocarcinoma --- tryptophanol --- concentration-guided dosing --- model informed dosing --- physiologically based pharmacokinetics --- sorafenib --- tyrosil-DNA-phosphodiesterase 1 --- adamantane --- resin acid --- TDP1 --- cytotoxic agents --- apoptosis induction --- HT-29 cells --- MDA-MB-231 cells --- mechanism prediction --- STAT inhibitors --- miR-21 --- hydrazide derivatives --- nitrogen scaffolds --- mitoxantrone --- cardiotoxicity --- inflammation --- oxidative stress --- age --- cumulative dose --- Trk --- NTRK --- tissue-agnostic --- larotrectinib --- entrectinib --- Trk fusion --- protein kinase inhibitors --- USFDA --- cancer --- patent review --- generic product --- doxazosin --- MD simulations --- combretastatin A-4 --- cytotoxic activity --- hybrid compounds --- indazole --- mucin --- MUC1 --- MUC16 --- immunotherapy --- cancer vaccine --- CAR (chimeric antigen receptor) --- ADC (antibody-drug conjugate) --- thiourea --- interleukin-6 --- trypan blue assay --- chalcones --- exportin-1 --- covalent binding --- CovDock --- anticancer activity --- xanthone --- in vitro --- in vivo --- isolation --- synthesis --- heterocyclic compound --- benzenesulfonamides --- imidazoles --- alkylated --- colony formation --- tumor spheroids --- HDAC inhibitors --- chalcone --- dual inhibitors --- carvedilol --- kidney --- toxicity --- 7-deaza-4'-thioadenosine derivatives --- multi-kinase inhibitor --- anticancer --- nucleoside --- Imiquimod --- drug efflux --- multidrug resistance --- Toll-Like Receptor --- thymidylate synthase --- cytotoxicity --- 1,2,3-triazole --- 1,3,4-oxadiazole --- 5-fluoruracil --- pemetrexed --- docking --- 3,4'-bis-guanidino --- 3-amino-4'-guanidino --- diphenyl ether --- phenyl pyridyl ether --- intramolecular hydrogen bond --- cancer cell viability --- HL-60 --- BRAF --- apoptosis --- thieno[2,3-d][1,2,3]triazine --- acetamide --- H1299 --- HER2 --- EGFR --- Bcl-2 inhibitors --- Indole-based analogues --- benzimidazole --- MTT cytotoxic assay --- cell cycle analysis --- DNA fragmentation --- ELISA --- solid/lipid nanoparticles --- phenstatin --- letrozole --- tubulin polymerisation inhibitor --- aromatase inhibitor --- breast cancer --- hybrid molecule --- dual-targeting molecule --- designed multiple ligand --- NaMSA --- cyclophosphamide --- histopathology --- testis --- urinary bladder --- anticancer agents --- enantioselective synthesis --- gastric adenocarcinoma --- tryptophanol --- concentration-guided dosing --- model informed dosing --- physiologically based pharmacokinetics --- sorafenib --- tyrosil-DNA-phosphodiesterase 1 --- adamantane --- resin acid --- TDP1 --- cytotoxic agents --- apoptosis induction --- HT-29 cells --- MDA-MB-231 cells --- mechanism prediction --- STAT inhibitors --- miR-21 --- hydrazide derivatives --- nitrogen scaffolds --- mitoxantrone --- cardiotoxicity --- inflammation --- oxidative stress --- age --- cumulative dose --- Trk --- NTRK --- tissue-agnostic --- larotrectinib --- entrectinib --- Trk fusion --- protein kinase inhibitors --- USFDA --- cancer --- patent review --- generic product --- doxazosin --- MD simulations --- combretastatin A-4 --- cytotoxic activity --- hybrid compounds --- indazole --- mucin --- MUC1 --- MUC16 --- immunotherapy --- cancer vaccine --- CAR (chimeric antigen receptor) --- ADC (antibody-drug conjugate) --- thiourea --- interleukin-6 --- trypan blue assay --- chalcones --- exportin-1 --- covalent binding --- CovDock --- anticancer activity --- xanthone --- in vitro --- in vivo --- isolation --- synthesis --- heterocyclic compound --- benzenesulfonamides --- imidazoles --- alkylated --- colony formation --- tumor spheroids --- HDAC inhibitors --- chalcone --- dual inhibitors --- carvedilol --- kidney --- toxicity --- 7-deaza-4'-thioadenosine derivatives --- multi-kinase inhibitor --- anticancer --- nucleoside --- Imiquimod --- drug efflux --- multidrug resistance --- Toll-Like Receptor

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Cancer is one of the major causes of death worldwide. It is a multifactorial heterogeneous disease characterized by the transformation of normal cells into malignant cells, which acquire an uncontrolled growth, immortality, invasiveness, and ability to form distant metastasis. Natural bioactive molecules may interfere with these processes and inhibit the carcinogenesis process. In this book, new molecules and extracts, mainly derived from plants, have been described as being able to alter tumor cell behavior and target several abnormal molecular pathways in cancer cells. Among different cancer cells, the more studied include those derived from glioblastoma, osteosarcoma, lung, breast and gastric cancer. These natural products could be an attractive source for the development of new preventative and therapeutic agents against cancer. They may be more selective and have weaker adverse effects compared to conventional chemotherapy drugs that are actually used for cancer treatment. Clinical trials are necessary to demonstrate whether the in vitro and in vivo animal data are reproduced in humans before the application of natural products in cancer prevention and treatment.

cytotoxic activity --- NCI-60 cancer cell line --- pristimerin --- Salacia crassifolia --- Celastraceae --- Brazilian Cerrado biome --- Salacia elliptica --- Cheiloclinium cognatum --- Plenckia populnea --- Aspergillus fumigatus --- Cordyceps sinensis --- isochromanes --- chiral resolution --- ECD calculation --- cytotoxicity --- coronarin D --- JNK --- osteosarcoma --- Zeylenone --- gastric cancer --- invasion --- migration --- apoptosis --- anti-cancer agents --- anthraquinones --- glycosyltransferase --- Dendrobium officinale --- structure elucidation --- anti-tumor activity --- plantation mode --- AR --- Ganoderma tsugae --- lipogenesis --- prostate cancer --- SREBP-1 --- ursolic acid --- betulinic acid --- triterpenoids --- necrotic --- quercetin --- quercetagetin --- patuletin --- lichen --- secondary metabolites --- tumidulin --- stemness potential --- colorectal cancer cells --- oncogene --- transcriptional regulation --- neferine --- FAK/S6K1 --- autophagy --- human neuroblastoma cells --- natural yellow Monascus pigments --- water-soluble --- antioxidation --- MCF-7 cells --- phloretin --- cell proliferation --- inflammation --- glucose uptake --- Catalpa speciosa --- Taxus cuspidata --- Magnolia acuminata --- phenols --- antioxidants --- anticancer --- Colocasia esculenta --- food bioactive --- tarin --- stable nanocapsules --- entrapment efficiency --- no-toxicity --- preclinical tests --- antitumoral activity --- chemotherapeutic adjuvant --- grape leaves --- ASE --- TP --- Antioxidant activities --- Antiproliferative --- pro-apoptotic effects --- Gene expression --- Nutraceuticals --- Cucurbitacin B --- gefitinib-resistant NSCLC --- EGFR --- lysosomal degradation --- CIP2A --- zerumbone --- cancer --- NF-κB --- IL-6/JAK2/STAT3 --- Akt --- FOXO1 --- multiple myeloma --- quality control --- naringenin --- flavonoids --- traditional preparation --- cancer stem cells --- phytochemicals --- plant-derived foods --- fruit --- vegetable --- cell signaling --- Artemisia absinthium --- endoplasmic reticulum stress --- mitochondrial-dependent pathway --- melanoma --- bee venom --- melittin --- temozolomide --- AKT --- MAPK --- antrodin C --- mTOR --- metabolic stability --- capsazepine --- inflammatory diseases --- ROS --- TRPV1 --- PI3K/AKT/mTOR --- CLE-10 --- LC3 --- MDA-MB-231 --- lactoferrin hydrolysate --- copper --- manganese --- gastric cancer cells --- anti-cancer activity --- molecular mechanism --- natural product alkaloids --- cephalotaxine --- protein synthesis inhibition --- antiproliferation agents --- folk medicine --- DLD-1 cells --- doxorubicin --- chemotherapy --- drug resistance --- CrataBL --- glioblastoma --- mesenchymal stem cells --- microenvironment --- plant lectin --- protease inhibitor --- cryptolepine --- neocryptolepine --- isocryptolepine --- antiproliferative activity --- structure activity relationships --- Licochalcone A --- ATM-Chk2 --- 13-ethylberberine --- mitochondrial ROS --- RT-R breast cancer cells --- diallyl disulfide --- PI3K/Akt/mTOR pathway --- Pulsatilla saponin D --- SB365 --- glioblastoma multiforme --- autophagic flux inhibition --- lysosomal membrane permeabilization --- mitochondrial membrane potential --- CLEFMA --- p38 --- proanthocyanins --- TNF-α --- lung adenocarcinoma --- natural compounds --- cervical cancer --- cell cycle arrest --- dicentrine --- metastasis --- glioma --- semi-synthetic derivative --- ingenol --- Euphorbia tirucalli --- protein kinase C --- seaweed --- porphyran --- carrageenan --- anti-cancer --- natural products --- n/a

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Cancer is one of the major causes of death worldwide. It is a multifactorial heterogeneous disease characterized by the transformation of normal cells into malignant cells, which acquire an uncontrolled growth, immortality, invasiveness, and ability to form distant metastasis. Natural bioactive molecules may interfere with these processes and inhibit the carcinogenesis process. In this book, new molecules and extracts, mainly derived from plants, have been described as being able to alter tumor cell behavior and target several abnormal molecular pathways in cancer cells. Among different cancer cells, the more studied include those derived from glioblastoma, osteosarcoma, lung, breast and gastric cancer. These natural products could be an attractive source for the development of new preventative and therapeutic agents against cancer. They may be more selective and have weaker adverse effects compared to conventional chemotherapy drugs that are actually used for cancer treatment. Clinical trials are necessary to demonstrate whether the in vitro and in vivo animal data are reproduced in humans before the application of natural products in cancer prevention and treatment.

cytotoxic activity --- NCI-60 cancer cell line --- pristimerin --- Salacia crassifolia --- Celastraceae --- Brazilian Cerrado biome --- Salacia elliptica --- Cheiloclinium cognatum --- Plenckia populnea --- Aspergillus fumigatus --- Cordyceps sinensis --- isochromanes --- chiral resolution --- ECD calculation --- cytotoxicity --- coronarin D --- JNK --- osteosarcoma --- Zeylenone --- gastric cancer --- invasion --- migration --- apoptosis --- anti-cancer agents --- anthraquinones --- glycosyltransferase --- Dendrobium officinale --- structure elucidation --- anti-tumor activity --- plantation mode --- AR --- Ganoderma tsugae --- lipogenesis --- prostate cancer --- SREBP-1 --- ursolic acid --- betulinic acid --- triterpenoids --- necrotic --- quercetin --- quercetagetin --- patuletin --- lichen --- secondary metabolites --- tumidulin --- stemness potential --- colorectal cancer cells --- oncogene --- transcriptional regulation --- neferine --- FAK/S6K1 --- autophagy --- human neuroblastoma cells --- natural yellow Monascus pigments --- water-soluble --- antioxidation --- MCF-7 cells --- phloretin --- cell proliferation --- inflammation --- glucose uptake --- Catalpa speciosa --- Taxus cuspidata --- Magnolia acuminata --- phenols --- antioxidants --- anticancer --- Colocasia esculenta --- food bioactive --- tarin --- stable nanocapsules --- entrapment efficiency --- no-toxicity --- preclinical tests --- antitumoral activity --- chemotherapeutic adjuvant --- grape leaves --- ASE --- TP --- Antioxidant activities --- Antiproliferative --- pro-apoptotic effects --- Gene expression --- Nutraceuticals --- Cucurbitacin B --- gefitinib-resistant NSCLC --- EGFR --- lysosomal degradation --- CIP2A --- zerumbone --- cancer --- NF-κB --- IL-6/JAK2/STAT3 --- Akt --- FOXO1 --- multiple myeloma --- quality control --- naringenin --- flavonoids --- traditional preparation --- cancer stem cells --- phytochemicals --- plant-derived foods --- fruit --- vegetable --- cell signaling --- Artemisia absinthium --- endoplasmic reticulum stress --- mitochondrial-dependent pathway --- melanoma --- bee venom --- melittin --- temozolomide --- AKT --- MAPK --- antrodin C --- mTOR --- metabolic stability --- capsazepine --- inflammatory diseases --- ROS --- TRPV1 --- PI3K/AKT/mTOR --- CLE-10 --- LC3 --- MDA-MB-231 --- lactoferrin hydrolysate --- copper --- manganese --- gastric cancer cells --- anti-cancer activity --- molecular mechanism --- natural product alkaloids --- cephalotaxine --- protein synthesis inhibition --- antiproliferation agents --- folk medicine --- DLD-1 cells --- doxorubicin --- chemotherapy --- drug resistance --- CrataBL --- glioblastoma --- mesenchymal stem cells --- microenvironment --- plant lectin --- protease inhibitor --- cryptolepine --- neocryptolepine --- isocryptolepine --- antiproliferative activity --- structure activity relationships --- Licochalcone A --- ATM-Chk2 --- 13-ethylberberine --- mitochondrial ROS --- RT-R breast cancer cells --- diallyl disulfide --- PI3K/Akt/mTOR pathway --- Pulsatilla saponin D --- SB365 --- glioblastoma multiforme --- autophagic flux inhibition --- lysosomal membrane permeabilization --- mitochondrial membrane potential --- CLEFMA --- p38 --- proanthocyanins --- TNF-α --- lung adenocarcinoma --- natural compounds --- cervical cancer --- cell cycle arrest --- dicentrine --- metastasis --- glioma --- semi-synthetic derivative --- ingenol --- Euphorbia tirucalli --- protein kinase C --- seaweed --- porphyran --- carrageenan --- anti-cancer --- natural products --- n/a

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This special issue brings together cutting edge research and insightful commentary on the currentl state of the Cancer Nanomedicine field.

Technology: general issues --- antibody drug conjugate (ADC) --- PD-L1 --- tumor spheroid disruption --- immune modulation --- doxorubicin --- graphene oxide --- adsorption --- cathepsin D --- cathepsin L --- anti-metastatic enzyme cancer therapy --- nanoparticles --- targeted delivery system --- siRNA --- osteopontin --- mammary carcinoma --- mesenchymal stem cells (MSCs) --- TAT peptide --- PLGA --- paclitaxel --- nano-engineered MSCs --- orthotopic lung tumor model --- intracranial glioma --- immunotherapy --- CPMV --- viral nanoparticles --- in situ vaccine --- albumin nanoparticles --- microbubble --- ultrasound --- theranostics --- hepatocellular carcinoma --- VX2 tumor --- intra-arterial chemotherapy --- lung cancer --- nanomedicine --- clinical status --- cancer therapy --- breast cancer --- cell signaling --- active targeting --- passive targeting --- EPR effect --- oncogenes --- nanoparticle --- drug delivery --- ligand --- tumor targeting --- biodistribution --- Mesoporous silica nanoparticle --- drug delivery system --- target treatment --- lanthanide metal --- hyaluronic acid --- hyaluronidase --- drug combination --- everolimus --- dual-targeting --- magnetic nanoparticles --- monoclonal antibodies --- nanostructured lipid carrier --- platelet membrane --- biomimicry --- plasmonic photothermal therapy --- gold nanorods --- surgery --- bleeding --- dogs --- cats --- stimuli-responsive --- DOX --- SN38 --- CSCs --- single-walled carbon nanotubes --- chirality separation --- NASH --- drug-gene delivery --- near IR hyperspectral imaging --- plasmonics --- copper --- VEGF --- glioblastoma --- differentiated neuroblastoma --- peptidomimetics --- real-time quantitative polymerase chain reaction (qPCR) --- actin --- combinatorial therapy --- anticancer and antibacterial activity --- temoporfin --- drug-in-cyclodextrin-in-liposome --- hybrid nanoparticles --- multicellular tumor spheroids --- cyclodextrins --- photodynamic therapy article --- yet reasonably common within the subject discipline --- antitumor strategy --- biomimetic core–shell nanoparticles --- NK cell-derived exosomes --- folate receptor --- albumin nanoparticle --- microfluidic --- cabazitaxel --- polydopamine nanoparticles --- size --- cytotoxicity --- iron affinity --- FA-DABA-SMA --- self-assembly --- oncogenic proteins --- intracellular disruption --- folic receptor alpha --- pancreatic cancer --- parvifloron D --- albumin --- erlotinib --- photodynamic therapy --- lipid nanoparticles --- tumor vectorization --- verteporfin --- ovarian carcinomatosis --- spheroids --- integrin --- RGD peptide --- cancer diagnosis --- radiotherapy --- hyperthermia therapy --- biomimetic --- nanocarrier --- membrane-wrapped --- cancer --- targeted delivery --- photothermal therapy --- imaging --- cancer nanomedicine --- tumor microenvironment --- nano–bio interactions --- clinical translation --- magnetic nanowires --- magnetic hyperthermia --- magnetic actuation --- magnetic drug targeting --- titanate nanotubes --- gold nanoparticles --- vectorization --- colloidal stability --- docetaxel --- prostate cancer --- mangiferin --- anti-topoisomerase activity --- extracellular vesicles --- exosomes --- chemico-physical functionalization --- loading --- translational medicine --- nanotechnology: bioengineering --- anacardic acid --- mitoxantrone --- targeted drug delivery --- liposomes --- melanoma --- apoptosis --- ascorbic acid --- angiogenesis --- epithelial-to-mesenchymal transition --- hypoxia --- immunosuppression --- metabolism --- nanotherapeutics --- tumour microenvironment --- DNA origami --- liposome --- remote loading --- acute toxicity --- organoids --- magnetic silica-coated iron oxide nanochains --- photothermal treatment --- hyperthermia --- collagen --- cellular microenvironment --- lymphadenectomy --- magnetometer --- sentinel lymph node dissection --- SPION --- superparamagnetic iron oxide nanoparticles --- Vδ2 T cells --- zoledronic acid --- polymeric nanoconstruct --- anti-tumor immunity --- colorectal carcinoma --- β-cyclodextrin nanosponges --- BALB-neuT mice --- brain tumours --- glioma --- blood brain barrier --- polymeric nanoparticles --- PEGylation --- dioleoylphosphatidylethanolamine --- poly(hydroxyethyl acrylate-co-allyl methyl sulfide) copolymer --- folate --- oxidation-sensitive release --- cellular interaction --- in vitro anti-cancer activity --- triple negative breast cancer --- organotin --- mesoporous silica nanoparticles --- MDA-MB-231 --- theranostic nanomaterials --- nanobiotechnology --- molecular imaging --- nanosystems --- nanomicelles --- ovarian cancer --- tumour targeting --- chemotherapeutics --- riboflavin --- vitamin B2 --- nanomedicines --- secondary structure --- mixed micelle --- pH responsive --- targeted therapy --- anti-cancer --- shear stress --- flow --- in vitro --- therapeutics --- diagnostics --- Immunotherapy