Giulianotti, Marcello
Contact Info
Overview
overview
- My lab utilizes novel techniques in combinatorial and computational chemistry for the identification of hit compounds as well as hit to lead optimization. We employee technologies that allow for the rapid assessment of millions of small molecules and peptides using exponentially less samples. The technology can be applied to virtually any assay paradigm. We currently have active programs in the areas of obesity, cachexia, neurite outgrowth, tachyphylaxis, diabetic kidney disease, and bacterial resistance. We are always open to new collaborations as well as discussing advancements in the use of our core capabilities.
research interests
- Peptide libraries, library screening, small molecule libraries, medicinal chemistry, computational chemistry, hit to lead
Scholarly & Creative Works
selected publications
-
Article
-
2021Functional Mixture-Based Positional Scan Identifies a Library of Antagonist Tetrapeptide Sequences (LAtTeS) with Nanomolar Potency for the Melanocortin-4 Receptor and Equipotent with the Endogenous AGRP(86-132) AntagonistFull Text via DOI: 10.1021/acs.jmedchem.1c01417 Web of Science: 000709633100049
-
2020Tissue Chips in Space: Modeling Human Diseases in MicrogravityFull Text via DOI: 10.1007/s11095-019-2742-0
-
2018Scaffold Ranking and Positional Scanning Identify Novel Neurite Outgrowth Promoters with Nanomolar PotencyFull Text via DOI: 10.1021/acsmedchemlett.8b00425 Web of Science: 000447471800021
-
2016Small-Molecule Inhibitors Targeting Topoisomerase I as Novel Antituberculosis Agents. ANTIMICROBIAL AGENTS AND CHEMOTHERAPY. 60:4028-4036.
-
2015Combinatorial Libraries As a Tool for the Discovery of Novel, Broad-Spectrum Antibacterial Agents Targeting the ESKAPE PathogensFull Text via DOI: 10.1021/jm501628s Web of Science: 000353602200006
-
2015Identification of Small Molecule Inhibitors of Human As(III) S-Adenosylmethionine Methyltransferase (AS3MT). CHEMICAL RESEARCH IN TOXICOLOGY. 28:2419-2425.
-
2015Interaction fingerprints and their applications to identify hot spotsFull Text via DOI: 10.1007/978-1-4939-2914-6_20
-
2013Scaffold Ranking and Positional Scanning Utilized in the Discovery of nAChR-Selective Compounds Suitable for Optimization StudiesFull Text via DOI: 10.1021/jm401543h Web of Science: 000329331600020
-
2013Parallel synthesis of 1,6-disubstituted-1,2,4-triazin-3-ones on solid-phaseFull Text via DOI: 10.1021/co400064d
-
2012Fluorescent Mu selective opioid ligands from a mixture based cyclic peptide libraryFull Text via DOI: 10.1021/co300110t
-
2011Potent antimicrobial small molecules screened as inhibitors of tyrosine recombinases and Holliday junction-resolving enzymesFull Text via DOI: 10.1007/s11030-011-9333-2 Web of Science: 000300364700017
-
2011Integrating Virtual Screening and Combinatorial Chemistry for Accelerated Drug DiscoveryFull Text via DOI: 10.2174/138620711795767866 Web of Science: 000292772100004
-
2011Integrating computational and mixture-based screening of combinatorial librariesFull Text via DOI: 10.1007/s00894-010-0850-1 Web of Science: 000291041800025
-
2010Conformational landscape of platinum(II)-tetraamine complexes: DFT and NBO studiesFull Text via DOI: 10.1007/s10822-010-9328-6 Web of Science: 000276965100005
-
2009Identification, structure-activity relationships and molecular modeling of potent triamine and piperazine opioid ligandsFull Text via DOI: 10.1016/j.bmc.2009.06.026 Web of Science: 000268099700026
-
2009Modeling of peptides containing D-amino acids: Implications on cyclizationFull Text via DOI: 10.1007/s10822-009-9295-y
-
2003Efficient approach for the diversity-oriented synthesis of macro-heterocycles on solid-supportFull Text via DOI: 10.1016/S0040-4039(03)01219-X Web of Science: 000183780300037
-
2002Solid-phase synthesis of linear ureas tethered to hydantoins and thiohydantoinsFull Text via DOI: 10.1021/cc010064l Web of Science: 000174633500013
-
2001Solid-phase synthesis of bis-heterocyclic compounds from resin-bound orthogonally protected lysineFull Text via DOI: 10.1021/cc000061t Web of Science: 000167935000010
-
2000Solid-phase synthesis of bis-2-imidazolidinethiones from resin-bound tripeptidesFull Text via DOI: 10.1021/ol000225e Web of Science: 000089831900026
-
2000Solid-phase synthesis of substituted 2,3-diketopiperazines from reduced polyamidesFull Text via DOI: 10.1016/S0040-4020(00)00253-2 Web of Science: 000087032100006
-
1999Solid phase synthesis of 1,4-benzothiazepin-5-one derivativesFull Text via DOI: 10.1016/S0040-4039(99)00964-8 Web of Science: 000081122400006
-
1999Solid-Phase Synthesis of trisubstituted 2-imidazolidones and 2-imidazolidinethionesFull Text via DOI: 10.1021/cc980019m Web of Science: 000081948200005
-
1998Efficient solid phase synthesis of 3,5-disubstituted hydantoinsFull Text via DOI: 10.1016/S0040-4039(98)01874-7 Web of Science: 000076524100004
-
1998Solid phase synthesis of 2,4,5-trisubstituted thiomorpholin-3-onesFull Text via DOI: 10.1016/S0040-4039(98)00645-5 Web of Science: 000073724300014
-
Book Chapter
-
2011Solid-phase synthesis of heterocycles from peptides and amino acids. 269-318.Full Text via DOI: 10.1002/9781118141649.ch9
-
2002Combinatorial libraries: Equimolar incorporation of benzaldehyde mixtures in reductive alkylation reactions. 57-58.Full Text via DOI: 10.1007/0-306-46862-x_18
-
2002Synthesis of cyclic ureas and cyclic thioureas from acyl dipeptides. 264-266.Full Text via DOI: 10.1007/0-306-46862-x_109
-
2000
-
2000Solid phase synthesis of heterocyclic combinatorial libraries derived from peptides. 192-197.Web of Science: 000166933900049
-
1999
-
-
Conference
-
2022Discovery and Characterization of the First Biased Beta-Agonist That Favors Gs-Coupling vs Beta-Arrestin Mediated Desensitization: A New Class of Structurally Distinct Beta-Agonists for Treating Obstructive Lung Diseases. a3249-a3249.Full Text via DOI: 10.1164/ajrccm-conference.2022.205.1_meetingabstracts.a3249
-
2013TNFα-Based Peptides as Bioprobes for Exosites of ADAM ProteasesFull Text via DOI: 10.17952/23aps.2013.136
-
-
Meeting Abstract
-
2015Identification of novel chemotherapies targeting mitochondrial-cell communication. FASEB JOURNAL.Web of Science: 000361722705237
-
-
Note
-
Review
-
2020The value of antimicrobial peptides in the age of resistance. e216-e230.Full Text via DOI: 10.1016/S1473-3099(20)30327-3
-
2013Shifting from the single to the multitarget paradigm in drug discovery. 495-501.Full Text via DOI: 10.1016/j.drudis.2013.01.008
-
2012Expanding the medicinally relevant chemical space with compound libraries. 718-726.Full Text via DOI: 10.1016/j.drudis.2012.04.001
-
2008Visualization of the chemical space in drug discovery. 322-333.Full Text via DOI: 10.2174/157340908786786010
-
Research
principal investigator on
- Synthesis of Select Compounds awarded by BTB Japan Inc 2021 - 2022
- Novel and potent compounds that promote axon growth awarded by Craig H. Neilsen Foundation 2020 - 2022
- Melanocortin Receptor Selective Ligands awarded by University of Minnesota 2021 - 2022
- Dealing with antibiotic resistance: antisense technology - novel compound synthesis 2021
- Synthesis of Compounds 2155-14 and 2155-18 awarded by Nova Southeastern University 2020 - 2021
- Synthesis of Select Compounds awarded by BTB Japan Inc 2020
- NPQ/SPEXIN THE ENDOGENOUS LIGAND FOR THE GALANIN RECEPTOR 3 awarded by National Institute on Drug Abuse 2020
Contact
full name
- Marcello Giulianotti
visualizations
Recent publications and grants in Scholars@FIU
