Aldo-Keto Reductase 1C3 Inhibitor Prodrug Improves Pharmacokinetic Profile and Demonstrates In Vivo Efficacy in a Prostate Cancer Xenograft Model

Authors: Maddeboina, Krishnaiah, Jonnalagadda, Sravan K., Morsy, Ahmed, Duan, Ling, Chhonker, Yashpal S., Murry, Daryl J., Penning, Trevor M., Trippier, Paul C.

Source: Journal of medicinal chemistry. 66(14):9894-9915

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Selective carbonic anhydrase IX and XII inhibitors based around a functionalized coumarin scaffold

Authors: Huwaimel, Bader I., Jonnalagadda, Sravan K., Jonnalagadda, Shirisha, Kumari, Shikha, Nocentini, Alessio, Supuran, Claudiu T., Trippier, Paul C.

Source: Drug development research. 84(4):681-702

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100184991977.0x000001&indx=1&recIds=ETOCvdc_100184991977.0x000001

Studies on diketopiperazine and dipeptide analogs as opioid receptor ligands

Authors: Shahbazi Nia, Siavash, Hossain, Mohammad Anwar, Ji, Guangchen, Jonnalagadda, Sravan K., Obeng, Samuel, Rahman, Md Ashrafur, Sifat, Ali Ehsan, Nozohouri, Saeideh, Blackwell, Collin, Patel, Dhavalkumar, Thompson, Jon, Runyon, Scott, Hiranita, Takato, McCurdy, Christopher R., McMahon, Lance, Abbruscato, Thomas J., Trippier, Paul C., Neugebauer, Volker, German, Nadezhda A.

Source: In European Journal of Medicinal Chemistry 5 June 2023 254

Pivotal role of nitrogen heterocycles in Alzheimer’s disease drug discovery

Authors: Kumari, Shikha, Maddeboina, Krishnaiah, Bachu, Rinda Devi, Boddu, Sai H.S., Trippier, Paul C., Tiwari, Amit K.

Source: In Drug Discovery Today October 2022 27(10)

Small molecule neurolysin activators, potential multi-mechanism agents for ischemic stroke therapy

Authors: Esfahani, Shiva Hadi, Abbruscato, Thomas J., Trippier, Paul C., Karamyan, Vardan T.

Source: Expert opinion on therapeutic targets. 26(5):401-404

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Chlorinated benzothiadiazines inhibit angiogenesis through suppression of VEGFR2 phosphorylation

Authors: Huwaimel, Bader I., Jonnalagadda, Sravan, Jonnalagadda, Shirisha, Zahra, Fatema T., Nocentini, Alessio, Supuran, Claudiu T., Mikelis, Constantinos M., Trippier, Paul C.

Source: In Bioorganic & Medicinal Chemistry 1 August 2022 67

Synthesis and biological characterization of a 17β hydroxysteroid dehydrogenase type 10 (17β-HSD10) inhibitor.

Authors: Dow, Louise F., Pathirage, Rasangi, Erickson, Helen E., Amani, Edrees, Ronning, Donald R., Trippier, Paul C.

Source: RSC Medicinal Chemistry; Feb2025, Vol. 16 Issue 2, p862-875, 14p

Identification and Characterization of Two Structurally Related Dipeptides that Enhance Catalytic Efficiency of Neurolysin

Authors: Jayaraman, Srinidhi ¹, Kocot, Joanna ¹, Esfahani, Shiva Hadi ¹, Wangler, Naomi J., Uyar, Arzu, Mechref, Yehia, Trippier, Paul C., Abbruscato, Thomas J., Dickson, Alex, Aihara, Hideki, Ostrov, David A., Karamyan, Vardan T. ^*

Source: In The Journal of Pharmacology and Experimental Therapeutics November 2021 379(2):191-202

Aldo-Keto Reductases and Cancer Drug Resistance

Authors: Penning, Trevor M. ^*, Jonnalagadda, Sravan, Trippier, Paul C., Rižner, Tea Lanišnik

Source: In Pharmacological Reviews July 2021 73(3):1150-1171

Design, synthesis and structure-activity relationship study of novel urea compounds as FGFR1 inhibitors to treat metastatic triple-negative breast cancer

Authors: Ashraf-Uz-Zaman, Md, Shahi, Sadisna, Akwii, Racheal, Sajib, Md Sanaullah, Farshbaf, Mohammad Jodeiri, Kallem, Raja Reddy, Putnam, William, Wang, Wei, Zhang, Ruiwen, Alvina, Karina, Trippier, Paul C., Mikelis, Constantinos M., German, Nadezhda A.

Source: In European Journal of Medicinal Chemistry 1 January 2021 209

Discovery of Halogenated Benzothiadiazine Derivatives with Anticancer Activity**

Authors: Huwaimel, Bader I., Bhakta, Myla, Kulkarni, Chaitanya A., Milliken, Alexander S., Wang, Feifei, Peng, Aimin, Brookes, Paul S., Trippier, Paul C.

Source: ChemMedChem. 16(7):1143-1162

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Coumarin‐Based Aldo‐Keto Reductase Family 1C (AKR1C) 2 and 3 Inhibitors.

Authors: Jonnalagadda, Sravan K., Duan, Ling, Dow, Louise F., Boligala, Geetha P, Kosmacek, Elizabeth, McCoy, Kristyn, Oberley‐Deegan, Rebecca, Chhonker, Yashpal Singh, Murry, Darryl J., Reynolds, C. Patrick, Maurer, Barry J., Penning, Trevor M., Trippier, Paul C.

Source: ChemMedChem; 11/4/2024, Vol. 19 Issue 21, p1-19, 19p

Molecule of the Month: Relating Organic Chemistry Principles to Drug Action

Authors: Trippier, Paul C. (ORCID 0000-0002-4947-5782)

Source: Journal of Chemical Education. Jul 2018 95(7):1112-1117.

Peer Reviewed: Y

Page Count: 6

Descriptors: Molecular Structure, Pharmacology, Pharmacy, Interdisciplinary Approach, Organic Chemistry, Scores, Standardized Tests, Student Participation, Grades (Scholastic), Educational Technology, Technology Uses in Education

Geographic Terms: Texas

Reversal of Apalutamide and Darolutamide Aldo-Keto Reductase 1C3-Mediated Resistance by a Small Molecule Inhibitor

Authors: Morsy, Ahmed, Trippier, Paul C.

Source: ACS chemical biology. 15(3):646-650

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In vitro ADME, mouse pharmacokinetics of LD14b, and bioanalysis of a novel aβ 17β-HSD10 modulator for the treatment of Alzheimer's disease.

Authors: Daria, Sohel, Kumar, Devendra, Gautam, Nagsen, Alamoudi, Jawaher Abdullah, Dow, Louise F., Trippier, Paul C., Alnouti, Yazen

Source: Xenobiotica; Sep2024, Vol. 54 Issue 9, p711-722, 12p

Subject Terms: BLOOD proteins, ALZHEIMER'S disease, PROTEIN-protein interactions, PROTEIN binding, PROTEIN stability, LUNGS

Structure-activity relationship studies of functionalized aromatic peptidomimetics as neurolysin activators

Authors: Rahman, Md. Shafikur, Esfahani, Shiva Hadi, Nozohouri, Saeideh, Kumari, Shikha, Kocot, Joanna, Zhang, Yong, Abbruscato, Thomas J., Karamyan, Vardan T., Trippier, Paul C.

Source: Bioorganic & medicinal chemistry letters. 64

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Imidazole Bioisostere Activators of Endopeptidase Neurolysin with Enhanced Potency and Metabolic Stability.

Authors: Rahman, Md. Shafikur, Hadi Esfahani, Shiva, Zhang, Yong, Queen, Aarfa, Aljarrah, Manar, Kandil, Haya, Baez, Andrew, Abbruscato, Thomas J., Karamyan, Vardan T., Trippier, Paul C.

Source: ACS Medicinal Chemistry Letters; 4/11/2024, Vol. 15 Issue 4, p510-517, 8p

Flupirtine derivatives as potential treatment for the neuronal ceroid lipofuscinoses

Authors: Makoukji, Joelle, Saadeh, Fadi, Mansour, Karl Albert, El‐Sitt, Sally, Al Ali, Jamal, Kinarivala, Nihar, Trippier, Paul C., Boustany, Rose‐Mary

Source: Annals of clinical and translational neurology. 5(9):1089-1103

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100083901143.0x000001&indx=1&recIds=ETOCvdc_100083901143.0x000001

Screening baccharin analogs as selective inhibitors against type 5 17β-hydroxysteroid dehydrogenase (AKR1C3)

Authors: Zang, Tianzhu, Verma, Kshitij, Chen, Mo, Jin, Yi, Trippier, Paul C., Penning, Trevor M.

Source: In Chemico-Biological Interactions 5 June 2015 234:339-348

Small molecule inhibitors for acute myeloid leukemia: where is the field heading?

Authors: Trippier, Paul C

Source: Future medicinal chemistry. 9(13):1453-1456

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100121092641.0x000001&indx=1&recIds=ETOCvdc_100121092641.0x000001