Jane V Aldrich, V

Jane V Aldrich, V, Ph.D.

Professor

Department: Medicinal Chemistry
Business Phone: (352) 273-8708
Business Email: jaldrich@cop.ufl.edu

About Jane V Aldrich, V

Jane V. Aldrich, Ph.D., joined the University of Florida as professor of medicinal chemistry in 2015 under UF’s preeminence initiative in drug discovery and development. Dr. Aldrich’s research on analogs of opioid peptides has been continuously funded by the National Institute on Drug Abuse for over 25 years, and she has been the principal investigator of over $14 million in research grants. Following receiving her Ph.D. in medicinal chemistry, Dr. Aldrich was an NIH postdoctoral fellow at the University of Minnesota where she began her research on opioid peptides. She subsequently rose through the ranks at Oregon State University and the University of Maryland Baltimore prior to moving to the University of Kansas as professor of medicinal chemistry in 2001. Dr. Aldrich has served the scientific community in multiple capacities. She is currently chair of the NIH Drug Discovery for the Nervous System Study Section and also a Councilor for the Medicinal Chemistry Division of the American Chemical Society. She has also served as chair of the Medicinal Chemistry Division, president of the American Peptide Society, and co-chair of the Gordon Research Conference on the Chemistry and Biology of Peptides. She is currently on the editorial board of the Journal of Medicinal Chemistry and previously was an editor of the journal Letters in Peptide Science.

Accomplishments

Distinguished Alumni Award
2013 · Michigan State University
Leroy B. Townsend Lecturer
2012 · University of Michigan
Independent Scientist Award
1998-2009 · National Institute on Drug Abuse
Postdoctoral Fellowship
1984-1986 · NIH

Research Profile

Dr. Aldrich’s research focuses on the design and synthesis of peptide and peptidomimetic analogs of opioid peptides, along with the development of synthetic methods to prepare these compounds. A major emphasis has been peptide ligands for kappa opioid receptors as potential treatments for pain and drug abuse. These have included novel cyclic peptides that are active after oral administration, in addition to analogs of the endogenous dynorphin opioid peptides. These peptides are studied both in vitro for opioid activity and in vivo in collaboration with Dr. Jay McLaughlin in the Department of Pharmacodynamics. Dr. Aldrich’s laboratory is also studying the anticancer activity of novel cyclic peptides and has designed and synthesized labeled opioid peptides as tools to study opioid receptors.

Areas of Interest
  • Drug abuse
  • Drug discovery
  • Medicinal chemistry
  • Peptides

Publications

2020
Design, Synthesis, and Characterization of the Macrocyclic Tetrapeptide cyclo[Pro-Sar-Phe-d-Phe]: A Mixed Opioid Receptor Agonist-Antagonist Following Oral Administration.
ACS chemical neuroscience. 11(9):1324-1336 [DOI] 10.1021/acschemneuro.0c00086. [PMID] 32251585.
2020
Phenylalanine Stereoisomers of CJ-15,208 and [d-Trp]CJ-15,208 Exhibit Distinctly Different Opioid Activity Profiles.
Molecules (Basel, Switzerland). 25(17) [DOI] 10.3390/molecules25173999. [PMID] 32887303.
2020
Multifunctional opioid receptor agonism and antagonism by a novel macrocyclic tetrapeptide prevents reinstatement of morphine-seeking behaviour.
British journal of pharmacology. 177(18):4209-4222 [DOI] 10.1111/bph.15165. [PMID] 32562259.
2020
Optimized Ring Closing Metathesis Reaction Conditions To Suppress Desallyl Side Products in the Solid-Phase Synthesis of Cyclic Peptides Involving Tyrosine(O-allyl).
The Journal of organic chemistry. 85(3):1407-1415 [DOI] 10.1021/acs.joc.9b02345. [PMID] 31880448.
2018
Design, synthesis, and opioid activity of arodyn analogs cyclized by ring-closing metathesis involving Tyr(allyl).
Bioorganic & medicinal chemistry. 26(6):1157-1161 [DOI] 10.1016/j.bmc.2017.11.029. [PMID] 29273415.
2017
Alanine scan of the opioid peptide dynorphin B amide.
Biopolymers. 108(5) [DOI] 10.1002/bip.23026. [PMID] 28464209.
2017
Macrocyclic peptides decrease c-Myc protein levels and reduce prostate cancer cell growth.
Cancer biology & therapy. 18(8):571-583 [DOI] 10.1080/15384047.2017.1345384. [PMID] 28692379.
2016
Development of a robust, sensitive and selective liquid chromatography-tandem mass spectrometry assay for the quantification of the novel macrocyclic peptide kappa opioid receptor antagonist [D-Trp]CJ-15,208 in plasma and application to an initial pharmacokinetic study.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences. 1028:11-15 [DOI] 10.1016/j.jchromb.2016.05.043. [PMID] 27318293.
2016
Species differences in the effects of the κ-opioid receptor antagonist zyklophin.
Alcohol (Fayetteville, N.Y.). 51:43-9 [DOI] 10.1016/j.alcohol.2015.11.012. [PMID] 26992699.
2015
Structure-Activity Relationships of the Peptide Kappa Opioid Receptor Antagonist Zyklophin.
Journal of medicinal chemistry. 58(22):8783-95 [DOI] 10.1021/jm501827k. [PMID] 26491810.
2014
Alanine analogues of [D-Trp]CJ-15,208: novel opioid activity profiles and prevention of drug- and stress-induced reinstatement of cocaine-seeking behaviour.
British journal of pharmacology. 171(13):3212-22 [DOI] 10.1111/bph.12664. [PMID] 24588614.
2014
Zyklophin, a short-acting kappa opioid antagonist, induces scratching in mice.
Neuroscience letters. 563:155-9 [DOI] 10.1016/j.neulet.2014.01.022. [PMID] 24503508.
2013
Involvement of dynorphin and kappa opioid receptor in yohimbine-induced reinstatement of heroin seeking in rats.
Synapse (New York, N.Y.). 67(6):358-61 [DOI] 10.1002/syn.21638. [PMID] 23345075.
2013
Targeting inhibitor 2 of protein phosphatase 2A as a therapeutic strategy for prostate cancer treatment.
Cancer biology & therapy. 14(10):962-72 [DOI] 10.4161/cbt.25943. [PMID] 24025258.
2013
The macrocyclic peptide natural product CJ-15,208 is orally active and prevents reinstatement of extinguished cocaine-seeking behavior.
Journal of natural products. 76(3):433-8 [DOI] 10.1021/np300697k. [PMID] 23327691.
2013
The macrocyclic tetrapeptide [D-Trp]CJ-15,208 produces short-acting κ opioid receptor antagonism in the CNS after oral administration.
British journal of pharmacology. 169(2):426-36 [DOI] 10.1111/bph.12132. [PMID] 23425081.
2012
Opioid Peptides: Potential for Drug Development.
Drug discovery today. Technologies. 9(1):e23-e31 [PMID] 23316256.
View on: PubMed
2012
The permeation of dynorphin A 1-6 across the blood brain barrier and its effect on bovine brain microvessel endothelial cell monolayer permeability.
Peptides. 38(2):414-7 [DOI] 10.1016/j.peptides.2012.09.031. [PMID] 23046728.
2012
Analytical and biological methods for probing the blood-brain barrier.
Annual review of analytical chemistry (Palo Alto, Calif.). 5:505-31 [DOI] 10.1146/annurev-anchem-062011-143002. [PMID] 22708905.
2012
Novel opioid cyclic tetrapeptides: Trp isomers of CJ-15,208 exhibit distinct opioid receptor agonism and short-acting κ opioid receptor antagonism.
British journal of pharmacology. 165(4b):1097-108 [DOI] 10.1111/j.1476-5381.2011.01544.x. [PMID] 21671905.
2011
A convenient approach to synthesizing peptide C-terminal N-alkyl amides.
Biopolymers. 96(6):715-22 [DOI] 10.1002/bip.21600. [PMID] 22252422.
2011
Deletion of Ac-NMePhe(1) from [NMePhe(1) ]arodyn under acidic conditions, part 1: effects of cleavage conditions and N-terminal functionality.
Biopolymers. 96(1):97-102 [DOI] 10.1002/bip.21496. [PMID] 20560149.
2011
Deletion of Ac-NMePhe(1) from [NMePhe(1) ]arodyn under acidic conditions, part 2: effects of substitutions on pharmacological activity.
Biopolymers. 96(1):103-10 [DOI] 10.1002/bip.21495. [PMID] 20560148.
2011
Unexpected opioid activity profiles of analogues of the novel peptide kappa opioid receptor ligand CJ-15,208.
ChemMedChem. 6(9):1739-45 [DOI] 10.1002/cmdc.201100113. [PMID] 21761566.
2011
κ-Opioid receptor inhibition of calcium oscillations in spinal cord neurons.
Molecular pharmacology. 79(6):1061-71 [DOI] 10.1124/mol.111.071456. [PMID] 21422300.
2010
Synthesis of CJ-15,208, a novel κ-opioid receptor antagonist.
Tetrahedron letters. 51(38):5020-5023 [PMID] 22865937.
View on: PubMed
2009
Design and synthesis of cyclic arodyn analogues by ring-closing metathesis (RCM) for kappa opioid receptor (KOP) antagonists.
Advances in experimental medicine and biology. 611:279-80 [PMID] 19400192.
View on: PubMed
2009
Design, synthesis, and pharmacological activities of dynorphin A analogues cyclized by ring-closing metathesis.
Journal of medicinal chemistry. 52(18):5619-25 [DOI] 10.1021/jm900577k. [PMID] 19715279.
2009
Discovery of dermorphin-based affinity labels with subnanomolar affinity for mu opioid receptors.
Journal of medicinal chemistry. 52(23):7372-5 [DOI] 10.1021/jm9007592. [PMID] 19621878.
2009
Dual labeled peptides as tools to study receptors: nanomolar affinity derivatives of TIPP (Tyr-Tic-Phe-Phe) containing an affinity label and biotin as probes of delta opioid receptors.
Bioconjugate chemistry. 20(2):201-4 [DOI] 10.1021/bc800420t. [PMID] 19175314.
2009
Peptide kappa opioid receptor ligands: potential for drug development.
The AAPS journal. 11(2):312-22 [DOI] 10.1208/s12248-009-9105-4. [PMID] 19430912.
2009
Solid phase and solution synthesis of NvocLys(CO(CH2)5NH-NBD)OCH2CN, a trifunctional fluorescent lysine derivative.
Amino acids. 36(2):203-7 [DOI] 10.1007/s00726-008-0048-3. [PMID] 18365133.
2009
Synthesis of cyclic tetrapeptide CJ 15,208: a novel kappa opioid receptor antagonist.
Advances in experimental medicine and biology. 611:269-70 [PMID] 19400188.
View on: PubMed
2009
The effects of C-terminal modifications on the opioid activity of [N-benzylTyr(1)]dynorphin A-(1-11) analogues.
Journal of medicinal chemistry. 52(21):6814-21 [DOI] 10.1021/jm900715m. [PMID] 19807094.
2009
The synthesis of DAMGO-based potential affinity labels with high mu opioid receptor affinity and the formation of cyclic O-alkyl thiocarbamates.
Advances in experimental medicine and biology. 611:265-6 [PMID] 19400186.
View on: PubMed
2009
Zyklophin, a systemically active selective kappa opioid receptor peptide antagonist with short duration of action.
Proceedings of the National Academy of Sciences of the United States of America. 106(43):18396-401 [DOI] 10.1073/pnas.0910180106. [PMID] 19841255.
2008
High affinity conformationally constrained nociceptin/orphanin FQ(1-13) amide analogues.
Journal of medicinal chemistry. 51(15):4385-7 [DOI] 10.1021/jm800394v. [PMID] 18624395.
2008
Solid Phase Synthesis and Application of Labeled Peptide Derivatives: Probes of Receptor-Opioid Peptide Interactions.
International journal of peptide research and therapeutics. 14(4):315-321 [PMID] 19956785.
View on: PubMed
2007
Reinstatement of cocaine place-conditioning prevented by the peptide kappa-opioid receptor antagonist arodyn.
European journal of pharmacology. 569(1-2):84-9 [PMID] 17568579.
View on: PubMed
2005
[Nalpha-benzylTyr1,cyclo(D-Asp5,Dap8)]- dynorphin A-(1-11)NH2 cyclized in the “address” domain is a novel kappa-opioid receptor antagonist.
Journal of medicinal chemistry. 48(14):4500-3 [PMID] 15999987.
View on: PubMed
2005
Structure-activity relationships of arodyn, a novel acetylated kappa opioid receptor antagonist.
The journal of peptide research : official journal of the American Peptide Society. 65(3):322-32 [PMID] 15787962.
View on: PubMed
2005
Translocation of dynorphin neuropeptides across the plasma membrane. A putative mechanism of signal transmission.
The Journal of biological chemistry. 280(28):26360-70 [PMID] 15894804.
View on: PubMed
2004
An affinity label for delta-opioid receptors derived from [D-Ala2]deltorphin I.
The journal of peptide research : official journal of the American Peptide Society. 63(2):108-15 [PMID] 15009532.
View on: PubMed
2004
Synthesis and opioid activity of side-chain-to-side-chain cyclic dynorphin A-(1-11) amide analogues cyclized between positions 2 and 5. 1. Substitutions in position 3.
Journal of medicinal chemistry. 47(2):446-55 [PMID] 14711314.
View on: PubMed
2003
A novel N-terminal cyclic dynorphin A analogue cyclo(N,5)[Trp(3),Trp(4),Glu(5)] dynorphin A-(1-11)NH(2) that lacks the basic N-terminus.
Journal of medicinal chemistry. 46(8):1279-82 [PMID] 12672226.
View on: PubMed
2003
A solid-phase synthetic strategy for labeled peptides: synthesis of a biotinylated derivative of the delta opioid receptor antagonist TIPP (Tyr-Tic-Phe-Phe-OH).
Organic letters. 5(5):613-6 [PMID] 12605472.
View on: PubMed
2003
Dermorphin-based potential affinity labels for mu-opioid receptors.
The journal of peptide research : official journal of the American Peptide Society. 61(1):40-5 [PMID] 12472847.
View on: PubMed
2003
Effects of the substitution of Phe4 in the opioid peptide [D-Ala8]dynorphin A-(1-11)NH2.
Journal of medicinal chemistry. 46(19):4002-8 [PMID] 12954053.
View on: PubMed
2003
Synthesis and evaluation of derivatives of leucine enkephalin as potential affinity labels for delta opioid receptors.
Biopolymers. 71(5):552-7 [PMID] 14635095.
View on: PubMed
2003
Synthesis and evaluation of potential affinity labels derived from endomorphin-2.
The journal of peptide research : official journal of the American Peptide Society. 61(2):58-62 [PMID] 12492899.
View on: PubMed
2003
Synthesis of novel basic head-to-side-chain cyclic dynorphin A analogs: strategies and side reactions.
Biopolymers. 71(6):620-37 [PMID] 14991673.
View on: PubMed
2002
Solid phase synthesis and evaluation of Tyr-Tic-Phe-Phe(p-NHCOCH(2)Br) ([Phe(p-bromoacetamide)(4)]TIPP), a potent affinity label for delta opioid receptors.
Journal of medicinal chemistry. 45(18):3820-3 [PMID] 12190304.
View on: PubMed
2002
Identification of arodyn, a novel acetylated dynorphin A-(1-11) analogue, as a kappa opioid receptor antagonist.
Journal of medicinal chemistry. 45(26):5617-9 [PMID] 12477343.
View on: PubMed
2001
Dynorphin A analogs containing a conformationally constrained phenylalanine derivative in position 4: reversal of preferred stereochemistry for opioid receptor affinity and discrimination of kappa vs. delta receptors.
Chirality. 13(3):125-9 [PMID] 11270320.
View on: PubMed
2000
Extended TIP(P) analogues as precursors for labeled delta-opioid receptor ligands.
Journal of medicinal chemistry. 43(26):5050-4 [PMID] 11150177.
View on: PubMed
2000
Synthesis and evaluation of isothiocyanate-containing derivatives of the delta-opioid receptor antagonist Tyr-Tic-Phe-Phe (TIPP) as potential affinity labels for delta-opioid receptors.
Journal of medicinal chemistry. 43(26):5044-9 [PMID] 11150176.
View on: PubMed
2000
Synthesis and evaluation of N,N-dialkyl enkephalin-based affinity labels for delta opioid receptors.
Journal of medicinal chemistry. 43(21):3941-8 [PMID] 11052799.
View on: PubMed
1999
A novel acetylated analogue of dynorphin A-(1-11) amide as a kappa-opioid receptor antagonist.
Journal of medicinal chemistry. 42(16):3011-3 [PMID] 10447942.
View on: PubMed
1997
N-alkylated derivatives of [D-Pro10]dynorphin A-(1-11) are high affinity partial agonists at the cloned rat kappa-opioid receptor.
European journal of pharmacology. 338(2):191-7 [PMID] 9456002.
View on: PubMed
1997
Synthesis and opioid activity of [D-Pro10]dynorphin A-(1-11) analogues with N-terminal alkyl substitution.
Journal of medicinal chemistry. 40(17):2733-9 [PMID] 9276018.
View on: PubMed
1997
Synthesis and opioid activity of conformationally constrained dynorphin A analogues. 2. Conformational constraint in the “address” sequence.
Journal of medicinal chemistry. 40(8):1211-8 [PMID] 9111295.
View on: PubMed
1995
Synthesis and opioid activity of conformationally constrained dynorphin A analogues. 1. Conformational constraint in the “message” sequence.
Journal of medicinal chemistry. 38(13):2410-7 [PMID] 7608905.
View on: PubMed
1993
Comparison of methods for the Fmoc solid-phase synthesis and cleavage of a peptide containing both tryptophan and arginine.
International journal of peptide and protein research. 42(1):58-63 [PMID] 8103765.
View on: PubMed
1993
Synthesis and opioid activity of dynorphin A-(1-13)NH2 analogues containing cis- and trans-4-aminocyclohexanecarboxylic acid.
Journal of medicinal chemistry. 36(8):1100-3 [PMID] 8097539.
View on: PubMed
1993
Synthesis and opioid activity of dynorphin A-(1-13)NH2 analogues containing cis- and trans-4-aminocyclohexanecarboxylic acid.
Journal of medicinal chemistry. 36(13):1921-2 [PMID] 8099977.
View on: PubMed
1992
Effect of modification of the basic residues of dynorphin A-(1-13) amide on kappa opioid receptor selectivity and opioid activity.
Journal of medicinal chemistry. 35(23):4330-3 [PMID] 1360025.
View on: PubMed
1992
N-terminal alkylated derivatives of [D-Pro10]dynorphin A-(1-11) are highly selective for kappa-opioid receptors.
Journal of medicinal chemistry. 35(24):4638-9 [PMID] 1361580.
View on: PubMed
1992
Synthesis and opioid activity of 2-substituted dynorphin A-(1-13) amide analogues.
International journal of peptide and protein research. 40(2):89-96 [PMID] 1359999.
View on: PubMed

Grants

Jul 2020 ACTIVE
OR-DRPD-ROF2020: Exploration of the SIM2 class as potential novel peptide anticancer therapeutics
Role: Principal Investigator
Funding: UF RESEARCH
Jun 2018 ACTIVE
A Novel Strategy for Prostate Cancer Therapy Targeting the c-Myc Oncoprotein
Role: Principal Investigator
Funding: US ARMY MED RES ACQUISITION
Sep 2015 – Aug 2020
Novel peptide antagonists as treatments for substance abuse
Role: Principal Investigator
Funding: US ARMY MED RES ACQUISITION
Apr 2015 ACTIVE
Peptidic Kappa Opioid Receptor Ligands as Potential Treatments for Drug Addiction
Role: Principal Investigator
Funding: NATL INST OF HLTH NIDA
Mar 2015 – Feb 2018
Peptidic Ligands for Kappa Opioid Receptors
Role: Principal Investigator
Funding: NATL INST OF HLTH NIDA

Education

Postdoc – Medicinal Chemistry
1986 · University of Minnesota
Ph.D. – Medicinal Chemistry
1983 · University of Michigan
B.S. – Biochemistry
1976 · Michigan State University

Teaching Profile

Courses Taught
2017-2018,2020
PHA5788C Patient Care 6
2015-2021
PHA7980 Research for Doctoral Dissertation
2019-2021
GMS6757 Introduction to Alzheimer’s Disease and Related Dementias: Clinical and Mechanistic Principles
2015-2021
PHA7979 Advanced Research
2015,2017-2020,2020-2021
PHA6447 Drug Design
2015,2020-2021
PHA6971 Research for Master’s Thesis
2018,2020-2021
DEN6251 Clin Manage Dent Pain
2016,2018-2021
PHA6935 Selected Topics in Pharmacy
2016,2020-2021
PHA6910 Supervised Research
2018-2019
PHA5789C Patient Care 7
2016-2018
PHA5878C Pt Care 3: Cv and Pulm
2015-2018
PHA6905C Research Procedures in Medicinal Chemistry
2018
CHM7980 Research for Doctoral Dissertation

Contact Details

Phones:
Business:
(352) 273-8708
Emails:

ALDRICH LAB