Gerona-Navarro

Gerona-Navarro, Guillermo

Academic Appointments:

Assistant Professor, Chemistry Department, Brooklyn College, The City University of New York
Faculty, Chemistry, Biology and Biochemistry PhD Programs, The Graduate Center, The City University of New York

Degree(s)

Instructor, Structural Biology Department, Mount Sinai School of Medicine NY, NY.
Postdoctoral Fellow, Structural Biology Department, Mount Sinai School of Medicine NY, NY.
Postdoctoral Fellow, Pharmacology Department. Weill Medical College of Cornell University, NY, NY.

Ph.D. (Chemistry, Cum Laude), Complutense University of Madrid (UCM), Madrid, Spain
B.S (Chemistry), University of Havana, Cuba

Research Focus:

Research in our laboratory encompasses a broad spectrum of bioorganic and synthetic chemistry in both solution and solid phase, together with a wide array of biochemical and cell assays. Development of small molecules and peptidomimetics targeting protein-protein interactions inside of the cell are being performed to investigate the role of these biologically important proteins in human biology and disease. In particular, we are focused on developing novel peptidomimetic molecules targeting epigenetic molecular mechanisms linked to development and progression of several types of cancers.

Our efforts to date has led to the identification of novel inhibitors of the catalytic activity of the Polycomb Repressive Complex 2 (PRC2), a multimeric complex of proteins responsible for the trimethylation of histone 3 at lysine 27 (H3K27me3), a repressive post-translational modification mark dysregulated in many different cancers. Our compounds target PRC2 allosterically. Their unique mechanism of PRC2 inhibition, together with their potency, remarkable H3K27me3 inhibition selectivity, and low cytotoxicity to non-cancerous cells suggest that they may have great potential for future development of novel epigenetic cancer therapies.

 

Selected Publications (last 5 years)

Rodriguez, Y.; Gerona-Navarro, G.; Osman, R.; Zhou, Ming-Ming. “In Silico Design and Molecular Basis for the Selectivity of Olinone Towards the First over the Second Bromodomain of BRD4” (R) Proteins 2020, 88 (3), 414-430. doi: 10.1002/prot.25818. [Epub 2019 Oct 21]

Pérez Gordillo, F. L.; Pérez de Vega, M. J.; Gerona-Navarro, G.; Rodríguez, Y.; Álvarez de la Rosa, D.; González Muñiz, R.; Martín-Martínez, M. “Aldosterone-Mineralocorticoid Receptor – Cell Biology to Translational Medicine,” 978-1-83962-199-4, 2019, Peer-Reviewed Book Chapter: Advances in the Development of non-steroidal mineralocorticoid-receptor antagonists. http://mts.intechopen.com/articles/show/title/advances-in-the-development-of-non-steroidal-mineralocorticoid-receptor-antagonists

Zhang, G.; Barragan, F.; Wilson, K.; Levy, N.; Herskovits, A.; Rodríguez, Y.; Sapozhnikov, M.; Kelmendi, L.; Alkasimi, H.; Korsmo, H.; Chouwdhury, M, Gerona-Navarro, G. “A Solid Phase Approach to Accessing Bisthioether Stapled Peptides Resulting in a Potent Inhibitor of PRC2 Catalytic Activity” (R) Angew. Chem. Int. Ed. Eng. 2018, 57, 17073

Zang, G.; Andersen, J.; Gerona-Navarro, G*. Peptidomimetics Targeting Protein-Protein Interactions for Therapeutic Development. (R, REV) Protein Pept. Lett. 2018, 25, 1076-1089

Gerona-Navarro*, G.; Zhang, G; Barragan. F. Bisthioether Stapled Peptides as Inhibitors of PRC2 Function. (US Provisional Patent Application, serial number: 62/736,005. Filed on 09/25/2018).

Martín-Martínez M, Pérez-Gordillo FL, Álvarez de la Rosa D, Rodríguez Y, Gerona-Navarro G, González-Muñiz R, Zhou MM. “Modulating Mineralocorticoid Receptor with Non-steroidal Antagonists. New Opportunities for the Development of Potent and Selective Ligands without Off-target side effects” (R, REV) J. Med. Chem 2017, 60(7), 2629-2650

Ming-Ming Zhou, Guillermo Gerona-Navarro, Yoel Rodriguez, Patrizia Cassaccia. “Small Molecules Transcription Modulators of Bromodomains” (R) US Patent, Number: 10065951. Filed on 05/29/2015).

Gacias, M.*; Gerona-Navarro, G.*; Plotnikov, A.N.; Guangtao, Z.; Lei, Z.; Kaur, J.; Moy, G.; Rusinova, E.; Rodriguez, Y.; Matikainen, B.; Vincek, A.; Joshua, J.; Casaccia, P. & Zhou, Ming-Ming . “Selective Chemical Modulation of Gene Transcription Favors Oligodendrocyte Lineage Progression” (R) Cell Chem. Biol. 2014, 21(7), 851-854. *These authors contributed equally to this work.

Grants over the last 5 years

Ongoing Research Support

National Institutes of Health
1SC1GM136635-01                           Gerona-Navarro (PI)                           04/01/20 – 03/31/24
“Allosteric Modulators of Polycomb Repressive 2 Gene Repression as Potential Therapeutics for the Development of Novel Epigenetic Cancer Therapies”
Amount Funded: $1,570,000
Role: PI

Research Foundation of CUNY, The City University of New York
PSC CUNY Traditional B Grant         Gerona-Navarro (PI)                   06/01/2020 – 05/31/2021 “Allosteric Modulators of Polycomb Repressive 2 Gene Repression as Potential Therapeutics for the Development of Novel Epigenetic Cancer Therapies”
Amount Funded: $6000
Role: PI

Completed Research Support

National Institutes of Health
1SC2GM111231-01                           Gerona-Navarro (PI)                  08/01/2014 – 05/31/2018
“Chemical Probes Targeting Polycomb Repressive Complex 2 Gene Repression”
Amount Funded: $471,000
Role: PI

Research Foundation of CUNY, The City University of New York
PSC CUNY Traditional B Grant         Gerona-Navarro (PI)                   06/01/2018 – 05/31/2019 “Targeting VEFS-SUZ12: An alternative Strategy to Develop Novel Epigenetic Cancer Therapies”
Amount Funded: $6000
Role: PI

National Institutes of Health
1R03NS072578-01(R03)                     Gerona-Navarro (PI)             12/01/2010 – 11/30/2012 “Small Molecules Modulating Oligodendrocyte Lineage Progression”
Amount Funded: $168,000
Role: PI