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Marine habitats are promising sources to identify novel organisms and compounds. A total of 70% of the planet’s surface is covered by ocean, and little is known about the biosphere within these habitats. In the last few years, numerous novel bioactive compounds or secondary metabolites from marine environments have been described. This is, and will be, a promising source of candidate compounds in pharma research and chemical biology. In recent years, a number of novel techniques have been introduced to the field and it has become easier to actually (bio-)prospect compounds such as enzyme inhibitors. Those novel compounds then need to be characterized and evaluated in comparison to well-known representatives. This Special Issue focuses on the description of novel enzyme inhibitors of marine origin, including bioprospecting, omic approaches, and structural and mechanistic aspects.

sponge Monanchora pulchra --- pentacyclic guanidine alkaloids --- GH36 α-galactosidase --- GH109 α-N-acetylgalactosaminidase --- slow-binding irreversible inhibitor --- monanchomycalin B --- monanhocidin A --- normonanhocidin A --- Alzheimer′s disease --- BACE1 --- acetylcholinesterase --- in silico docking --- phlorotannins --- Ulva intestinalis --- ACE inhibitory peptide --- optimization --- purification --- structural identification --- molecular docking --- secondary metabolites --- Mycosphaerella sp. --- asperchalasine --- α-glucosidase --- kinase inhibitors --- drug development --- marine natural products --- inhibitor --- macroalgae --- marine fish --- protease --- Ulva ohnoi --- functional annotation --- structure–function relation --- natural products --- bioactives --- enzyme inhibition --- inactivation --- marine bacteria --- marine fungi --- marine sponges

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Marine habitats are promising sources to identify novel organisms and compounds. A total of 70% of the planet’s surface is covered by ocean, and little is known about the biosphere within these habitats. In the last few years, numerous novel bioactive compounds or secondary metabolites from marine environments have been described. This is, and will be, a promising source of candidate compounds in pharma research and chemical biology. In recent years, a number of novel techniques have been introduced to the field and it has become easier to actually (bio-)prospect compounds such as enzyme inhibitors. Those novel compounds then need to be characterized and evaluated in comparison to well-known representatives. This Special Issue focuses on the description of novel enzyme inhibitors of marine origin, including bioprospecting, omic approaches, and structural and mechanistic aspects.

Research & information: general --- sponge Monanchora pulchra --- pentacyclic guanidine alkaloids --- GH36 α-galactosidase --- GH109 α-N-acetylgalactosaminidase --- slow-binding irreversible inhibitor --- monanchomycalin B --- monanhocidin A --- normonanhocidin A --- Alzheimer′s disease --- BACE1 --- acetylcholinesterase --- in silico docking --- phlorotannins --- Ulva intestinalis --- ACE inhibitory peptide --- optimization --- purification --- structural identification --- molecular docking --- secondary metabolites --- Mycosphaerella sp. --- asperchalasine --- α-glucosidase --- kinase inhibitors --- drug development --- marine natural products --- inhibitor --- macroalgae --- marine fish --- protease --- Ulva ohnoi --- functional annotation --- structure–function relation --- natural products --- bioactives --- enzyme inhibition --- inactivation --- marine bacteria --- marine fungi --- marine sponges --- sponge Monanchora pulchra --- pentacyclic guanidine alkaloids --- GH36 α-galactosidase --- GH109 α-N-acetylgalactosaminidase --- slow-binding irreversible inhibitor --- monanchomycalin B --- monanhocidin A --- normonanhocidin A --- Alzheimer′s disease --- BACE1 --- acetylcholinesterase --- in silico docking --- phlorotannins --- Ulva intestinalis --- ACE inhibitory peptide --- optimization --- purification --- structural identification --- molecular docking --- secondary metabolites --- Mycosphaerella sp. --- asperchalasine --- α-glucosidase --- kinase inhibitors --- drug development --- marine natural products --- inhibitor --- macroalgae --- marine fish --- protease --- Ulva ohnoi --- functional annotation --- structure–function relation --- natural products --- bioactives --- enzyme inhibition --- inactivation --- marine bacteria --- marine fungi --- marine sponges

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Natural products hold a prominent position in the current discovery and development of drugs and have diverse indications for both human and animal health. Plants, in particular, play a leading role as a source of specialized metabolites with medical effects. Other organisms, such as marine and terrestrial animals and microorganisms, produce very important drug candidate molecules. Specialized metabolites from these varied natural sources can be used directly as bioactive compounds or drug precursors. In addition, due to their broad chemical diversity, they can act as drug prototypes and/or be used as pharmacological tools for different targets. Some examples of natural metabolites that have been developed into useful medical drug are cardiotonic digoxin from Digitalis sp., antimalarial artemisinin from Artemisia annua, anti-cancer taxol from Taxus sp., or podophyllotoxin from Podophyllum peltatum, which served as a synthetic model for the anti-cancer etoposide. The study of natural products is still attracting great scientific attention and their current importance, as a valuable lead for drug discovery, is undebatable. I cordially invite authors to contribute original articles, as well as survey articles, that give the readers of Molecules **MOLECULES NEEDS TO BE ITALICIZED** updated and new perspectives on natural products in drug discovery, including but not limited to natural sources, identification and separation of bioactive phytochemicals, standardization, new biological targets, pre-clinical and clinical trials, pharmacological effects/side effects, and bioassays.

dihydrochalcones --- cytotoxicity-guided --- n/a --- harpagoside --- biotechnology --- synergy --- Imperata cylindrica --- 5?-dimethylchalcone (DMC) --- antioxidant activity --- marine resources --- phenolic derivatives --- secondary metabolites --- antimicrobial agents --- antimicrobial resistance --- metabolomics --- Humulus lupulus --- chromatography --- stereochemistry --- FSE --- cytokines --- cytotoxic activity --- glutamate --- angiogenesis --- traditional medicine --- Ca2+ --- L6 cell --- human colon cancer cell lines --- siphonous green algae --- anti-inflammatory activity --- Phyllanthus chamacristoides --- spectroscopic analysis --- Physcomitrella patens --- Leishmania mexicana mexicana --- dementia --- prenylated phenolic compounds --- T2DM --- HPLC-ESI-microTOF-Q-MS/MS --- Eruca sativa --- Dryopteris fragrans --- chemosystematics --- 2? --- cerebellum --- Cleistocalyx operculatus --- inflammation --- multivariate data analysis --- Phyllanthus orbicularis --- HPLC --- cardiovascular disease --- Kv7 potassium channels --- marine peptides --- proliferation --- sulfated coumarins --- Orobanche s.l. --- phenylpropanoid glycosides --- Harpagophytum procumbens --- sesquiterpenoids --- TRPV1 --- Fideloside --- phenylethanoid glycosides --- Cuba --- molecular network --- NMR --- ketamine --- aging --- GLUT4 --- diabetes --- oxidative stress --- Lamiales --- circular dichroism --- psychosis --- antinociceptive --- immuno-regulation activity --- terpenoids --- NADPH oxidases --- diabetic neuropathy --- spagyric tincture --- H2S --- celastrol --- isolation and quantification --- 4?-dihydroxy-6?-methoxy-3? --- Leea indica --- C-glycoside --- neuropathic pain --- PANC-1 --- glucosinolates --- flavonoids --- bioactivities of natural products --- cardamonin --- isoflavones --- terpenes --- methicillin-resistant Staphylococcus aureus --- malaria --- artemisinin --- natural products --- devil’s claw --- ACE inhibitory peptide --- pPancreatic cancer --- growth inhibitory activity --- mass spectrometry --- flavonoid --- phenolics --- Astragalus boeticus L. --- proanthocyanidins --- opioid --- Trifolium --- Trypanosoma brucei brucei --- acetylated astragalosides --- Fabaceae --- bioactive peptides --- LC-MS --- Dasycladus vermicularis --- Orobanchaceae --- migration --- glucoerucin --- ESI-MS/MS --- cancer --- zebrafish --- antihypertensive --- Bacopa monnieri --- chemical derivatization --- hypertension --- devil's claw