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410 37 18 $2 - College of PharmacyRanjala Ratnayake, Ph.D. Assistant Director. PO Box 100485 •...

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Hendrik Luesch, Ph.D. Director PO Box 100485 • Gainesville, FL 32610 • 352-273-7738 PHARMACY.UFL.EDU/MC/RESEARCH/RESEARCH-CENTERS/CNPD3 CENTER FOR NATURAL PRODUCTS, DRUG DISCOVERY & DEVELOPMENT Hendrik Luesch, Ph.D. Debbie and Sylvia DeSantis Chair in Natural Products Drug Discovery and Development Professor and Chair, Department of Medicinal Chemistry Director, Center for Natural Products, Drug Discovery and Development 410 square-foot screening laboratory 37 graduate students and postdoctoral fellows 18 faculty and co-faculty $2.2 million in research funds The instatement of the Center for Natural Products, Drug Discovery and Development, or CNPD3, was approved in summer of 2013 in recognition of the urgent need for concerted drug discovery and development at the University of Florida. The CNPD3 headquarters is based in the department of medicinal chemistry in the College of Pharmacy at the Medical Science Building. Mission The mission of UF’s CNPD3 is to foster early-stage drug discovery by providing the infrastructure, chemical libraries and expertise to screen for disease-relevant targets and for drug-like disease-modifying molecules that modulate target activity. The CNPD3 provides the academic home for the identification of drug leads and subsequent development campaigns carried out in concert with other biomedical centers at UF to drive forward preclinical and clinical drug development. Focus The focus of the CNPD3 is on unique natural products, and the goal is to fully exploit the biosynthetic and therapeutic potential of untapped biodiversity for drug discovery. Lead compounds are investigated for further development through interactive chemistry and pharmacology efforts. Natural product-like libraries that cover therapeutically relevant chemical space are generated and screened. Education and Training The educational and training objective is to integrate all Ph.D. graduate students and postdoctoral fellows whose interdisciplinary interests are focused on drug discovery. The CNPD3 provides both drug discovery expertise and the infrastructure to screen for novel targets and chemical entities that modulate target activity.
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Page 1: 410 37 18 $2 - College of PharmacyRanjala Ratnayake, Ph.D. Assistant Director. PO Box 100485 • Gainesville, FL 32610 • 352-627-9220. PHARMACY.UFL.EDU/MC/RESEARCH/RESEARCH-CENTERS/CNPD3

Hendrik Luesch, Ph.D. Director PO Box 100485 • Gainesville, FL 32610 • 352-273-7738

P H A R M A C Y . U F L . E D U / M C / R E S E A R C H / R E S E A R C H - C E N T E R S / C N P D 3

CENTER FOR NATURAL PRODUCTS, DRUG DISCOVERY & DEVELOPMENT

Hendrik Luesch, Ph.D.Debbie and Sylvia DeSantis Chair

in Natural Products Drug Discovery and Development

Professor and Chair, Department of Medicinal Chemistry

Director, Center for Natural Products, Drug Discovery and Development

410 square-foot screening

laboratory

37 graduate students and

postdoctoral fellows

18 faculty and co-faculty

$2.2 million in research funds

The instatement of the Center for Natural Products, Drug Discovery and Development, or CNPD3, was approved in summer of 2013 in recognition of the urgent need for concerted drug discovery and development at the University of Florida. The CNPD3 headquarters is based in the department of medicinal chemistry in the College of Pharmacy at the Medical Science Building.

MissionThe mission of UF’s CNPD3 is to foster early-stage drug discovery by providing the infrastructure, chemical libraries and expertise to screen for disease-relevant targets and for drug-like disease-modifying molecules that modulate target activity. The CNPD3 provides the academic home for the identification of drug leads and subsequent development campaigns carried out in concert with other biomedical centers at UF to drive forward preclinical and clinical drug development.

FocusThe focus of the CNPD3 is on unique natural products, and the goal is to fully exploit the biosynthetic and therapeutic potential of untapped biodiversity for drug discovery. Lead compounds are investigated for further development through interactive chemistry and pharmacology efforts. Natural product-like libraries that cover therapeutically relevant chemical space are generated and screened.

Education and TrainingThe educational and training objective is to integrate all Ph.D. graduate students and postdoctoral fellows whose interdisciplinary interests are focused on drug discovery. The CNPD3 provides both drug discovery expertise and the infrastructure to screen for novel targets and chemical entities that modulate target activity.

Page 2: 410 37 18 $2 - College of PharmacyRanjala Ratnayake, Ph.D. Assistant Director. PO Box 100485 • Gainesville, FL 32610 • 352-627-9220. PHARMACY.UFL.EDU/MC/RESEARCH/RESEARCH-CENTERS/CNPD3

Ranjala Ratnayake, Ph.D. Assistant Director PO Box 100485 • Gainesville, FL 32610 • 352-627-9220

P H A R M A C Y . U F L . E D U / M C / R E S E A R C H / R E S E A R C H - C E N T E R S / C N P D 31/31/17

ResearchThe center embraces all aspects of natural products research from discovery, biosynthesis and chemical synthesis, assay development, screening and target identification to drug development. CNPD3 members prepare and annotate diverse natural and synthetic chemical libraries for screening and subsequent medicinal chemistry efforts and use genomic approaches to manipulate microbial natural products chemistry.

ê Natural Products Discovery

ê Synthesis of Natural Products and Natural Product-Like Libraries

ê Drug Design and Medicinal Chemistry

ê Biosynthetic Engineering

ê Targets and Pharmacology

ê PK/PD and Development

ê Drug Metabolism

ê Screening in Model Organisms

ActivitiesThe CNPD3 provides the infrastructure to screen for novel targets and chemical entities that modulate target activity. Target discovery and validation require genomic scale libraries for overexpression, or gain-of-function, and siRNA-mediated knockdown, or loss-of-function. Validated targets are screened against drug-like small molecule libraries. Assays are miniaturized and made “HTS-ready.” Hits are optimized and developed into probes and/or drug candidates through medicinal chemistry and pharmaceutical development campaigns. To complement these activities, genomes of unexplored microbes will be analyzed for biosynthetic potential to discover new natural products that are not expressed under “standard” conditions. Additionally, the CNPD3 explores the scientific basis of selected nutraceuticals and dietary supplements.

CENTER FOR NATURAL PRODUCTS, DRUG DISCOVERY & DEVELOPMENT

% A

ctiv

ity

[Drug] (nM)1 10 100 1000

20

40

60

80

100

HN

N OO

NO

N O

O

S

NO

O

OH

Discovery

Screening

Medicinal Chemistry

Microbial Genomics

Medicinal ChemistryMicrobial GenomicsAssay Development

Molecular Diversity & Screening Structure Based Drug Design

CNPD3


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