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Protein import into the endoplasmic reticulum (ER) is the first step in the biogenesis of approximately 10,000 different soluble and membrane proteins of human cells, which amounts to about 30% of the proteome. Most of these proteins fulfill their functions either in the membrane or lumen of the ER plus the nuclear envelope, in one of the organelles of the pathways for endo- and exocytosis (ERGIC, Golgi apparatus, endosome, lysosome, and trafficking vesicles), or at the cell surface as plasma membrane or secreted proteins. An increasing number of membrane proteins destined to lipid droplets, peroxisomes or mitochondria are first targeted to and inserted into the ER membrane prior to their integration into budding lipid droplets or peroxisomes or prior to their delivery to mitochondria via the ER-SURF pathway. ER protein import involves two stages, ER targeting, which guarantees membrane specificity, and the insertion of nascent membrane proteins into or translocation of soluble precursor polypeptides across the ER membrane. In most cases, both processes depend on amino-terminal signal peptides or transmembrane helices, which serve as signal peptide equivalents. However, the targeting reaction can also involve the ER targeting of specific mRNAs or ribosome–nascent chain complexes. Both processes may occur co- or post-translationally and are facilitated by various sophisticated machineries, which reside in the cytosol and the ER membrane, respectively. Except for resident ER and mitochondrial membrane proteins, the mature proteins are delivered to their functional locations by vesicular transport.

chaperones --- contact sites --- endoplasmic reticulum --- ER-SURF --- membrane extraction --- mitochondria --- protein targeting --- bimolecular luminescence complementation --- competition --- split luciferase --- membrane proteins --- protein–protein interactions --- Sec61 complex --- Sec63 --- synthetic peptide complementation --- TRAP complex --- ER protein translocase --- signal peptide --- protein translocation --- nascent peptide chain --- membrane insertion --- molecular modelling --- molecular dynamics simulations --- molecular docking --- signal peptidase --- ER translocon --- signal recognition particle dependent protein targeting --- Sec61 dependent translocation --- co-translational translocation --- inhibitor --- high throughput screening --- Sec61 --- Sec62 --- folding --- insertion --- membrane protein --- translocon --- ribosome --- transmembrane segment --- lipid droplets --- peroxisomes --- PEX3 --- membrane protein insertion --- label-free quantitative mass spectrometry --- differential protein abundance analysis --- Zellweger syndrome --- GET --- protein transport --- SND --- SRP --- EMC --- positive-inside rule --- hydrophobicity --- transmembrane helix --- signal recognition particle --- nascent polypeptide-associated complex --- fidelity --- cyclotriazadisulfonamide --- ER quality control --- DNAJC3 --- preprotein --- Sec61 translocon --- ribosome stalling --- signal sequence --- Sec61 translocase --- NAC --- n/a --- protein-protein interactions

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This book is conceived to promote synergy between research and industrial activities in the design and development of new drugs and, therefore, is not limited to any specific aspect of development. It covers the entire process from the identification of a molecular target, studies of drug–protein interactions, the modeling and optimization of the functional activity, design and chemical synthesis, biological evaluation, and the development of new pharmaceutical carriers.The original articles and reviews are focused on the design and development of new anticancer treatments, new anticancer low-molecular-weight agents as potential drug substances, and the elucidation of their mechanisms of action. The book also includes studies on novel modulators of the serotonergic system used to treat central nervous system disorders, novel agents against infectious diseases, and the development of anti-plasmodial and anti-inflammatory agents. The successful identification of new compounds for development as drug substances comes from rich sources of medicinal plants and medicinal chemistry approaches.

Research & information: general --- Chemistry --- alpha-ketoglutarate --- cell cycle --- apoptosis --- JNK --- cell migration --- cell invasion --- TGF-β --- VEGF --- glycoconjugates --- methotrexate --- cancer treatment --- glucose metabolism --- drug design and discovery --- anticancer drugs --- targeted therapy --- Warburg effect --- antidepressants --- pyrido[1,2-c]pyrimidines --- dual 5-HT1A/SERT activity --- drug design --- anticancer activity --- lung cancer --- resveratrol --- PRI-2191 --- vitamin D --- active substance delivery systems --- biomedical hydrogels --- active substance-controlled release --- genistein --- hydrogels for cosmetology --- hydrogels for dermatology --- transdermal active substance delivery systems --- histone deacetylase (HDAC) --- depression --- biomarker --- anti-depressant therapy --- human DNA topoisomerase --- cancer --- drug --- molecular docking --- synthesis --- fluorine --- vitamin D3 --- metabolite --- A-ring --- CD-ring --- side-chain --- nanoparticles --- molecular modeling --- oxidation mechanisms --- electrochemistry --- MALDI --- spectroscopic data --- cytotoxic study --- self-assembled monolayer --- gold electrode --- multimodal activity --- calcium-sensing receptor --- enantiomer --- calcimimetic --- calcilytic --- colon cancer --- stereospecificity --- HT-29 --- IL-8 --- inflammation --- cyclooxygenase --- 1,2,4-triazole --- pyridazinone --- SAR --- anti-inflammatory activity --- antioxidant activity --- ADME --- anticancer drug --- antimicrobial peptide (AMP) --- dermaseptin --- frog skin peptides --- LHRH --- prostate cancer --- Phyllomedusa bicolor --- therapeutic peptides --- copper (II) complexes --- thiourea --- cytotoxic activity --- proteome analysis --- antimicrobial activity --- major latex protein --- Chelidonium majus --- greater celandine --- defense-related proteins --- alkaloids --- cancer cells --- vitamin D receptor --- split luciferase-based biosensor --- CYP24A1-dependent metabolism --- CYP27B1 --- rickets --- genome editing --- vitamin D biology and action --- transcription --- ChIP-chip analysis --- distal enhancers --- histone H3 acetylation --- RNA polymerase II --- analogue actions at genes --- vitamin D hormone (1,25(OH)2D3) --- latex --- antiviral proteins --- antimicrobial compounds --- cytotoxicity --- drug discovery --- CRISPR/Cas9 --- tetrahydro-β-carbolines --- Plasmodium falciparum (P. falciparum) --- antimalarial --- antiparasitic agents --- hemolysis --- vitamin D analogs --- 25 vitamin D 24-hydroxylase --- CYP24A1 --- proliferation --- high-grade serous ovarian cancer cells --- gold --- Au(III) complex --- colorectal cancer --- organometallic --- cancer therapy --- metallodrugs --- alpha-ketoglutarate --- cell cycle --- apoptosis --- JNK --- cell migration --- cell invasion --- TGF-β --- VEGF --- glycoconjugates --- methotrexate --- cancer treatment --- glucose metabolism --- drug design and discovery --- anticancer drugs --- targeted therapy --- Warburg effect --- antidepressants --- pyrido[1,2-c]pyrimidines --- dual 5-HT1A/SERT activity --- drug design --- anticancer activity --- lung cancer --- resveratrol --- PRI-2191 --- vitamin D --- active substance delivery systems --- biomedical hydrogels --- active substance-controlled release --- genistein --- hydrogels for cosmetology --- hydrogels for dermatology --- transdermal active substance delivery systems --- histone deacetylase (HDAC) --- depression --- biomarker --- anti-depressant therapy --- human DNA topoisomerase --- cancer --- drug --- molecular docking --- synthesis --- fluorine --- vitamin D3 --- metabolite --- A-ring --- CD-ring --- side-chain --- nanoparticles --- molecular modeling --- oxidation mechanisms --- electrochemistry --- MALDI --- spectroscopic data --- cytotoxic study --- self-assembled monolayer --- gold electrode --- multimodal activity --- calcium-sensing receptor --- enantiomer --- calcimimetic --- calcilytic --- colon cancer --- stereospecificity --- HT-29 --- IL-8 --- inflammation --- cyclooxygenase --- 1,2,4-triazole --- pyridazinone --- SAR --- anti-inflammatory activity --- antioxidant activity --- ADME --- anticancer drug --- antimicrobial peptide (AMP) --- dermaseptin --- frog skin peptides --- LHRH --- prostate cancer --- Phyllomedusa bicolor --- therapeutic peptides --- copper (II) complexes --- thiourea --- cytotoxic activity --- proteome analysis --- antimicrobial activity --- major latex protein --- Chelidonium majus --- greater celandine --- defense-related proteins --- alkaloids --- cancer cells --- vitamin D receptor --- split luciferase-based biosensor --- CYP24A1-dependent metabolism --- CYP27B1 --- rickets --- genome editing --- vitamin D biology and action --- transcription --- ChIP-chip analysis --- distal enhancers --- histone H3 acetylation --- RNA polymerase II --- analogue actions at genes --- vitamin D hormone (1,25(OH)2D3) --- latex --- antiviral proteins --- antimicrobial compounds --- cytotoxicity --- drug discovery --- CRISPR/Cas9 --- tetrahydro-β-carbolines --- Plasmodium falciparum (P. falciparum) --- antimalarial --- antiparasitic agents --- hemolysis --- vitamin D analogs --- 25 vitamin D 24-hydroxylase --- CYP24A1 --- proliferation --- high-grade serous ovarian cancer cells --- gold --- Au(III) complex --- colorectal cancer --- organometallic --- cancer therapy --- metallodrugs