Arnold Group at University of Wisconsin-Milwaukee-Home Page
We are an academic research laboratory in field of chemical biology in the Department of Chemistry and Biochemistry at the University of Wisconsin -Milwaukee.

Our research is focused on two primary targets: 1) the vitamin D receptor and 2) the GABA (A) receptors.

Our approach is to develop small molecules that can function as molecular probes in complex biological systems and new drug candidates for diseases mediated by the two primary targets mentioned above.

We are combining many areas of science including medicinal chemistry, biochemistry, molecular biology, (bio)analytical chemistry, high throughput screening, assay development, virtual screening, molecular docking and pharmacological profiling.

PI: Prof. Alexander (Leggy) Arnold

 

News

November 27th: Our group got highlighted by a local TV station in regard to our Asthma work.

October 8th 2014: Dr. Arnold will present a seminar titled: Small Molecule-Mediated Gene Regulation Caused by Vitamin D Receptor-Coactivator Binding Inhibition at the Department of Biochemistry, Medical College of Wisconsin.

September 10th 2014: 1R01HL118561-01A1 grant"Development of new drugs for asthma by targeting GABA(A) receptors in the lung" got awarded by the National Heart, Lung, and Blood Institute to Dr. James Cook as Priniple Investigator and Dr. Alexander (Leggy) Arnold as Co-Investigator.

September 9th 2014: Christopher Goetz presents his research at the Medical College of Wisconsin Research Day 2014.

September 4th 2014: Luis Sanchez received the SURF2014 award.

August 15th 2014: Joshua Preston, Skylar Gabel-Eissens, and Chris Goetz presented their research at the Summer Undergraduate Research Symposium. Chris Goetz won the Best Poster Award.

August 13th 2014: Kelly Teske will present her oral presentation titled: "Development of Selective Non-Secosteroid Vitamin D Receptor Inhibitors" at the 248th ACS National Meeting & Exposition at the MEDI section in San Francisco.

August 10th 2014: Kelly Teske will present her poster titled: "Identification of New Vitamin D Receptor-Coregulator Inhibitors among Nuclear Receptor Ligands" at the 248th ACS National Meeting & Exposition in San Francisco.

July 31st 2014: Dr. Arnold will present a talk at the University of Groningen, Netherlands title: "Novel Modulators for the Vitamin D Receptor As Drug Candidates".

July 25th 2014: Our publication titled: "Anticancer activity of VDR-Coregulator Inhibitor PS121912" was accepted in Cancer Chemotherapy and Pharmacology.

July 8th 2014: The catalyst grant "Pharmacological Proof of Concept for a First-in-Class Asthma Therapy" got awarded by the UWM Research Foundation to Dr. James Cook as Priniple Investigator and Dr. Alexander (Leggy) Arnold as Co-Investigator.

July 8th 2014: The catalyst grant "The pharmacokinetics and in vivo efficacy of ROS-activated anticancer prodrugs" got awarded by the UWM Research Foundation to Dr. Xiaohua Peng as Priniple Investigator and Dr. Alexander (Leggy) Arnold as Co-Investigator.

July 6th 2014: Nina Yuan will present her oral talk at the Gordon Research Seminar for Ion Channels at Mount Holyoke College in South Hadley MA United States titled: Development of high-throughput assays to identify new alpha subtype-selective GABAa receptor modulators to treat anxiety and depression disorders.

June 19th 2014: Dr. Arnold will present a talk at the Vitamin D Workshop at Chicago with the title: "Vitamin D Receptor-Coregulator Inhibitors as Anti-Cancer Reagents.

June 1st 2014: Skylar Gabel-Eissens from UW-Whitewater will join the Arnold Group during the summer to synthesize new VDR-Coregulator Inhibitors.

May 15th 2014: Luis Sanchez, Joshua Preston, and Chris Goetz received each the SURF2014 award.

April 23th 2014: Nina Yuan received a travel grant for the Gordon Research Seminar for Ion Channels.

April 20th 2014: Kelly Teske received a travel grant from the ACS MEDI for 248th ACS National Meeting & Exposition in San Francisco.

April 18th 2014: Department of Chemistry and Biochemistry Research Symposium: Jonathan Bogart received the “Kovacic Award of Outstanding Performance in Organic Chemistry” and the “Outstanding Performance Award in Analytical Chemistry”

April 18th 2014: Department of Chemistry and Biochemistry Research Symposium: Kelly Teske received the Chemistry Alumni Award for Graduate Research for the 3rd best poster presentation titled: “Further Investigation of the First Non-Secosteroidal Antagonist for the Vitamin D Receptor”.

April 18th 2014: Our group presented the following work at the Department of Chemistry and Biochemistry Research Symposium: 1. Kelly Teske “Development of Selective Non-Secosteroid Vitamin D Receptor Inhibitors”; 2. Jonathan W. Bogart "The Synthesis and Evaluation of Potential Non-Secosteroid VDR-coactivator Inhibitors”; 3. Margaret L. Guthrie “Development of a Metabolic Stability Assay to Determine Drug-like Properties of Small Molecules”; 4. Joshua Preston “Sequence Verification of Nuclear Receptor Plasmids for Ligand-mediated Transcription Assays”; 5. Belaynesh Feleke “Novel VDR-Coregulator Inhibitors”; 6. Nina Yuan "Identifying New Treatments for the Brain: Electrophysiological Assay and Generation of a Stable Recombinant Cell Line”.

April 16th 2014: Dr. Arnold was selected to recieve the Office of Research/UWM Foundation Research Award.

April 11th 2014: Our group presented that following work at the UW-System Symposium for Undergraduate Researrch and Creatice Activity: Joshua Preston “Sequence Verification of Nuclear Receptor Plasmids for Ligand-mediated Transcription Assays” and Jonathan W. Bogart "The Synthesis and Evaluation of Potential Non-Secosteroid VDR-coactivator Inhibitors”. Jonathan was awared for his Outstanding Presentation.

April 10th 2014: Dr. Arnold will give a seminar about high throughput screening, assay development and hit validation at the Medical College of Wisconsin in course of the 2014 spring class titled Models of Disease and Drug Discovery.

April 9th 2014: Our group in collaboration with AviMed Pharmaceuticals got awarded a Translational Grant sponsored by the SE Wisconsin Applied Chemistry Center of Excellence titled: Commercialization of a Universal Kinase and GTPase Assay.

April 8th 2014: Our manuscript: "Identification of Pan Nuclear Receptor Modulators Among Nuclear Receptor Ligands using virtual screening" was accepted in Nuclear Receptor Research.

April 6th 2014: Kelly Teske's presentation titled “Development of Selective Non-Secosteroid Vitamin D Receptor Inhibitors” got accepted as oral presentation at the 248th ACS National Meeting & Exposition in San Francisco.

April 3rd 2014: Nina Yuan received the Student Travel Award sponsored by the UWM Department of Chemistry and Biochemistry.

April 2nd 2014: Kelly Teske and Nina Yuan received both the Graduate Student Travel Award sponsored by the UWM Graduate school

April 1st 2014: Nina Yuan got accepted for the Gordon Research Seminar for Ion Channels at Mount Holyoke College in South Hadley MA United States.

March 19th 2014: Dr. Sidhu will present "Development and Biology of Anti-Tumor effect of a novel Inhibitor of VDR and its coactivator interactions" at the ACS conference in Dallas, on Wednesday March 19th at 1:30 pm.

March 16th 2014: Dr. Arnold will present "Discovery of transcriptional modulators that target the vitamin D receptor" at the ACS conference in Dallas, on Sunday March 16th at 9:10 am.

March 8th, 2014: Our group presented the following work at the 6th Yao Yuan Biotech-Pharma Symposium at the Illinois Institute of Technology at Chicago 1. Kelly Teske “Further Investigation of the First Non-Secosteroidal Antagonist for the Vitamin D Receptor”; 2. Nina Yuan “Identifying New Treatments for the Brain: Anxiolytic Neurochemistry and Electrophysiology”; 3. Belaynesh Feleke “Novel VDR-Coregulator Inhibitors”; 4. Preetpal S. Sidhu “Novel VDR-Coactivator Inhibitors and Their Anti-Cancer Effects”; 5. Joshua Preston “Sequence Verification of Nuclear Receptor Plasmids for Ligand-mediated Transcription Assays”; 6. Jonathan W. Bogart “The Synthesis and evaluation of potential non-secosteroid VDR-coactivator inhibitors”.

March 5th-7th 2014: Dr. Arnold will host the Sosnovsky Lecture Series speaker 2014 Professor Lawrence Marnett, Director of the Vanderbilt Institute of Chemical Biology. Prof. Marnett will give a talk on Thursday the 6th titled "Targeting Cyclooxygenases as a Strategy for Improved Cancer Detection and Therapy" and a second talk on Friday the 7th titled "Oxygenation of Endocannabinoids by Cyclooxygenase-2: Novel Bioactive Lipid and Therapeutic Opportunities.

March 3rd 2014: Dr. Arnold was received the Technology Licensing Award from the UWM Research Foundation for the MSTI Assay Technology.

February 21st 2014: Dr. Arnold will present " Novel Vitamin D receptor Modulators as Drug Candidates" at the University of Illinois at Chicago, Dpartment of Medicianl Chemistry and Pharmacognosy from 11:30-12:30.

Feburary 10th 2014: We commercialized our MSTI probe to KeraFAST (Boston, USA). This probe can now be ordered online to identify promiscuous compounds among screening libraries.

February 5th 2014: Nina Yuan will present her Advanced Qualifying Examination titled: Application of automated patch clamp to determine GABA(A) receptor modulation by small molecules, Location Chemistry 110, 9:00 am.

Feburary 4th 2014: Our manuscript: "Modulation of Transcription mediated by the Vitamin D Receptor and the Peroxisome Proliferator-Activated Receptor δ in the presence of GW0742 analogs" was accepted in Journal of Biomolecular Research & Therapeutics.

January 30th 2014: Jonathan Bogart, Luis Sanchez, Robin Goy, and Joshua Preston received each the SURF2014 award.

January 29th 2014: Dr. Arnold accepted to served on the Advisory Boad of Bridges and Cures.

January 24th 2014: Dr. Chris Veldkamp (UW Whitewater) will present his semiar titled: "Chemokines, Cancer Metastasis and Drug Discovery Efforts" at UWM in room CHEM190 at 3:00 pm.

January 8th 2014: Our manuscript: "Development of Novel Vitamin D Receptor-Coactivator Inhibitors" was accepted in ACS Medicinal Chemistry Letters.

December 6th 2013: Our manuscript: "A Fluorescence-Based High Throughput Assay for the Determination of Small Molecule-Human Serum Albumin Protein Binding",  was accepted in Analytical and Bioanalytical Chemistry.

November 5th 2013: The abstract from Preetpal Sidhu"Development and Biology of Anti-Tumor effect of a novel Inhibitor of VDR and its coactivator interactions" was accepted for the ACS conference in Dallas, for Wednesday March 19th at 1:30 pm.

November 5th 2013: The abstract from Prof. Arnold"Discovery of Transcriptional Modulators that target the Vitamin D Receptor" was accepted for the ACS conference in Dallas, for Sunday March 16th at 8:30 pm.

November 1st 2013: The following students presented their research work at the American Chemical Society's Younger Chemists Committee poster presentation: 1. Joshua Preston “Sequence Verification of Nuclear Receptor Plasmids for Ligand-mediated Transcription Assays”; 2. Jonathan Bogart “The Synthesis and Evaluation of Potential Non-Secosteroid VDR-Coactivator Inhibitors”; 3. Belaynesh Feleke “Novel VDR-Coregulator inhibitors”; 4. Kelly Teske "Identification of the first non-secesteroid antagonist for the vitamin D receptor".

October 30th 2013: Collaborative publication in Genes & Cancer with Dr. Rakesh Singh: PT19c, Another Nonhypercalcemic Vitamin D2 Derivative, Demonstrates Antitumor Efficacy in Epithelial Ovarian and Endometrial Cancer Models.

October 15th 2013: Dr. Arnold accepted the invitation of Biomolecular Research & Therapeutics to become an editorial board member.

October 11th 2013: Dr. Arnold presented at the University of Wisconsin Whitewater, WI, titled:Discovery and Development of of non-secosteroid vitamin D receptor antagonists.

October 11th 2013: Dr. Arnold accepted the invitation of Nuclear Receptor Research to become an accociate edtior.

August 19th 2013: Jonathan Bogart presented the second best poster at the Undergraduate Research Summer Poster Session at UWM, Milwaukee. His poster was titled: The synthesis of non-seco-steroid VDR-coactivator inhibitors using the Hantzsch reaction.

August 19th 2013: Robin Goy presented his poster at the Undergraduate Research Summer Poster Session at UWM, Milwaukee, which was titled: Expression and Purification of the Retinoid X Receptor Gamma (RXRG).

August 19th 2013: Joshua Preston presented his poster at the Undergraduate Research Summer Poster Session at UWM, Milwaukee, which was titled: Gene sequencing of the Peroxisome Proliferator-Activated Receptor Alpha (PPARα) in pBIND.

August 3-4th 2013: Preetpal Sidhu presented at the Gordon Research Seminar "Medicinal Chemistry", Colby-Sawyer College New London NH, titled:  Development of first nanomolar inhibitor of the Vitamin D Receptor-Coactivator interaction.

June 13th 2013: Dr. Arnold recieved the Young Investigator Award at the 16th Workshop on Vitamin D, San Francisco, CA.

June 11-14th 2013: Dr. Arnold presented at the 16th Workshop on Vitamin D, San Francisco, CA, titled: Discovery and Development of of non-secosteroid vitamin D receptor antagonists.

June 2-7th 2013: Dr. Arnold presented at the Gordon Research Conference "High Throughput Chemistry & Chemical Biology, June 2-7, Colby-Sawyer College New London NH, titled: Identification and development of three new distinct classes of VDR non-secosteroidal modulators for metabolic diseases and cancer.

May 30th 2013: Dr. Arnold presented at Medical College of Wisconsin at the MASBIG meeting at 4:00 pm, room C2195 titled: Identification and Development of Three Different Classes of Vitamin D Receptor-Coactivator Binding Inhibitors.

May 29th 2013: Our manuscript titled: PPAR δ agonist GW0742 interacts weakly with multiple nuclear receptors including the vitamin D receptor was accepted for publication by Biochemistry.

May 22th 2013: Joshua Preston (Undergraduate Student) received the Summer 2013 SURF award.

May 19th 2013: Megan McCallum (Ph.D.) and Nicholas Nassif (B.S.) graduated from UWM.

May 17th 2013: Robin Goy (Undergraduate Student) received the Summer 2013 SURF award.

May 17th 2013: Jon Bogart (Undergraduate Student) received the Summer 2013 SURF award.

April 20th 2013: Megan McCallum received the Graduate School Research Award (Poster Award).

April 20th 2013: Nina Yuan received the Keith Hall Award for Excellence in Graduate Research (Poster Award).

April 20th 2013: Kelly Teske received the Moszynski Outstanding Teaching Assistant Award.

April 20th 2013: Megan McCallum received the Sosnovsky Award for Excellence in Graduate Research.

April 19th 2013: Nina Yuan presented at the Chemistry&Biochemistry Recruitment Day: Uppers, Downers, All Arounders: Identifying New Treatments for the Human Brain.

April 18th 2013: Megan McCallum passed her final defense. Her thesis is titled: High throughput approaches for the assessment for factors influencing bioavailability of small molecules in preclinical drug development.

April 12th 2013: R01MH096463 grant"Design fo New Therapeutic Agents to Tread Schizophrenia" got awarded by the National Institute of Mental Health to Dr. James Cook as Priniple Investigator and Dr. Alexander (Leggy) Arnold as Co-Investigator.

April 12th 2013: Nicholas Nassif will present at the NCUR 2013 in La Crosse, at 3:30 pm, poster session 8, titled: Expression and purification of the vitamin D receptor ligand binding domain for the identification of vitamin D receptor-coactivator inhibitors.

April 10th 2013: Dr. Preetpal Sidhu will present at the ACS meeting in New Orleans at 8:30 am, session: MEDI: Division of Medicinal Chemistry, titled:Chemical improvement of pharmacological properties of irreversible VDR-coactivator inhibitors and their evaluation in vivo using an ovarian cancer animal model.

April 10th 2013: Kelly Teske will present at the ACS meeting in New Orleans at 7:00 pm, session: MEDI: Division of Medicinal Chemistry, titled: Identification of the first non-secesteroid antagonist for the vitamin D receptor.

April 8th 2013: Kelly Teske will present at the ACS meeting in New Orleans at 8:00 pm, session: MEDI: Division of Medicinal Chemistry, titled: Identification of the first non-secesteroid antagonist for the vitamin D receptor.

April 7th 2013: Megan McCallum will present at the ACS meeting in New Orleans at 1:05 pm, session: Advances in Biopharmaceutical and Pharmaceutical Analysis, titled: A new fluoresent-based high throuphput method for the quantification of drug-protein binding interactions.

April 7th 2013: Megan McCallum will present at the ACS meeting in New Orleans at 1:45 pm, session: Advances in Biopharmaceutical and Pharmaceutical Analysis, titled: A high throuput approach for the identification of promiscuous inhibitors among screening libraries with the use of a nucleophilic fluorescent probe. Megan will also be the co-moderator for this session.

March 10th 2013: Dr. Arnold will present at the 2nd Congress of Steroid Research in Chicago at 10:15 am and 15:45 pm, poster session A, titled: Development of the first non-secosteroid antagonist to modulate vitamin D receptor function.

March 8th 2013: Kelly Teske presented her Advanced Qualifying Examination titled: Development of of novel vitamin D receptor modulators. Location Chemistry 110, 11:00 am.

February 8th 2013: Both, Megan McCallum and Kelly Teske, received the Graduate Student Travel Support awarded by the UWM Graduate School.

February 4th 2013: Nicholas Nassif (undergraduate student) received the Spring 2013 SURF award.

January 25th 2013: Dr. Moray Campbell from the Roswell Park Cancer Institute will give a talk titled "Expression and Regulation of micro-RNA in prostate cancer", room CHEM180 at 3:00 pm.

January 16th 2013: Nicholas Nassif's (undergraduate student) abstract submission was accepted at the NCUR conference 2013 in La Crosse, WI

January 14th 2013: Dr Premchendar Nandhikonda is presenting at the slas 2nd annual conference in Orlando (FL): Identification of Promiscuous Inhibitors in Screening Libraries with the use of an Intrinsically Fluorescent Probe: A High Throughput Screening Approach.

January 6th 2013: Publication in Journal of Biomolecular Screening accepted: High throughput identification of promiscuous inhibitors from screening libraries with the use of a thiol-containing fluorescent probe.

December 7th 2012: Megan McCallum will present her preliminary thesis review titled: High throughput approaches for the assessment of factions influencing bioavalability of small molecules in pre-clinial drug development. Location Chemistry 110, 1:30 pm.

November 6th 2012: Postdoctoral Researcher Interview: Varun Dewan (Department of Chemistry and Biochemistry), Ohio State University Columbus - "Dissecting Host-Viral Interactions in HIV-1 for Therapeutic Development" Location: Chem123, 2:30 pm.

November 1st 2012: Collaboration with CoNCERT Pharmaceuticals Inc. to further characterize CTP-354; a non-sedating subtype selective GABA(A) modulator.

September 21st 2012: Nina Yuan will present her seminar titled: Tunable, light-controlled interacting protein tags (TULIPs): a LOV story. Location: Chemistry 180, 3:00 pm.

August 27th 2012: 1R01NS076517-01A1 grant"Synthesis of Alpha2/Alpha3 GABA Agonists to Treat Neuropathic Pain" got awarded by the National Institute of Neurological Disorders and Stroke to Dr. James Cook as Priniple Investigator and Dr. Alexander (Leggy) Arnold as Co-Investigator.

August 17th 2012: Second Best Poster: Robin Goy presented the second best poster during the Summer Undergraduate Research Poster Session, UWM.

July 31st 2012: Catalyst Grant: Our group got awarded with the Catalyst Grant by the UWM Research Foundation "In vivo evaluation of selective inhibitors of the vitamin D receptor-coregulator interaction" funded by the Lynde and Harry Bradley Foundation and the Richard and Ethel Herzfeld Foundation.

July 18th 2012: New Postdoctoral Researcher Hire: Dr. PreetPal Singh Sidu accepted the position of a postdoctoral researcher in our group. Welcome Preetpal!

June 24th 2012: Postdoctoral Researcher Interview: PreetPal Singh Sidu (Department of Medicinal Chemistry and Institute for Structural Biology and Drug Discovery Virginia Commonwealth University, Richmond, VA) - Designing Allosteric Inhibitors of Thombin, Wednesday June 27th, 2012, 2:00pm.

May 7th 2012: Publication in Journal of Medicinal Chemistry accepted: "Discovery of the First Irreversible Small Molecule Inhibitors of the Interaction between the Vitamin D Receptor and Coactivators".

March 7th 2012: Research Growth Initiative grant "Vitamin D Receptor-Coregulator Interactions as Anticancer Targets" got awarded by the UWM Graduate School to Dr. Alexander (Leggy) Arnold.