A Review Discussing Synthesis and Translational Studies of Medicinal Agents Targeting Sphingolipid Pathways

Sphingolipids (SLs) are a class of bioactive lipids characterized by sphingoid bases (SBs) as their backbone structure. These molecules exhibit distinct cellular functions, including cell growth, apoptosis, senescence, migration, and inflammatory responses, by interacting with esterases, amidases, k...

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Main Authors: Sameena Mateen, Jordan Oman, Soha Haniyyah, Kavita Sharma, Ali Aghazadeh-Habashi, Srinath Pashikanti
Format: Article
Language:English
Published: MDPI AG 2025-07-01
Series:Biomolecules
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Online Access:https://www.mdpi.com/2218-273X/15/7/1022
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author Sameena Mateen
Jordan Oman
Soha Haniyyah
Kavita Sharma
Ali Aghazadeh-Habashi
Srinath Pashikanti
author_facet Sameena Mateen
Jordan Oman
Soha Haniyyah
Kavita Sharma
Ali Aghazadeh-Habashi
Srinath Pashikanti
author_sort Sameena Mateen
collection DOAJ
description Sphingolipids (SLs) are a class of bioactive lipids characterized by sphingoid bases (SBs) as their backbone structure. These molecules exhibit distinct cellular functions, including cell growth, apoptosis, senescence, migration, and inflammatory responses, by interacting with esterases, amidases, kinases, phosphatases, and membrane receptors. These interactions result in a highly interconnected network of enzymes and pathways, known as the sphingolipidome. Dysregulation within this network is implicated in the onset and progression of cardiovascular diseases, metabolic disorders, neurodegenerative disorders, autoimmune diseases, and various cancers. This review highlights the pharmacologically significant sphingoid-based medicinal agents in preclinical and clinical studies. These include myriocin, fingolimod, fenretinide, safingol, spisulosine (ES-285), jaspine B, D-e-MAPP, B13, and α-galactosylceramide. It covers enantioselective syntheses, drug development efforts, and advances in molecular modeling to facilitate an understanding of the binding interactions of these compounds with their biological targets. This review provides a comprehensive evaluation of chiral pool synthetic strategies, translational studies, and the pharmacological relevance of sphingolipid-based drug candidates, offering a pathway for future research in sphingolipid-based therapeutic development.
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spelling doaj-art-81d789eaa89b4659a98cd1a4fe92ed8b2025-08-20T03:08:05ZengMDPI AGBiomolecules2218-273X2025-07-01157102210.3390/biom15071022A Review Discussing Synthesis and Translational Studies of Medicinal Agents Targeting Sphingolipid PathwaysSameena Mateen0Jordan Oman1Soha Haniyyah2Kavita Sharma3Ali Aghazadeh-Habashi4Srinath Pashikanti5Biomedical and Pharmaceutical Sciences Department, Kasiska Division of Health Sciences, L.S. Skaggs College of Pharmacy, Idaho State University, Pocatello, ID 83209-8288, USABiomedical and Pharmaceutical Sciences Department, Kasiska Division of Health Sciences, L.S. Skaggs College of Pharmacy, Idaho State University, Pocatello, ID 83209-8288, USABiomedical and Pharmaceutical Sciences Department, Kasiska Division of Health Sciences, L.S. Skaggs College of Pharmacy, Idaho State University, Pocatello, ID 83209-8288, USABiomedical and Pharmaceutical Sciences Department, Kasiska Division of Health Sciences, L.S. Skaggs College of Pharmacy, Idaho State University, Pocatello, ID 83209-8288, USABiomedical and Pharmaceutical Sciences Department, Kasiska Division of Health Sciences, L.S. Skaggs College of Pharmacy, Idaho State University, Pocatello, ID 83209-8288, USABiomedical and Pharmaceutical Sciences Department, Kasiska Division of Health Sciences, L.S. Skaggs College of Pharmacy, Idaho State University, Pocatello, ID 83209-8288, USASphingolipids (SLs) are a class of bioactive lipids characterized by sphingoid bases (SBs) as their backbone structure. These molecules exhibit distinct cellular functions, including cell growth, apoptosis, senescence, migration, and inflammatory responses, by interacting with esterases, amidases, kinases, phosphatases, and membrane receptors. These interactions result in a highly interconnected network of enzymes and pathways, known as the sphingolipidome. Dysregulation within this network is implicated in the onset and progression of cardiovascular diseases, metabolic disorders, neurodegenerative disorders, autoimmune diseases, and various cancers. This review highlights the pharmacologically significant sphingoid-based medicinal agents in preclinical and clinical studies. These include myriocin, fingolimod, fenretinide, safingol, spisulosine (ES-285), jaspine B, D-e-MAPP, B13, and α-galactosylceramide. It covers enantioselective syntheses, drug development efforts, and advances in molecular modeling to facilitate an understanding of the binding interactions of these compounds with their biological targets. This review provides a comprehensive evaluation of chiral pool synthetic strategies, translational studies, and the pharmacological relevance of sphingolipid-based drug candidates, offering a pathway for future research in sphingolipid-based therapeutic development.https://www.mdpi.com/2218-273X/15/7/1022sphingolipidsnatural productsceramidechiral poolenantioselective synthesis
spellingShingle Sameena Mateen
Jordan Oman
Soha Haniyyah
Kavita Sharma
Ali Aghazadeh-Habashi
Srinath Pashikanti
A Review Discussing Synthesis and Translational Studies of Medicinal Agents Targeting Sphingolipid Pathways
Biomolecules
sphingolipids
natural products
ceramide
chiral pool
enantioselective synthesis
title A Review Discussing Synthesis and Translational Studies of Medicinal Agents Targeting Sphingolipid Pathways
title_full A Review Discussing Synthesis and Translational Studies of Medicinal Agents Targeting Sphingolipid Pathways
title_fullStr A Review Discussing Synthesis and Translational Studies of Medicinal Agents Targeting Sphingolipid Pathways
title_full_unstemmed A Review Discussing Synthesis and Translational Studies of Medicinal Agents Targeting Sphingolipid Pathways
title_short A Review Discussing Synthesis and Translational Studies of Medicinal Agents Targeting Sphingolipid Pathways
title_sort review discussing synthesis and translational studies of medicinal agents targeting sphingolipid pathways
topic sphingolipids
natural products
ceramide
chiral pool
enantioselective synthesis
url https://www.mdpi.com/2218-273X/15/7/1022
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