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UF Health University of Florida

College of Pharmacy

UNIVERSITY of FLORIDA

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Hendrik Luesch

Hendrik Luesch, Ph.D.

Professor And Chair, Debbie And Sylvia DeSantis Chair In Natural Products Drug Discovery And Development

Department: Medicinal Chemistry
Business Phone: (352) 273-7738
Business Email: luesch@cop.ufl.edu
CV: View Curriculum Vitae

About Hendrik Luesch

Hendrik Luesch, Ph.D., a professor of medicinal chemistry, received his Diplom in Chemistry at the University of Siegen (Germany) in 1997. He attended the University of Hawaii at Manoa to study marine natural products chemistry and obtained his Ph.D. in Chemistry under the supervision of Professor Richard E. Moore in 2002. He then undertook three years of postdoctoral studies as an Irving S. Sigal Fellow at The Scripps Research Institute in La Jolla working with Professor Peter G. Schultz in the area of functional genomics and chemical biology. In 2005 he joined the faculty of the Department of Medicinal Chemistry at the University of Florida as an assistant professor and was tenured and promoted to associate professor in 2010 and to full professor in 2015. He combines his interest in marine natural products chemistry with genomics and proteomics approaches for the discovery and characterization of potential drugs and molecular drug targets.

Publications

2020
Natural products as modulators of eukaryotic protein secretion
Natural Product Reports
2020
Tutuilamides A-C: Vinyl-Chloride-Containing Cyclodepsipeptides from Marine Cyanobacteria with Potent Elastase Inhibitory Properties
ACS Chemical Biology
2019
Isolation, Structure Elucidation and Biological Evaluation of Lagunamide D: A New Cytotoxic Macrocyclic Depsipeptide from Marine Cyanobacteria
Marine Drugs
2019
Discovery of Amantamide, a Selective CXCR7 Agonist from Marine Cyanobacteria
Organic Letters
2019
Discovery and Total Synthesis of Doscadenamide A: A Quorum Sensing Signaling Molecule from a Marine Cyanobacterium
Organic Letters
2019
Apratoxin S4 Inspired by a Marine Natural Product, a New Treatment Option for Ocular Angiogenic Diseases
Investigative Ophthalmology & Visual Science
2019
Chemical and Metagenomic Studies of the Lethal Black Band Disease of Corals Reveal Two Broadly Distributed, Redox-Sensitive Mixed Polyketide/Peptide Macrocycles
Journal of Natural Products
2019
Seaweed natural products modify the host inflammatory response via Nrf2 signaling and alter colon microbiota composition and gene expression
Free Radical Biology and Medicine
2018
The adaptive regulation of thiamine pyrophosphokinase-1 facilitates malignant growth during supplemental thiamine conditions
Oncotarget
2018
High-Yield Production of Herbicidal Thaxtomins and Thaxtomin Analogs in a Nonpathogenic Streptomyces Strain
2018
Discovery, Synthesis, Pharmacological Profiling, and Biological Characterization of Brintonamides A-E, Novel Dual Protease and Gpcr Modulators From a Marine Cyanobacterium
Journal Of Medicinal Chemistry
2018
Rational engineering of Streptomyces albus J1074 for the overexpression of secondary metabolite gene clusters
Microbial Cell Factories
2018
Apratyramide, a Marine-Derived Peptidic Stimulator of Vegf-a and Other Growth Factors With Potential Application in Wound Healing
ACS Chemical Biology
2018
Photosynthetic Production of Sunscreen Shinorine Using an Engineered Cyanobacterium
ACS Synthetic Biology
2018
Discovery of New A- and B-Type Laxaphycins With Synergistic Anticancer Activity
Bioorganic & medicinal chemistry
2018
Development of apratoxin S10 (Apra S10) as an anti-pancreatic cancer agent and its preliminary evaluation in an orthotopic patient-derived xenograft (PDX) model.
Investigational New Drugs
2018
Structural Diversity and Anticancer Activity of Marine-Derived Elastase Inhibitors: Key Features and Mechanisms Mediating the Antimetastatic Effects in Invasive Breast Cancer
Chembiochem
2018
An Efficient Buchwald-Hartwig/Reductive Cyclization for the Scaffold Diversification of Halogenated Phenazines: Potent Antibacterial Targeting, Biofilm Eradication, and Prodrug Exploration
2017
A Tryptoline Ring-Distortion Strategy Leads to Complex and Diverse Biologically Active Molecules from the Indole Alkaloid Yohimbine
Chemistry (Weinheim. Internet)
2017
Poly(<i>N</i>-(2-Hydroxypropyl) Methacrylamide)-Valproic Acid Conjugates as Block Copolymer Nanocarriers
Polymer Chemistry
2017
Cyanobacterial Sfp-Type Phosphopantetheinyl Transferases Functionalize Carrier Proteins of Diverse Biosynthetic Pathways
Scientific Reports
2017
Poly(N-(2-Hydroxypropyl)-Methacrylamide)-Valproic Acid Conjugates As Block Copolymer Nanocarriers
Polymer Chemistry
2017
Kempopeptin C, a Novel Marine-Derived Serine Protease Inhibitor Targeting Invasive Breast Cancer
Marine Drugs
2017
A Highly Potent Class of Halogenated Phenazine Antibacterial and Biofilm-Eradicating Agents Accessed Through a Modular Wohl-Aue Synthesis
Scientific Reports
2017
Grassystatins D-F, Potent Aspartic Protease Inhibitors From Marine Cyanobacteria As Potential Antimetastatic Agents Targeting Invasive Breast Cancer
Journal of Natural Products
2017
Synthesis and Biological Evaluation of Largazole Zinc-Binding Group Analogs
2016
Pitiamides a and B, Multifunctional Fatty Acid Amides From Marine Cyanobacteria
Planta Medica
2016
Structure-Activity Relationships of a Diverse Class of Halogenated Phenazines That Targets Persistent, Antibiotic-Tolerant Bacterial Biofilms and Mycobacterium tuberculosis
Journal of Medicinal Chemistry
2016
Total Synthesis of the Potent Marine-Derived Elastase Inhibitor Lyngbyastatin 7 and in Vitro Biological Evaluation in Model Systems for Pulmonary Diseases
Journal of organic chemistry (Online)
2016
Discovery, Total Synthesis and Key Structural Elements for the Immunosuppressive Activity of Cocosolide, a Symmetrical Glycosylated Macrolide Dimer From Marine Cyanobacteria
2015
Biological Targets and Mechanisms of Action of Natural Products From Marine Cyanobacteria
Natural Product Reports
2015
Caldora Penicillata Gen. Nov., Comb. Nov (Cyanobacteria), a Pantropical Marine Species With Biomedical Relevance
Journal of Phycology
2015
Amantelides a and B, Polyhydroxylated Macrolides With Differential Broad-Spectrum Cytotoxicity From a Guamanian Marine Cyanobacteriurn
Journal of Natural Products
2015
A Dive Into Membrane Dynamics With Sponge Peptides
Chemistry and Biology
2015
Halogenated Phenazines That Potently Eradicate Biofilms, Mrsa Persister Cells in Non-Biofilm Cultures, and Mycobacterium Tuberculosis
2015
Targeted Natural Products Discovery From Marine Cyanobacteria Using Combined Phylogenetic and Mass Spectrometric Evaluation
Journal of Natural Products
2014
Improved Total Synthesis and Biological Evaluation of Potent Apratoxin S4 Based Anticancer Agents With Differential Stability and Further Enhanced Activity
2014
Improved Total Synthesis and Biological Evaluation of Potent Apratoxin S4 Based Anticancer Agents With Enhanced Activity
Planta Medica
2014
Modulation of Activity Profiles for Largazole-Based Hdac Inhibitors Through Alteration of Prodrug Properties
ACS Medicinal Chemistry Letters
2014
Largazole Pharmacokinetics in Rats By Lc-Ms/Ms
Marine Drugs
2014
Grassypeptolides as Natural Inhibitors of Dipeptidyl Peptidase 8 and T-Cell Activation
Chembiochem
2014
Evaluation of Class I Hdac Isoform Selectivity of Largazole Analogues
Bioorganic & Medicinal Chemistry Letters
2013
Cultivated Sea Lettuce Is a Multiorgan Protector From Oxidative and Inflammatory Stress By Enhancing the Endogenous Antioxidant Defense System
Cancer Prevention Research
2013
Seaweed Extracts and Unsaturated Fatty Acid Constituents From the Green Alga Ulva Lactuca as Activators of the Cytoprotective Nrf2-Are Pathway
Free Radical Biology and Medicine
2013
Total Synthesis and Biological Evaluation of Grassypeptolide a
2013
In Vitro and in Vivo Characterization of a Tunable Dual-Reactivity Probe of the Nrf2-Are Pathway
ACS Chemical Biology
2013
Glucocorticoids and Histone Deacetylase Inhibitors Cooperate To Block the Invasiveness of Basal-Like Breast Cancer Cells Through Novel Mechanisms
Oncogene
2013
Potent Elastase Inhibitors From Cyanobacteria: Structural Basis and Mechanisms Mediating Cytoprotective and Anti-Inflammatory Effects in Bronchial Epithelial Cells
2013
Modular Strategies for Structure and Function Employed By Marine Cyanobacteria: Characterization and Synthesis of Pitinoic Acids
2012
Novel Elastase Inhibitors From Marine Cyanobacteria: Structural Diversity, Target-Bound Crystal Structures and Cellular Effects
Planta Medica
2012
Discovery and Mechanism of Natural Products as Modulators of Histone Acetylation
Current Drug Targets
2012
Cyanobacterial Peptides as a Prototype for the Design of Potent Beta-Secretase Inhibitors and the Development of Selective Chemical Probes for Other Aspartic Proteases
2012
Marine Cyanobacterial Fatty Acid Amides Acting On Cannabinoid Receptors
Chembiochem
2012
Chemistry and Biology of Novel Cyanobacterial Secondary Metabolites From Guam
Planta Medica
2012
Largazole: From Discovery To Broad-Spectrum Therapy
Natural Product Reports
2012
Total Synthesis of Grassystatin A, a Probe for Cathepsin E Function
2011
Pitiprolamide, a Proline-Rich Dolastatin 16 Analogue From the Marine Cyanobacterium Lyngbya Majuscula From Guam
Journal of Natural Products
2011
Combination Therapy Targeting Cancer Metabolism
Medical Hypotheses
2011
In Vitro and in Vivo Osteogenic Activity of Largazole
ACS Medicinal Chemistry Letters
2011
Pitipeptolides C-F, Antimycobacterial Cyclodepsipeptides From the Marine Cyanobacterium Lyngbya Majuscula From Guam
Phytochemistry
2011
Veraguamides A-G, Cyclic Hexadepsipeptides From a Dolastatin 16-Producing Cyanobacterium Symploca Cf. Hydnoides From Guam
Journal of Natural Products
2011
Bioactive Modified Peptides From Marine Cyanobacteria
Biopolymers
2011
Malyngamide 3 and Cocosamides a and B From the Marine Cyanobacterium Lyngbya Majuscula From Cocos Lagoon, Guam
Journal of Natural Products
2011
Systematic Chemical Mutagenesis Identifies a Potent Novel Apratoxin A/E Hybrid With Improved in Vivo Antitumor Activity
ACS Medicinal Chemistry Letters
2011
Combination Therapy for Renal Cell Cancer: What Are Possible Options?
Oncology
2011
Biological Effects of Byrsocarpus Coccineus in Vitro
Pharmaceutical Biology
2011
Lyngbyoic Acid, a "Tagged" Fatty Acid From a Marine Cyanobacterium, Disrupts Quorum Sensing in Pseudomonas Aeruginosa
Molecular bioSystems
2011
Marine Natural Products: a New Wave of Drugs?
Future Medicinal Chemistry
2011
Porpoisamides a and B, Two Novel Epimeric Cyclic Depsipeptides From a Florida Keys Collection of Lyngbya Sp.
2010
Weapons in Disguise-Activating Mechanisms and Protecting Group Chemistry in Nature
2010
Caylobolide B, a Macrolactone From Symplostatin 1-Producing Marine Cyanobacteria Phormidium Spp. From Florida
Journal of Natural Products
2010
Grassypeptolides A-C, Cytotoxic Bis-Thiazoline Containing Marine Cyclodepsipeptides
Journal of organic chemistry (Online)
2010
A Small-Molecule Inducer of the Antioxidant Response Element
Chemistry and Biology
2010
Isolation and Biological Evaluation of 8-Epi-Malyngamide C From the Floridian Marine Cyanobacterium Lyngbya Majuscula
Journal of Natural Products
2010
Anticolon Cancer Activity of Largazole, a Marine-Derived Tunable Histone Deacetylase Inhibitor
Journal of Pharmacology and Experimental Therapeutics
2010
Molassamide, a Depsipeptide Serine Protease Inhibitor From the Marine Cyanobacterium Dichothrix Utahensis
Journal of Natural Products
2010
Cytotoxic Halogenated Macrolides and Modified Peptides From the Apratoxin-Producing Marine Cyanobacterium Lyngbya Bouillonii From Guam
Journal of Natural Products
2010
Intramolecular Modulation of Serine Protease Inhibitor Activity in a Marine Cyanobacterium With Antifeedant Properties
Marine Drugs
2009
Lyngbyastatins 8-10, Elastase Inhibitors With Cyclic Depsipeptide Scaffolds Isolated From the Marine Cyanobacterium Lyngbya Semiplena
Marine Drugs
2009
Largamides A-C, Tiglic Acid-Containing Cyclodepsipeptides With Elastase-Inhibitory Activity From the Marine Cyanobacterium Lyngbya Confervoides
Planta Medica
2009
Apratoxin a Reversibly Inhibits the Secretory Pathway By Preventing Cotranslational Translocation
Molecular Pharmacology
2009
Construction and Characterization of Melanocortin-2 And-4 Receptor Chimeras
2009
A natural products approach to drug discovery: probing modes of action of antitumor agents by genome-scale cDNA library screening
Methods in Molecular Biology
2009
Phylogenetic and Chemical Diversity of Three Chemotypes of Bloom-Forming Lyngbya Species (Cyanobacteria: Oscillatoriales) From Reefs of Southeastern Florida
2009
Bioassay-Guided Isolation and Identification of Desacetylmicrocolin B From Lyngbya Cf. Polychroa
Planta Medica
2009
Tiglicamides A-C, Cyclodepsipeptides From the Marine Cyanobacterium Lyngbya Confervoides
Phytochemistry
2009
Activation of the Antioxidant Response Element By Specific Oxidized Metabolites of Linoleic Acid
Prostaglandins Leukotrienes and Essential Fatty Acids
2009
Grassystatins A-C From Marine Cyanobacteria, Potent Cathepsin E Inhibitors That Reduce Antigen Presentation
2009
Protection of Human Cultured Cells Against Oxidative Stress By Rhodiola Rosea Without Activation of Antioxidant Defenses
Free Radical Biology and Medicine
2009
Combinatorial Strategies By Marine Cyanobacteria: Symplostatin 4, An Antimitotic Natural Dolastatin 10/15 Hybrid That Synergizes With the Coproduced Hdac Inhibitor Largazole
Chembiochem
2009
Novel Natural Activators of the Antioxidant Response Element
Journal of the Neurological Sciences
2008
Total Synthesis and Molecular Target of Largazole, a Histone Deacetylase Inhibitor
Journal of the American Chemical Society.
2008
Orgn 523-Total Synthesis of Largazole
2008
Pompanopeptins a and B, New Cyclic Peptides From the Marine Cyanobacterium Lyngbya Confervoides
2008
Structure and Activity of Largazole, a Potent Antiproliferative Agent From the Floridian Marine Cyanobacterium Symploca Sp.
Journal of the American Chemical Society.
2008
Kempopeptins a and B, Serine Protease Inhibitors With Different Selectivity Profiles From a Marine Cyanobacterium, Lyngbya Sp.
Journal of Natural Products
2008
Total Structure Determination of Grassypeptolide, a New Marine Cyanobacterial Cytotoxin
2008
Bioactive Natural Products From Marine Cyanobacteria: New Structures and Modes of Action
Planta Medica
2008
Dragonamides C and D, Linear Lipopeptides From the Marine Cyanobacterium Brown Lyngbya Polychroa
Journal of Natural Products
2008
Synthesis and Activity of Largazole Analogues With Linker and Macrocycle Modification
2008
Serine Protease Inhibitors From the Floridian Marine Cyanobacterium Lyngbya Confervoides
Planta Medica
2008
Apratoxin E, a Cytotoxic Peptolide From a Guamanian Collection of the Marine Cyanobacterium Lyngbya Bouillonii
Journal of Natural Products
2008
Genome-wide overexpression screen for activators of antioxidant gene transcription
Methods in Molecular Biology
2007
A genomic screen for activators of the antioxidant response element
Proceedings of the National Academy of Sciences of the United States of America
2007
Lyngbyastatins 5-7, potent elastase inhibitors from Floridian marine cyanobacteria, Lyngbya spp
Journal of Natural Products
2006
Towards high-throughput characterization of small molecule mechanisms of action.
Molecular bioSystems
2006
A functional genomics approach to the mode of action of apratoxin A.
Nature Chemical Biology

Grants

Sep 2019 ACTIVE
Novel Targeted Anticancer Agents from Marine Cyanobacteria
NATL INST OF HLTH NCI · Principal Investigator
Aug 2019 – Mar 2020
Portential Anticancer Drug Leads from the Marine Sponges Collected off the Coast of Surigao City
MINDANAO STATE UNIVERSITY · Principal Investigator
Dec 2018 – Nov 2019
Identifying CxCR4 Receptor Agonists to Improve Diabetic Healing
UNIVERSITY OF COLORADO DENVER · Project Manager
Dec 2018 ACTIVE
Small Molecule Discovery for Particulate Guanylyl Cyclase Receptor B Enhancers
MAYO CLINIC · Project Manager
Aug 2018 ACTIVE
MRI: Acquisition of an X-Ray Diffractometer for Next Generation Functional Molecules and Materials
NATL SCIENCE FOU ·
Jul 2018 ACTIVE
Alkaloid Ring Distortion: A Platform for New Cancer Therapies
AMER CANCER SOC · Project Manager
Jul 2018 ACTIVE
OR-DRPD-ROF2018: A C. elegans based drug discovery platform for modulators of re-mRNA processing
UF RESEARCH ·
Sep 2017 ACTIVE
Utilization of Phenotypic Precision Medicine to Identify Optimal Drug Combinations for the Treatment of Hepatocellular Carcinoma
NATL INST OF HLTH NCATS ·
Dec 2016 ACTIVE
UF PASS: Regulation of exercise transducers
NATL INST OF HLTH NIA ·
Sep 2016 ACTIVE
Development of Complex Natural Product Libraries and Multidimensional Anticancer Screening Platforms
NATL INST OF HLTH NCI · Mentor
Jul 2016 – Jun 2018
NOVEL SYNTHETIC APRATOXINS ACTING THROUGH A NEW MECHANIS
OCALA ROYAL DAMES FOR CANCER RESEARCH · Principal Investigator
Jun 2014 – May 2017
Novel Therapeutics for activation of the antioxidant res
UF DSR OPPORTUNITY FUND · Project Manager
Dec 2013 – Nov 2015
Chemistry and Biology of Apratoxins
FL DEPT OF HLTH BANKHEAD-COLEY CANCER RE · Principal Investigator
Mar 2013 – Aug 2019
Novel Targeted Anticancer Agents from Marine Cyanobacteria
NATL INST OF HLTH NCI · Principal Investigator
Mar 2011 – Feb 2016
Mitochondrial Oxidative Stress in the Retinal Pigment Ep
NATL INST OF HLTH NEI · Project Manager

Patents

Published March 2010
Macrocyclic Compounds, Protease Inhibition, and Methods of Treatment
#US2011-0124569A1
Published December 2010
Macrocyclic Compounds and Methods of Treatment (New App.)
#2011-0123644 A1
Published May 2011
Apratoxin Therapetuic Agents: Mechanism and Methods of Treatment
#US 2011-0294720 A1
Issued March 2012
Macrocyclic Compounds and Methods of Treatment
#8,129,418
Published November 2012
Macrocyclic Compounds and Methods of Treatment
#US2013-0281497 A1
Issued January 2013
Macrocyclic Compounds and Methods of Treatment (DIV of 12606)
#8,357,708
Issued October 2013
Structure and Protease Activity of Grassystatins
#8,569,245
Issued June 2014
Methods of Preparation of Macrocyclic Compounds
#8,759,512
Published August 2014
Macrocyclic Compounds
#US2015-0038404 A1
Issued May 2015
Macrocyclic Compounds and Methods of Treatment (DIV of UF#12606)
#9,023,875
Issued June 2015
Macrocyclic Antiproliferation Agents and Methods of Treatment
#9,051,350
Published October 2015
Macrocyclic Compounds and Methods of Treatment
#US 2016/0106720
Published November 2015
Potent New Synthetic Apratoxins
#US-2016-0060299-A1
Issued November 2015
Macrocyclic Compounds and Methods of Treatment
#9,181,304
Published August 2016
Macrocyclic Therapeutic Agents, Methods of Manufacture, and Methods of Treatment
#US-2017-0057996
Issued November 2016
Combination Compositions and Methods of Treatment
#9,492,434
Issued August 2017
Seaweed Extracts, Unsaturated Aldehydes, and Methods of Treatment
#9,730,970
Issued November 2017
Macrocyclic Compounds and Methods of Treatment
#9,815,852
Issued July 2018
Seaweed Extracts, Unsaturated Fatty Acids, and Methods of Treatment
#10,010,569

Education

Postdoctoral Fellow
2002-2005 · The Scripps Research Institute
Ph.D.
2002 · University of Hawaii at Manoa
Diplom in Chemistry
1997 · University of Siegen

Contact Details

Phones:
Business:
(352) 273-7738
Emails:
Business:
luesch@cop.ufl.edu

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Research

Lab Members

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