Irina Gaisina
Research Associate Professor, Pharmaceutical Sciences
Contact
Address:
833 South Wood Street, R. 497, Chicago, IL
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About Heading link
Overview:
I have extensive experience in hit-to-lead and lead optimization medicinal chemistry and preclinical drug development. One of the compounds I invented, a Glycogen Synthase Kinase beta (GSK-3β) inhibitor 9-ING-41 (licensed to a biopharmaceutical company Actuate Therapeutics, Inc.), has been recently approved by FDA for use in human clinical trials, phase 1/2 study in patients with refractory hematologic malignancies or solid tumors (ClinicalTrials.gov Identifiers: NCT03678883, NCT04239092 and NCT04218071). I have also worked in the epigenetic area, having successfully developed a new class of deacetylase-6 (HDAC6) inhibitors exhibiting tripartite inhibition of HDAC6, inhibition of HIF-1 prolyl hydroxylase (PHD), and activation of Nrf2 for the treatment of neurodegenerative diseases (two patents are licensed to Celgene Corporation). Beyond achievements in medicinal synthetic chemistry, my expertise includes drug database development for RTT therapy under an IRSF (International Rett Syndrome Foundation) initiative aimed to repurpose known drugs to facilitate drug development for this orphan disease. I created and managed a SMART (Selected Molecular Agents for Rett Therapy) Library of FDA-approved and experimental drugs that operate by diverse mechanisms (e.g. ampakines, growth hormone secretagogues, monoamine reuptake inhibitors, carbonic anhydrase inhibitors, HDAC inhibitors, histone lysine methyltransferase inhibitors, BDNF mimetics and others).The SMART Library Initiative had been supported with the funds from IRSF’s win in the Pepsi Refresh Project. Since 2014, I have been working at UICentre on multiple drug discovery projects and lead the design, planning and execution of organic synthesis of novel small molecules. My current research is focused on the development of anti-infective agents.
Teaching and Supervision Heading link
Selected Grants
High throughput screen for henipavirus drug development, Bill and Melinda Gates Foundation., 11/29/2022 - 11/30/2025, Obligated Amount: $3101691; Anticipated Amount: $3101691
Optimizing Ridaifen-B analogs as potential therapeutics for Ebola viruses, National Institutes of Health (National Institute of Allergy and Infectious Diseases)., 9/20/2022 - 7/31/2027, Obligated Amount: $2362748; Anticipated Amount: $3937392
Midwest AViDD Center-Project 1, University of Minnesota., 5/16/2022 - 4/30/2025, Obligated Amount: $911430; Anticipated Amount: $911430
Midwest AViDD Center-Core C, University of Minnesota., 5/16/2022 - 4/30/2024, Obligated Amount: $826788; Anticipated Amount: $826788
Development of 4-(aroylamino)piperidine-based entry inhibitors as anti-influenza therapeutics, Chicago BioSolutions Inc., 5/5/2022 - 4/30/2025, Obligated Amount: $1351877; Anticipated Amount: $1351877
The development of HDAC6 inhibitors for the treatment of opioid induced hyperalgesia, CCTS., 11/15/2019 - 11/15/2020, Obligated Amount: $30000; Anticipated Amount: $30000
★ 4- (Aminomethyl) Benzamides as Novel Anti-Ebola Agents, Chicago BioSolutions Inc., 8/16/2019 - 7/31/2023, Obligated Amount: $1039788; Anticipated Amount: $1039788
★ Development of group 2 influenza A virus entry inhibitors, Chicago BioSolutions Inc., 4/1/2019 - 3/31/2022, Obligated Amount: $336139; Anticipated Amount: $336139
★ Targeting APOE Modulated Neurovascular Dysfunction, National Institutes of Health (National Institute on Aging)., 4/1/2017 - 3/31/2021, Obligated Amount: $439725; Anticipated Amount: $439725
Selected Publications
Durante, Destiny, Bott, Ryan, Cooper, Laura, Owen, Callum, Morsheimer, Kimberly M, Patten, JJ, Zielinski, Christian, Peet, Norton P, Davey, Robert A, Gaisina, Irina N, Rong, Lijun, Moore, Terry W. (2024). N‑Substituted Pyrrole-Based Heterocycles as Broad-Spectrum Filoviral Entry Inhibitors. Journal of Medicinal Chemistry, 67, (16), 13737-13764. doi:10.1021/acs.jmedchem.4c00527.
Hushpulian, Dmitry M, Gaisina, Irina N, Nikulin, Sergey V, Chubar, Tatiana A, Savin, Svyatoslav S, Gazaryan, Irina G, Tishkov, Vladimir I. (2024). HIGH THROUGHPUT SCREENING IN DRUG DISCOVERY: PROBLEMS AND SOLUTIONS. Lomonosov chemistry journal, 65, (№2, 2024), 96-112. doi:10.55959/su0579-9384-2-2024-65-2-96-112.
Gaisina, Irina, Li, Ping, Du, Ruikun, Cui, Qinghua, Dong, Meiyue, Zhang, Chengcheng, Manicassamy, Balaji, Caffrey, Michael, Moore, Terry, Cooper, Laura, Rong, Lijun. (2024). An orally active entry inhibitor of influenza A viruses protects mice and synergizes with oseltamivir and baloxavir marboxil. Science Advances, 10, (8), eadk9004. doi:10.1126/sciadv.adk9004.
Alqarni, Saad, Cooper, Laura, Achi, Jazmin Galvan, Bott, Ryan, Sali, Veeresh Kumar, Brown, Andrew, Santarsiero, Bernard D, Krunic, Aleksej, Manicassamy, Balaji, Peet, Norton P, Zhang, Pin, Thatcher, Gregory RJ, Gaisina, Irina N, Rong, Lijun, Moore, Terry W. (2022). Synthesis, Optimization, and Structure–Activity Relationships of Imidazo[1,2‑a]pyrimidines as Inhibitors of Group 2 Influenza A Viruses. Journal of Medicinal Chemistry, 65, (20), 14104-14120. doi:10.1021/acs.jmedchem.2c01329.
Ahuja, Manuj, Kaidery, Navneet Ammal, Attucks, Otis C, McDade, Erin, Hushpulian, Dmitry M, Gaisin, Arsen, Gaisina, Irina, Ahn, Young Hoon, Nikulin, Sergey, Poloznikov, Andrey, Gazaryan, Irina, Yamamoto, Masayuki, Matsumoto, Mitsuyo, Igarashi, Kazuhiko, Sharma, Sudarshana M, Thomas, Bobby. (2021). Bach1 derepression is neuroprotective in a mouse model of Parkinson’s disease. Proceedings of the National Academy of Sciences of the United States of America, 118, (45), e2111643118. doi:10.1073/pnas.2111643118.
Gaisina, Irina N, Hushpulian, Dmitry M, Gaisin, Arsen M, Kazakov, Eliot H, Ammal Kaidery, Navneet, Ahuja, Manuj, Poloznikov, Andrey A, Gazaryan, Irina G, Thatcher, Gregory RJ, Thomas, Bobby. (2021). Identification of a potent Nrf2 displacement activator among aspirin-containing prodrugs. Neurochemistry International, 149, 105148. doi:10.1016/j.neuint.2021.105148.
Amaya, Moushimi, Cheng, Han, Borisevich, Viktoriya, Navaratnarajah, Chanakha K, Cattaneo, Roberto, Cooper, Laura, Moore, Terry W, Gaisina, Irina N, Geisbert, Thomas W, Rong, Lijun, Broder, Christopher C. (2021). A recombinant Cedar virus based high-throughput screening assay for henipavirus antiviral discovery. Antiviral Research, 193, 105084. doi:10.1016/j.antiviral.2021.105084.
Knopp, Rachel C, Jastaniah, Ammar, Dubrovskyi, Oleksii, Gaisina, Irina, Tai, Leon, Thatcher, Gregory RJ. (2021). Extending the Calpain–Cathepsin Hypothesis to the Neurovasculature: Protection of Brain Endothelial Cells and Mice from Neurotrauma. ACS Pharmacology & Translational Science, 4, (1), 372-385. doi:10.1021/acsptsci.0c00217.
Du, Ruikun, Cheng, Han, Cui, Qinghua, Peet, Norton P, Gaisina, Irina N, Rong, Lijun. (2021). Identification of a novel inhibitor targeting influenza A virus group 2 hemagglutinins. Antiviral Research, 186, 105013. doi:10.1016/j.antiviral.2021.105013.
Education
Degrees:
PhD, Institute of Organic Chemistry, Russian Academy of Sciences, Ufa, Russian Federation, 1994
Postgraduate Training:
Postdoc, Institut de Chimie des Substances Naturelles CNRS, France, 1999
Postdoc, Institut de Chimie des Substances Naturelles CNRS, France, 2002
Postdoc, Georgetown University, United States, 2003