PUBLICATIONS & PATENTS FROM THE TRIPPIER LAB
73. Angelica V. Carmona, Shirisha Jonnalagadda, Alfie M. Case, Krishnaiah Maddeboina, Sravan K. Jonnalagadda, Louise F. Dow, Ling Duan, Trevor M. Penning and Paul C. Trippier. Discovery of an Aldo-keto reductase 1C3 (AKR1C3) degrader. Commun. Chem. 2024, 7, 95.
72. Md. Shafikur Rahman, Shiva Hadi Esfahani, Yong Zhang, Andrew Baez, Thomas J. Abbruscato, Vardan T. Karamyan and Paul C. Trippier. Imidazole-based amide bioisosteres yield activators of endopeptidase neurolysin with enhanced potency and stability. ACS Med. Chem. Lett. 2024, 15, 510-517.
71. Paul C. Trippier and Angelica V. Carmona, ‘AKR1C3 Targeted Heterobifunctional Small Molecule Proteolysis Targeting Chimeras’.
70. Paul C. Trippier, Krishnaiah Maddeboina, Sravan Jonnalagadda, ‘Inhibitors of AKR1C3 and Methods of Use’.
69. Louise F. Dow, Rasangi Pathirage, Edress Amani, Donald R. Ronning, Paul C. Trippier. Synthesis and Biological Characterization of a 17β Hydroxysteroid Dehydrogenase Type 10 (17β-HSD10) Inhibitor. ChemRxiv. 2024, Preprint, DOI: 10.26434/chemrxiv-2024-5jfcv.
68. Paul C. Trippier, Ahmed Morsy and Krishnaiah Maddeboina, ‘Functionalized Allopurinol Derivatives for Alzheimer’s Disease’.
PCT/US2023/011500
67. Yong Zhang, Sejal Sharma, Shirisha Jonnalagadda, Shikha Kumari, Aarfa Queen, Shiva Hadi Esfahani, Sabrina Rahman Archie, Saeideh Nozohouri, Dhavalkumar Patel, Paul C. Trippier, Vardan T. Karamyan and Thomas J. Abbruscato; Discovery of the next generation of non-peptidomimetic neurolysin activators with high blood-brain barrier permeability: a pharmacokinetics study in healthy and stroke animals. Pharm. Res. 2023, 40, 2747-2758.
66. Louise F. Dow, Alfie M. Case, Megan P. Paustian, Braeden R. Pinkerton, Princess Simeon and Paul C. Trippier; The evolution of small molecule enzyme activators. RSC Med. Chem. 2023, 14, 2206-2230.
65. Krishna Maddeboina, Sravan K. Jonnalagadda, Ahmed Morsy, Ling Duan, Yashpal S. Chhonker, Daryl H. Murry, Trevor M. Penning and Paul C. Trippier; Aldo-keto reductase 1C3 inhibitor prodrug improves pharmacokinetic profile and demonstrates in vivo efficacy in a prostate cancer xenograft model. J. Med. Chem. 2023, 66, 9894-9915.
64. Maria-Jesus Blanco, Amanda Bryant-Friedrich, Gunda Georg, Amjad Ali, Paul L. Ornstein, Lori Ferrins and Paul C. Trippier. Excellence in Medicinal Chemistry: Celebrating ACS Medicinal Chemistry Division (MEDI) Awards, a Call for Nominations. J. Med. Chem. 2023, 66, 7067-7969.
63. Maria-Jesus Blanco, Amanda Bryant-Friedrich, Gunda Georg, Amjad Ali, Paul L. Ornstein, Lori Ferrins and Paul C. Trippier. Excellence in medicinal chemistry: Celebrating ACS Medicinal Chemistry Division (MEDI) Awards, a call for nominations. ACS Med. Chem. Lett. 2023, 14, 682-684.
62. Siavash Nia Shahbazi, Mohammad Anwar Hossain, Guangchen Ji, Sravan K. Jonnalagadda, Samuel Obeng, Ali Ehsan Sifat, Saeideh Nozohouri, Patel Dhavalkumar, Jon Thompson, Scott Runyon, Takato Hiranita, Lance McMahon, Thomas J. Abbruscato, Paul C. Trippier, Volker Neugebauer and Nadezhda A. German; Studies on diketopiperazine and dipeptide analogs as opioid ligands. Eur. J. Med. Chem 2023, 254, 115309.
61. Bader I. Huwaimel, Sravan K. Jonnalagadda, Shirisha Jonnalagadda, Shikha Kumari, Alessio Nocentini, Claudiu T. Supuran and Paul C. Trippier; Selective carbonic anhydrase IX and XII inhibitors based around a functionalized coumarin scaffold. Drug Dev. Res. 2023, 84, 681-702.
60. Ahmed Morsy, Krishna Maddeboina, Ju Gao, Hezhen Wang, Juan Valdez, Louise F. Dow, Xinglong Wang and Paul C. Trippier; Functionalized allopurinols targeting amyloid-binding alcohol dehydrogenase rescue Abeta-induced mitochondrial dysfunction. ACS Chem. Neurosci. 2022, 13, 2176-2190.
59. Bader I. Huwaimel, Sravan Jonnalagadda, Shirisha Jonnalagadda, Fatema Zahra, Alessio Nocentini, Claudiu T. Supuran, Constantinos M. Mikelis, Paul C. Trippier; Chlorinated benzothiadiazines inhibit angiogenesis by suppression of VEGFR2 phosphorylation. Bioorg. Med. Chem. 2022, 67, 116805.
(Invited submission in honor of Richard B. Silverman’s Tetrahedron Prize for Creativity in Organic Chemistry).
58. Shiva H. Esfahani, Thomas. J. Abbruscato, Paul C. Trippier and Vardan K. Karamyan; Small Molecule Neurolysin Activators, Potential Multi-Mechanism Agents for Ischemic Stroke Therapy. Expert Opin. Ther. Targets 2022, 26, 401-404.
57. Md. Shafikur Rahman, Shiva Hadi Esfahani, Saeideh Nozohouri, Shikha Kumari, Joanna Kocot, Yong Zhang, Thomas J. Abbruscato, Vardan T. Karamyan and Paul C. Trippier; Structure-Activity Relationship Studies of Functionalized Aromatic Peptidomimetics as Neurolysin Activators. Bioorg. Med. Chem. Lett. 2022, 64, 128669.
56. Sravan Jonnalagadda, Bader I. Huwaimel, Shirisha Jonnalagadda, Jered C. Garrison and Paul C. Trippier; Access to Highly Strained Tricyclic Ketals Derived from Coumarins. J. Org. Chem. 2022, 87, 4476-4482.
55. Saeideh Nozohouri, Shiva Hadi Esfahani, Behnam Noorani, Dhaval Patel, Heidi Villalba, Yashwardhan Ghanwatkar, Md. Shafikur Rahman, Yong Zhang, Ulrich Bickel, Paul C. Trippier, Vardan T. Karamyan, and Thomas J. Abbruscato. In-Vivo and Ex-Vivo Brain Uptake Studies of Peptidomimetic Neurolysin Activators in Healthy and Stroke Animals. Pharm. Res. 2022, 39, 1587-1598.
54. Md. Ashraf-Uz-Zaman, Guangchen Ji, Dalton Tidwell, Linda Yin, Smathorn Thakolwiboon, Jie Pan, Sadisna Shahi, Md. Sanaullah Sajib, Paul C. Trippier, Constantinos Mikelis, Mirla Avila, Volker Neugebauer, and Nadezhda German; Evaluation of Urea-Based Inhibitors of Dopamine Transporter Using the Experimental Autoimmune Encephalomyelitis Model. ACS Chem. Neurosci. 2022, 13, 217-228.
53. Mariateresa Giustiniano, Christian W. Gruber, Catlin N. Kent and Paul C. Trippier; Back to the Medicinal Chemistry Future. J. Med. Chem. 2021, 64, 15515-15518.
52. Ahmed Morsy, Angelica V. Carmona and Paul C. Trippier; Patient-Derived Induced Pluripotent Stem Cell Models for Phenotypic Screening in the Neuronal Ceroid Lipofuscinoses. Molecules 2021, 26, 6235.
51. Md. Shafikur Rahman, Shikha Kumari, Shiva Hadi Esfahani, Saeideh Nozohouri, Srinidhi Jayaraman, Nihar Kinarivala, Joanna Kocot, Andrew Baez, Delaney Farris, Thomas J. Abbruscato, Vardan T. Karamyan, and Paul C. Trippier; Discovery of First-in-Class Peptidomimetic Neurolysin Activators Possessing Enhanced Brain Penetration and Stability. J. Med. Chem. 2021, 64, 12705-12722.
Cover Image
50. Srinidhi Jayaraman, Joanna Kocot, Shiva Hadi Esfahani, Naomi J. Wangler, Arzu Uyar, Yehia Mechref, Paul C. Trippier, Thomas J. Abbruscato, Alex Dickson, Hideki Aihara, David A. Ostrov, and Vardan T. Karamyan; Identification and Characterization of Two Structurally Related Dipeptides that Enhance Catalytic Efficiency of Neurolysin. J. Pharmacol. Exp. Ther. 2021, 379, 191-202.
49. Sravan Jonnalagadda, Bader I. Huwaimel, Shirisha Jonnalagadda, Jered C. Garrison, and Paul C. Trippier; Expedient Single Step Access to Strained Tricyclic Ketals.
Preprint on ChemRxiv. DOI: 10.33774/chemrxiv-2021-574sw.
48. Trevor M. Penning, Sravan Jonnalagadda, Paul C. Trippier and Tea Lanišnik Rižner; Aldo-Keto Reductases and Cancer Drug Resistance. Pharmacol. Rev. 2021, 73, 1150-1171.
47. Bader I. Huwaimel, Myla Bhakta, Chaitanya A. Kulkarni, Alexander S. Milliken, Feifei Wang, Aimin Peng, Paul S. Brookes and Paul C. Trippier; Discovery of Halogenated Benzothiadiazine Derivatives with Anticancer Activity.
ChemMedChem 2021, 16, 1143-1162.
Preprint on ChemRxiv. DOI: 10.26434/chemrxiv.12350912.v2.
46. Joelle Makoukji, Sara Saab, Katia Maalouf, Nadine J. Makhoul, Angelica V. Carmona, Nihar Kinarivala, Paul C. Trippier and Rose-Mary Boustany; Sex-Specific Gene Expression in Flupirtine-Treated Cln3?ex7/8 Mouse Brain. Biochem. Pharmacol. 2021, 10, 272.
45. Md Ashraf-Uz-Zaman, Sadisna Shahi, Racheal Aikwii, Md Sanaullah Sajib, Mohammad Jodeiri Farshbaf, Raja Reddy Kallem, William Putnam, Wei Wang, Ruiwen Zhang, Karina Alvina, Paul C. Trippier, Constantinos M. Mikelis and Nadezhda A. German. Design, Synthesis and Structure-Activity Relationship Study of Novel Urea Compounds as FGFR1 inhibitors to Treat Metastatic Triple-Negative Breast Cancer. Eur. J. Med. Chem. 2021, 209, 112866.
44. Katia Maalouf, Joelle Makoukji, Sara Saab, Nadine J. Makhoul, Angelica V. Carmona, Nihar Kinarivala, Noel Ghanem, Paul C. Trippier and Rose-Mary Boustany. Exogenous Flupirtine as Potential Treatment of CLN3 Disease. Cells 2020, 9, 1872. DOI: 10.3390/cells9081872.
43. Shikha Kumari, Angelica V. Carmona, Amit K. Tiwari and Paul C. Trippier; Amide Bond Bioisosteres: Strategies, Synthesis and Successes. J. Med. Chem. 2020, 63, 12290-12358.
42. Paul C. Trippier and Bader Huwaimel; ”Halogenated Benzothiadiazines for the Treatment of Cancer’
PCT Int. Appl. (2021), WO 236818 A1
41. Paul C. Trippier; The Current State of Drug Repurposing and Rare Diseases: An Interview with Paul Trippier. Future Drug. Discov. 2020, 2, FDD30.
40. Ahmed Morsy and Paul C. Trippier; Reversal of Apalutamide and Darolutamide Aldo-Keto Reductase 1C3-Mediated Resistance by a Small Molecule Inhibitor. ACS Chem. Biol. 2020, 15, 646-650.
39. Vardan T. Karamyan, Paul C. Trippier, David A. Ostrov, Tom Abbruscato and Srinidhi Jayaraman; ”Enhancers of Neurolysin Activity’
U. S. Patent Appl. US 62/725444, 20189.
PCT Int. Appl. (2020), WO 2020047185
38. Nihar Kinarivala, Ahmed Morsy, Ronak Patel, Angelica V. Carmona, Md. Sanaullah Sajib, Snehal Raut, Constantinos M. Mikelis, Abraham Al-Ahmad, Paul C. Trippier; An iPSC-Derived Neuron Model of CLN3 Disease Facilitates Small Molecule Phenotypic Screening.
ACS Pharmacol. Transl. Sci. 2020, 3, 931-947.
Preprint on ChemRxiv. DOI: 10.26434/chemrxiv.11493132.
37. Paul C. Trippier and Paul S. Brookes; ‘Method of Treating Cancer with Atpenin A5 Derivatives’
U. S. Patent Appl. US 62/670479, 2018?.
PCT Int. Appl. (2019), WO 2019217631
36. Ahmed Morsy and Paul C. Trippier; Current and Emerging Pharmacological Targets for the Treatment of Alzheimer’s Disease. J. Alzheimers Dis. 2019, 72, S145-S176.
35. Ahmed Morsy and Paul C. Trippier; Amyloid-Binding Alcohol Dehydrogenase (ABAD) Inhibitors for the Treatment of Alzheimer’s Disease. J. Med. Chem. 2019, 62, 4252-4264.
34. Kshitij Verma, Tianzhu Zang, Trevor M. Penning and Paul C. Trippier; Potent and Highly Selective Aldo-Keto Reductase 1C3 (AKR1C3) Inhibitors Act as Chemotherapeutic Potentiators in Acute Myeloid Leukemia and T-Cell Acute Lymphoblastic Leukemia. J. Med. Chem. 2019, 62, 3590-3616.
33. Paul C. Trippier, Nihar Kinarivala and Rose-Mary Boustany; ‘Functionalized Pyridine Carbamates with Enhanced Neuroprotective Activity’
U. S. Patent Appl. US 62/532624, 2017.
PCT Int. Appl. (2019), WO 2019014547.
United States Patent 11,369,593.
32. Joelle Makoukji, Fadi Saadeh, Karl Albert Mansour, Sally El-Sitt, Jamal Al Ali, Nihar Kinarivala, Paul C. Trippier and Rose-Mary Boustany; Flupirtine Derivatives as Potential Treatment for the Neuronal Ceroid Lipofuscinoses. Ann. Clin. Transl. Neurol. 2018, 5, 1089-1103.
Clearer structures for Figure 1A
31. Kshitij Verma, Nehal Gupta, Tianzhu Zang, Phumvadee Wangtrakuldee, Sanjay K. Srivastava, Trevor M. Penning and Paul C. Trippier; AKR1C3 Inhibitor KV-37 Exhibits Antineoplastic Effects and Potentiates Enzalutamide in Combination Therapy in Prostate Adenocarcinoma Cells. Mol. Cancer Ther. 2018?, 17, 1833-1845.
30. Paul C. Trippier; Molecule of the Month: Relating Organic Chemistry Principles to Drug Action. J. Chem. Educ. 2018, 95?, 1112-1117.
29. Thomas J. Abbruscato and Paul C. Trippier; DARK Classics in Chemical Neuroscience: Methamphetamine. ACS Chem. Neurosci. 2018, 9, 2373-2378.
28. Paul C. Trippier, Kshitij Verma, Tianzhu Zang and Trevor M. Penning; ‘Highly selective AKR1C3 inhibitors and methods of use thereof’
U. S. Patent Appl. US 62/458267, 2017.
?PCT Int. Appl. (2018) WO 2018148721
27. Nihar Kinarivala, Ronak Patel, Rose-Mary Boustany, Abraham J. Al-Ahmad and Paul C. Trippier; Discovery of Aromatic Carbamates that Confer Neuroprotective Activity by Enhancing Autophagy and Inducing the Anti-Apoptotic Protein B-cell lymphoma 2 (BCL-2). J. Med. Chem. 2017, 60?, 9739-9756.
26. Paul C. Trippier; Small Molecule Inhibitors for Acute Myeloid Leukemia: Where is the Field Heading? Future Med. Chem. 2017, 9?, 1453-1456.
25. Hezhen Wang, Bader Huwaimel, Kshitij Verma, James Miller, Todd Germain, Nihar Kinarivala, Dimitri Pappas, Paul S. Brookes and Paul C. Trippier; Synthesis and Antineoplastic Evaluation of Mitochondrial Complex II (Succinate Dehydrogenase) Inhibitors Derived from Atpenin A5. ChemMedChem 2017, 12, 1033-1044.
- Highlighted in the MedChem in the USA virtual issue (Link)
24. Nihar Kinarivala, Kaushik Shah, Thomas J. Abbruscato and Paul C. Trippier; Passage Variation of PC12 Cells Results in Inconsistent Susceptibility to Externally Induced Apoptosis. ACS Chem. Neurosci. 2017, 8, 82-88.
23. Kshitij Verma, Tianzhu Zang, Nehal Gupta, Trevor M. Penning and Paul C. Trippier; Selective AKR1C3 Inhibitors Potentiate Chemotherapeutic Activity in Multiple Acute Myeloid Leukemia (AML) Cell Lines. ACS Med. Chem. Lett. 2016, 7?, 774-779.
22. Paul C. Trippier; Selecting Good ‘Drug-Like’ Properties to Optimize Small Molecule Blood-Brain Barrier Penetration. ?Curr. Med. Chem. 2016, 23, 1392-1407.
21. Nihar Kinarivala and Paul C. Trippier; Progress in the Development of Small Molecule Therapeutics for the Treatment of Neuronal Ceroid Lipofuscinoses (NCLs). J. Med. Chem. 2016, 59,? 4415-4427.
20. Nihar Kinarivala, Ji Ho Suh, Mina Botros, Paul Webb and Paul C. Trippier; Pharmacophore Elucidation of Phosphoiodyn A – Potent and Selective Peroxisome Proliferator-Activated Receptor ß/d Agonists with Neuroprotective Activity. ?Bioorg. Med. Chem. Lett. 2016, 26, 1889-1893.
19. Paul C. Trippier and Paul Webb; ‘Potent and selective peroxisome proliferator-activated receptor beta/delta agonists’
U. S. Patent Appl. US 62/422797, 2016.
17. Paul C. Trippier, Hezhen Wang and Paul S. Brookes; Mitochondrial Complex II Inhibitors / mKATP Activators: Chemical Tools to Probe the Mitochondria and a New Target for Anticancer Drug Discovery. Assay Drug Dev. Technol. 2015, 13, 138-139.
16. Tianzhu Zang, Kshitij Verma, Mo Chen, Yi Jin, Paul C. Trippier and Trevor M. Penning; Screening Baccharin Analogs as Selective Inhibitors Against Type 5 17ß-hydroxysteroid Dehydrogenase (AKR1C3). Chem. Biol. Interact. 2015, 234, 339-348.
15. Nihar Kinarivala, and Paul C. Trippier; Exploration of Relative Chemoselectivity in the Hydrodechlorination of 2-Chloropyridines.
Tetrahedron Lett. 2014, 55, 5386-5389.
14. Paul C. Trippier; Synthetic Strategies for the Biotinylation of Bioactive Small Molecules. ChemMedChem, 2013, 8, 190-203.
Highlighted in: ChemInform 2013, 44, DOI: 10.1002/chin.201315272
PUBLICATIONS FROM GRADUATE AND POSTDOCTORAL WORK
13. Paul C. Trippier, Kevin Tianmeng Zhao, Susan G. Fox, Isaac T. Schiefer, Radhia Benmohamed, Jason Moran, Donald R. Kirsch, Richard I. Morimoto, and Richard B. Silverman; Proteasome activation is a mechanism of pyrazolone small molecules displaying therapeutic potential in Amyotrophic Lateral Sclerosis. ACS Chem. Neurosci. 2014, 5, 823-829.
12. Paul C. Trippier, Kristin J. Labby, Dustin D. Hawker, Jan Mataka, and Richard B. Silverman; Target- and Mechanism-Based Therapeutics for Neurodegenerative Diseases: Strength in Numbers. J. Med. Chem. 2013, 56, 3121-3147.
11. Paul C. Trippier, Radhia Benmohammed, Donald R. Kirsch, and Richard B. Silverman; Substituted pyrazolones require N2 hydrogen bond donating ability to protect against cytotoxicity from protein aggregation of mutant superoxide dismutase 1. Bioorg. Med. Chem. Lett. 2012, 22, 6647-6650.
10. Plamen Angelov, Sonia Chau, Paul J. Fryer, Mark G. Moloney and Paul C. Trippier; Biomimetic synthesis, antibacterial activity and structure activity properties of the pyroglutamate core of oxazolomycin. Org. Biomol. Chem. 2012, 10, 3472-3485.
9. Paul C. Trippier; “Bis(cyclopentadienyl)dimethyltitanium – second update” in e-EROS Encyclopedia of Reagents for Organic Synthesis. 2012, Eds: Crich, D.; Charette, A. B.; Fuchs, P. L.; Rovis, T. John Wiley & Sons Ltd. Chichester, UK.
8. Lada Klaic, Paul C. Trippier, Rama K. Mishra, Richard I. Morimoto and Richard B. Silverman; Remarkable stereoselective conjugate additions to the Hsp90 inhibitor Celastrol. J. Am. Chem. Soc. 2011, 133, 19634-19637.
7. Paul C. Trippier, Christopher McGuigan and Jan Balzerini; Phenylboronic acid-based carbohydrate binders as antiviral therapeutics: bisphenylboronic acids. Antiviral Chem. Chemother. 2011, 21, 129-142.
6. Paul C. Trippier and Christopher McGuigan; Boronic acids in medicinal chemistry: anticancer, antibacterial and antiviral applications. Med. Chem. Commun. 2010, 1, 183-198.
5. Paul C. Trippier, Christopher McGuigan and Jan Balzerini; Phenylboronic acid-based carbohydrate binders as antiviral therapeutics: monophenylboronic acids. Antiviral Chem. Chemother. 2010, 20, 249-257.
4. Paul C. Trippier; Synthesis of Highly Substituted Heterocycles – the oxazolomycins. D.Phil. Thesis, 2007, University of Oxford, UK.
3. Mark G. Moloney, Paul C. Trippier, Muhammad Yaqoob and Zhaoyang Wang; The Oxazolomycins: A Structurally Novel Class of Bioactive Compounds. Curr. Drug Discovery Technol. 2004, 1, 181-199.
2. Paul G. Bulger, Mark G. Moloney and Paul C. Trippier; A multi-component coupling suitable for the synthesis of the triene component of the oxazolomycin antibiotics. Org. Biomol. Chem. 2003, 1, 3726-3737.
1. Paul G. Bulger, Mark G. Moloney and Paul C. Trippier; Strategies for the synthesis of the triene component of the oxazolomycin antibiotics. Synlett, 2002, 11, 1871-1873.
ARTICLES ABOUT OUR RESEARCH
A barrier to progress: getting drugs to the brain. 2017 The Pharmaceutical Journal, Vol 298, No 7901, online. DOI: 10.1211/PJ.2017.20202723
