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Photo of Irina Gaisina

Irina Gaisina


Research Associate Professor, Pharmaceutical Sciences

Contact

Address:

833 South Wood Street, R. 497, Chicago, IL

Related Sites:

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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.

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: $1575355; Anticipated Amount: $3937392

Midwest AViDD Center-Project 1, University of Minnesota., 5/16/2022 - 4/30/2024, 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 - 4/30/2023, Obligated Amount: $901251; Anticipated Amount: $901251

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

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.. Sci Adv, 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.

Jastaniah, Ammar, Gaisina, Irina N, Knopp, Rachel C, Thatcher, Gregory RJ. (2020). Synthesis of α‐Ketoamide‐Based Stereoselective Calpain‐1 Inhibitors as Neuroprotective Agents. ChemMedChem, 15, (23), 2280-2285. doi:10.1002/cmdc.202000385.

Antanasijevic, Aleksandar, Durst, Matthew A, Cheng, Han, Gaisina, Irina N, Perez, Jasmine T, Manicassamy, Balaji, Rong, Lijun, Lavie, Arnon, Caffrey, Michael. (2020). Structure of avian influenza hemagglutinin in complex with a small molecule entry inhibitor. Life Science Alliance, 3, (8), e202000724. doi:10.26508/lsa.202000724.

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

Professional Memberships

International Society for Antiviral Research, 1/27/2020 - Present

Selected Presentations

Ahuja, M, N. Ammal, Kaidery, Gaisina, Irina, Igarashi, K, Gomez, I Pina, Hamann, M, Attucks, O, Sharma, S, Thomas, Bobby. (2019 October 23). Screening of non-electrophilic Bach1 inhibitors in in vitro and in vivo models of neuroprotection. Society for Neuroscience Meeting.