Gopal Pundlik Jadhav, PhD
Board Membership, Creighton University, Health ans Safety
Assistant Professor
Contact
School of Medicine
Pharmacology and Neuroscience
Translational Hearing
CRISS III - Criss 3 - 558A
Gopal Pundlik Jadhav, PhD
Board Membership, Creighton University, Health ans Safety
Assistant Professor
After that, Dr. Jadhav worked for about two years as a senior research scientist at GlaxoSmithKline's RD Alternative Discovery & Development (Madrid Trescants, Spain) on a collaborative project that involved structural optimization of the hPDE4 inhibitor GSK675728A to produce novel pharmacophore(s) as potent TbrPDE1 inhibitors that are selective over hPDEs in the management of African sleeping sickness (CNS disorder).
Dr. Gopal started working as a postdoctoral researcher at Creighton University in June 2016 and was later promoted to assistant professor of medicinal chemistry in early 2017. He is presently tenure track faculty in the school of medicine working under Dr. Peter Abel.
Lab Research Focus: Dr. Jadhav’s Lab is aimed at;
A) Molecular docking and Structure Activity Relationship (SAR) based small molecular drug discovery to tackle biological problems such as Neuroinfllamatory disorders, Cancers, Noise induced hearing loss (NIHL) and Antibiotic resistant Bacterial infections. Current projects involve (1) Development of Triggering receptors expressed on myeloid cells-1 (TREM1) inhibitors to treat neuronal disorders, NIHL and liver cancer. (2) Development of small molecules as Mvfr inhibitors to treat antibiotic resistant Pseudomonas aeruginosa infections.
B) PROTAC (Proteolysis targeting chimeras) therapeutics: to address liver cancer and Neuroinflmmations.
C) Dual conjugates of Latanoprost acid to release Nitrous oxide (NO) and Hydrogen suflide (H2S) in the management of gloucoma.
Curriculum Vitae
Teaching Interests
- Synthetic organic chemistry: Hands on experience in modern synthetic organic chemistry like multi-step syntheses of drug like molecules, heterocycles, peptides, etc., parallel synthesis using Radley’s. Independent planning and execution of SAR.
Research Focus
Drug discovery in Cardiac and cardiovascular disordersDrug discovery in immuno and inflammatory disorders
Drug discovery in Quorum sensing
Drug discovery in Highly neglected diseases
Department
Pharmacology and Neuroscience
Position
Assistant Professor
Articles
- Molecules
Gopal P. Jadhav, Ishwinder Kaur, Peter M Fischer, Gerlof Sebastiaan Winkler Ishwinder Kaur,Gopal P. Jadhav *,† ,Peter M. Fischer * and Gerlof Sebastiaan Winkler * School of Pharmacy and Centre for Biomolecular Sciences, University of Nottingham, Nottingham NG7 2RD, UK * Authors to whom correspondence should be addressed. †Current address: School of Medicine, Creighton University, Omaha, NE 68178, USA. Molecules 2024, 29(18), 4351;
29(18), p. 4351 2024 - Epigenetics in Organ Specific Disorders
Gopal P. Jadhav, Amit M. Pant; Christopher J. Pelham Chapter 25 - Epigenetic drug discovery: Recent advances through structure-activity relationships and phenotypic profiling studies Abstract Epigenetic programming of gene expression is vital to normal physiology, and dysregulation of epigenetic proteins correlates with numerous diseases. Gene expression is known to be regulated through DNA and histone modifications. However, it is complicated to assess systematic changes caused by epigenetic modulators. Tools for epigenetic drug discovery continue to be developed through structure-activity relationship studies. Phenotypic profiling of human primary cells and cell lines opens the gateway to target identification and lead optimization to guide drug discovery campaigns. Epigenetic proteins, including readers, writers, and erasers, are putative drug targets in many diseases. Profiling assays provide insight into molecular mechanisms of epigenetic targets, predictive biomarker analysis, and chemical safety assessment. In this chapter, we highlight the advancements in epigenetic drug development via structure-activity relationship studies and cellular/phenotypic profiling assays. More extensive profiling system databases and focused chemical libraries will aid medicinal chemistry efforts toward development of small molecule epigenetic modulators that can have high implications in disease treatment.
34, p. 615-630 2023 - Nova Science
Book chapter entitled "Laser Technology to facilitate Drug Discovery and Development Processes; Perspective to recent advancements", Advances in Laser and Optic research, Laser therapies -Types, uses and safety; Chapter 10; Jan 2020Authors: Shantanu Hati and *Gopal P. Jadhav*Gopal Jadhav@creighton.eduhttps://novapublishers.com/shop/laser-therapies-types-uses-and-safety/
Chapter 10, p. 237-250 2020 - FEBS Openbio
Article ID: FEB412605Article DOI: 10.1002/2211-5463.12605Internal Article ID: 16393586Article: 1-Hydroxy-xanthine derivatives inhibit the human Caf1 nuclease and Caf1-containing nuclease complexes via Mg2+-dependent bindingJournal: FEBS Open BioCongratulations on the acceptance of your article for publication in FEBS Open Bio.https://doi.org/10.1002/2211-5463.12605Abstract:In eukaryotic cells, cytoplasmic mRNA is characterised by a 3’poly(A) tail. The shortening and removal of poly(A) tails(deadenylation) by the Ccr4-Not nuclease complex leads to reduced translational efficiency and RNA degradation.Using recombinant human Caf1 (CNOT7) enzyme as a screening tool, we recently described the discovery and synthesis of a series of substituted 1-hydroxy-3,7-dihydro-1H-purine-2,6-diones(1-hydroxy-xanthines) as inhibitors of the Caf1 catalytic subunit of the Ccr4-Not complex. Here, we used a chemiluminescence-based AMP detection assay to show that active 1-hydroxy-xanthines inhibit both isolated Caf1 enzyme and human Caf1-containing complexes that also contain the second nuclease subunit Ccr4(CNOT6L)to a similar extent,indicating that the active site of the Caf1 nuclease subunit does not undergo substantial conformational change when bound to other Ccr4-Not subunits. Using differential scanning fluorimetry, we also show that binding of active 1-hydroxy-xanthinesrequiresthe presence of Mg2+ions, which are present in the active site of Caf1. 2019 - Annals of Vascular Medicine & Surgery
Rai V, Jadhav GP, Boosani CS. Annals Vasc Med Surg. 2019; 2(1): 1007AbstractAtherosclerosis is a chronic inflammatory disease of the vasculature that results in hardening of the vessel wall and narrowed lumen. Development of the atherosclerotic plaque starts from the deposition of the lipids in the fatty streak followed by its progression to atheroma, atheromatous plaque, and fibroatheroma. Diabetes mellitus (hyperglycemia), hypertension, smoking, obesity (hypercholesterolemia, dyslipidemia), male sex, family history of atherosclerosis, or genetic susceptibility are the risk factors for atherosclerosis. Chronic inflammation, immune cells infiltration, a bacterial or viral infection of the plaque, intraplaque hemorrhage, and endothelial and vascular smooth muscle dys regulation renders a stable plaque (rich in VSMC and collagen with few inflammatory cells) unstable (few VSMCs, more macrophages, and less collagen) which are prone to rupture. The role of various mediators of inflammation (damage associated molecular proteins), pro inflammatory cytokines (interleukin-1β, -6, -8, tumor necrosis factor-α etc.), and surface receptors (triggering receptors expressed on myeloid cell 1, Toll-like receptors, receptor for glycation end products etc.) in the pathogenesis of plaque development and rupture has been discussed in the literature. The mechanistic aspects of plaque progression have been discussed mainly at the protein level. The epigenetic regulation of atherosclerosis is a current area of interest to researchers. However, regulation of the development, progression, and rupture of the atherosclerotic plaque at the transcriptional level has not been studied in detail. This review emphasizes the role of transcription factors associated with atherosclerotic plaque progression and rupture.http://www.remedypublications.com/annals-of-vascular-medicine/articles/pdfs_folder/avms-v2-id1007.pdf
2 (1), p. 1007 2019 - Journal of Cardiovascular Development and Disease — Open Access Journal
TREM-1; Is It a Pivotal Target for Cardiovascular Diseases?by Kouassi T. Kouassi,Palanikumar Gunasekar,Devendra K. Agrawal andGopal P. JadhavJ. Cardiovasc. Dev. Dis. 2018, 5(3), 45; https://doi.org/10.3390/jcdd5030045 (registering DOI) - 7 September 2018Abstract Cardiovascular diseases (CVDs) are as menacing as ever and still continue to kill adults worldwide, notwithstanding tremendous efforts to decrease their consequent mortality and morbidity. Lately, a growing body of research indicated that inflammation plays a pivotal role in the pathogenesis and complications of CVDs. A receptor of the immunoglobulin superfamily, triggering receptors expressed on myeloid cells-1 (TREM-1) was shown to induce and amplify the inflammation in both acute and chronic disease’ pathogenesis and progression, which hence makes it one of the most important complication factors of CVDs. Thus, studies endeavored to investigate the role played by TREM-1 in CVDs with respect to their etiologies, complications, and possible therapeutics. We examined here, for the first time, the most relevant studies regarding TREM-1 involvement in CVDs. We critically analyzed and summarized our findings and made some suggestions for furtherance of the investigations with the aim to utilize TREM-1 and its pathways for diagnostic, management, and prognosis of CVDs. Overall, TREM-1 was found to be involved in the pathogenesis of acute and chronic cardiovascular conditions, such as acute myocardial infarction (AMI) and atherosclerosis. Although most therapeutic approaches are yet to be elucidated, our present research outcome displays a promising future to utilizing the TREM-1 pathway as a potential target for understanding and managing CVDs
5 (3), p. 45 2018 - Molecules
Jitendra D. Bhosale 1,Rajesh Dabur 2,Gopal P. Jadhav 3,* andR. S. Bendre 1,* 1 School of Chemical Sciences, North Maharashtra University, Jalgaon 425001, India2 Department of Biochemistry, Maharshi Dayanand University, Rohtak 124001, India3 School of Medicine, Department of clinical & translational sciences, Creighton University, Omaha, NE 68178, USA* Authors to whom correspondence should be addressed.https://www.ncbi.nlm.nih.gov/pubmed/29641457
23 (4), p. 875 2018 - FASEB Journal
Jillian G Baker, Sheila M Gardiner, Jeanette Woolard, Christophe Fromont, Gopal P Jadhav, Shailesh Mistry, Kevin SJ Thompson, Barrie Kellam, Stephen J Hill, Peter M Fischer; Novel selective β1-adrenoceptor antagonists for concomitant cardiovascular and respiratory disease; FASEB J. 31, 000–000 (2017). www.fasebj.org
31 2017 - Journal of Medicinal Chemistry
Murray Ewan, Crowley Rebecca, Truman Alex, Clarke Simon, Cottam James, Jadhav Gopal, O'Shea Paul, Lindholm Catharina, Cockayne Alan, Chan Weng, Chhabra Siri, Williams Paul; Targeting Staphylococcus aureus Quorum Sensing with Non-Peptidic Small Molecule Inhibitors J. Med. Chem., 2014, 57 (6), pp 2813–2819
57(6), p. 2813-2819 2014 - Nucleic Acids Research
Maryati Maryati, Ishwinder Kaur, Gopal P. Jadhav, Loyin Olotu-Umoren, Blessing Oveh, Lubna Hashmi, Peter M. Fischer and G. Sebastiaan Winkler*
42(5), p. 1–10 2013 - Journal of Medicinal Chemistry
Gopal P. Jadhav, Siri Ram Chhabra, Gary Telford, Doreen S. W. Hooi, Karima Righetti, Paul Williams, Barrie Kellam, David I. Pritchard, and Peter M. Fischer ; Immunosuppressive but Non-LasR-Inducing Analogues of the Pseudomonas aeruginosa Quorum-Sensing Molecule N-(3- Oxododecanoyl)-L-homoserine Lactone ; J. Med. Chem. 2011, 54, 3348– 3359;
54, p. 3348– 3359 2011 - Indian Drugs
*Gopal P. Jadhav; Tanya Ray H. N. More; K. R. Mahadik and A. D. Deshpande; Estimation of Piroxicam beta cyclodextrin by High Performance Liquid Chromatography from marketed formulations; Indian Drugs;
36(8), p. 505-508 1999 - Indian Drugs
*Gopal P. Jadhav; Tanya Ray H. N. More; K. R. Mahadik and A. D. Deshpande; Estimation of Piroxicam beta cyclodextrin by High Performance Liquid Chromatography from marketed formulations; Indian Drugs
36(8), p. 505-508 1999 - Indian Drugs
Gopal P. Jadhav; H. N. More, K. R. Mahadik ; Simultaneous estimation of Nalidixic acid and Metronidazole using UV/Visible spectrophotometer; Indian Drugs;
35(8), p. 475-480 1998 - Indian Drugs
*A. D. Kale, S. J. Kachhwaha, Gopal P. Jadhav and Piyush Trivedi; Spectrophotometric estimation of Dicyclomine hydrochloride from combined dosage forms by ion pair complex; Indian Drugs
35(11), p. 718-720 1998 - Indian Journal of Pharmaceutical Sciences
Author(s): G. P Jadhav, H. N More, K. R MahadikA simple, rapid, economical and reproducible method has been developed for simultaneous estimation of nalidixic acid and metronidazole from pharmaceutical formulations using multicomponent mode of Jasco V-530 UV/VIS spectrophotometer. Wavelength range between 400 to 220 nm was used for estimated of both drugs. For analysis, six mixed standards were used. The results were confirmed by recovery studies and statistical evaluation. The method requires no manual calculations.http://www.ijpsonline.com/articles/simultaneous-uvspectrophotometric-estimation-of-nalidixic-acid-and-metronidazole-from-various-multicomponent-formulation.pdf
60(4), p. 246-248 1998
Editing and Reviews
- Expert Opinion on Drug Discovery
Surface Plasmon Resonance, Orbitrap mass spec and Raman advancements: Exciting new techniques in drug Discovery; Editorial (Invited)Gopal Jadhav, Pavan Prathipati, Harsh ChauhanThanks again for submitting your revised manuscript and for your time spent making the revisions. We are delighted to now accept your paper in its current form for publication in Expert Opinion On Drug Discovery. It will now be forwarded to our Production team for copy editing and typesetting. You will receive the proofs from them for checking, and instructions for transfer of copyright in due course. The publisher requests that proofs are checked and returned within 48 hours of receipt. The publisher will contact you, as part of the acceptance process, for confirmation on any colour figure requirements. 2020
Presentations
- Invited talk on " The development of selective Beta 1adrenergic receptor inhibitors for the management of Cardiovascular diseases".Venue: SGMSPM's Dnyanvilas College of Pharmacy, Pune, India.https://www.dvcop.com 2018
- Invited talk on "TREM-1 drug discovery, a pivotal target for Cardiovascular disorders"Venue: STES's Sinhgad College of Pharmacy, Pune, India.www.sinhgad.edu 2018