Publications
2026
4-Anilinoquinazoline carbamate derivatization as a platform for prodrug design and localized drug delivery Link
Bioorganic Chemistry 2026, 178, 109912
Mabel Barreiro Carpio, Coleman D. Walker, Audrey Fikes, Tuomo Laitinen, M. Alejandro Valdes-Pena, Osman Gani, Micah Mallory, Christopher R. M. Asquith,* Yevgeny Brudno,* Joshua G. Pierce*
PIP4K2C: an emerging fulcrum for multiple diseases Link
Nature Reviews Drug Discovery 2026, 25, (3) 166
Luca Pozzetti, Manjari Mishra, Shirit Einav, Christopher R. M. Asquith*
2025
Myeloid-specific CAMKK2 deficiency protects against diet-induced obesity and insulin resistance by rewiring metabolic gene expression and enhancing energy expenditure Link
Molecular Metabolism 2025, 101, 102250
Andrea R. Ortiz , Kevin Nay, Brittany A. Stork, Adam M. Dean, Sean M. Hartig, Cristian Coarfa, Surafel Tegegne, Christopher R. M. Asquith, Daniel E. Frigo , Brian York, Anthony R. Means, Mark A. Febbraio, John W. Scott*
PIP4K2C inhibition reverses autophagic flux impairment induced by SARS-CoV-2 Link
Nature Communications 2025, 16, (1), 6397
Marwah Karim, Manjari Mishra, Chieh-Wen Lo, Sirle Saul, Halise Busra Cagirici, Manon Gourdelier, Luca Ghita, Amrita Ojha, Do Hoang Nhu Tran, Aditi Agrawal,…,Christopher R. M. Asquith, Shirit Einav*
Medicinal chemistry applications of the Dimroth Rearrangement to the synthesis of biologically active compounds Link
European Journal of Medicinal Chemistry 2025, 289, 117399
Luca Pozzetti, Maja M. Pinhammer, Christopher R. M. Asquith*
2024
Pentathiepins are an understudied molecular prism of biological activities Link
Archiv Der Pharmazie 2024, 357, (12), 2400646
Luca Pozzetti, Christopher R. M. Asquith*
TLK2: a target for cancer and viral latency Link
Nature Reviews Drug Discovery 2024, 23, (12), 886
Luca Pozzetti, Michael P. East, Tuomo Laitinen, Christopher R. M. Asquith*
Enhancing colistin efficacy against Salmonella infections with a quinazoline-based dual therapeutic strategy Link
Scintific Reports 2024, 14, 5148
Carlos A. Lobertti, Fernán O. Gizzi, Christian Magni, Analía Rial, José A. Chabalgoity, Lucía Yim, Víctor S. Blancato, Christopher R. M. Asquith, Eleonora García Véscovi*
Discovery and optimization of narrow spectrum inhibitors of Tousled like kinase 2 (TLK2) using quantitative structure activity relationships Link
European Journal of Medicinal Chemistry 2024, 271, 116357
Christopher R. M. Asquith,* Michael P. East, Tuomo Laitinen, Carla Alamillo-Ferrer, Erkka Hartikainen, Carrow I. Wells, Alison D. Axtman, David H. Drewry, Graham J. Tizzard, Antti Poso, Timothy M. Willson, Gary L. Johnson*
2023
The synthesis and biological applications of the 1,2,3-dithiazole scaffold Link
Molecules 2023, 28, (7), 3193
Andreas S. Kalogirou, Hans J. Oh Christopher R. M. Asquith*
Utilization of Supervised Machine Learning to Understand Kinase Inhibitor Toxophore Profiles Link
International Journal of Molecular Sciences 2023, 24, (6), 5088
Andrew A. Bieberich, Christopher R. M. Asquith*
Small-molecule inhibition of the archetypal UbiB protein COQ8 Link
Nature Chemical Biology 2023, 19, (2), 230-238
Nathan H. Murray, Christopher R. M. Asquith, Zixiang Fang, Michael P. East, Naomi Ptak, Robert W. Smith, James D. Vasta, Chad A. Zimprich, Cesear R. Corona, Matthew B. Robers, Gary L. Johnson, Craig A. Bingman & David J. Pagliarini*
2022
PKN3: a regulator of angiogenesis and metastasis Link
Nature Reviews Drug Discovery 2022, 21, (10), 70466
Louisa Temme,* Tuomo Laitinen & Christopher R. M. Asquith*
Optimization of structural features of the 4-anilinoquinazoline based epidermal growth factor receptor (EGFR) inhibitors for chordoma utilizing a toxicology profiling assay platform Link
Scientific Reports 2022, 12, (1), 12820
Andrew A. Bieberich, Tuomo Laitinen, Kaitlyn Maffuid, Raymond O. Fatig III, Chad D. Torrice, David C. Morris, Daniel J. Crona & Christopher R. M. Asquith*
Numb-associated kinases are required for SARS-CoV-2 infection and are cellular targets for antiviral strategies Link
Antiviral Research 2022, 204, 105367
Marwah Karim, Sirle Saul, Luca Ghita, Malaya Kumar Sahoo, Chengjin Ye, Nishank Bhalla, Chieh-Wen Lo, Jing Jin, Jun-Gyu Park, Belén Martinez-Gualda, Michael P. East, Gary L. Johnson, Benjamin A. Pinsky, Luis Martinez-Sobrido , Christopher R. M. Asquith, Aarthi Narayanan, Steven De Jonghe, Shirit Einav*
Synthesis and evaluation of 1,2,3-dithiazole inhibitors of the nucleocapsid protein of feline immunodeficiency virus (FIV) as a model for HIV infection Link
Bioorganic & Medicinal Chemistry 2022, 68, 116834
Tuomo Laitinen, Theres Meili, Maria Koyioni, Panayiotis A. Koutentis, Antti Poso, Regina Hofmann-Lehmann, Christopher R. M. Asquith*
Small Molecule Modulation of the Atypical Kinase/ATPase COQ8A Link
Federation of American Societies for Experimental Biology 2022, 361, R3719
Nathan Murray, Adam Lewis, Christopher R. M. Asquith, Juan Rincon Pabon, Zixiang Fang, Naomi Ptak, Robert Smith, Craig Bingman, Michael Gross, Katherine Henzler-Wildman, David Pagliarini*
Identification of 4-Anilinoquin(az)oline as a Cell-Active Protein Kinase Novel 3 (PKN3) Inhibitor Chemotype Link
ChemMedChem 2022, 17, (12), e202200161
Christopher R. M. Asquith,* Louisa Temme, Michael P. East, Tuomo Laitinen, Julie Pickett, Frank E. Kwarcinski, Parvathi Sinha, Carrow I. Wells, Gary L. Johnson, Reena Zutshi, David H. Drewry*
2021
Optimization of potent 4-anilinoquinoline dengue virus inhibitors Link
Molecules 2021, 26, (23), 7338
Pei-Tzu Huang, Sirle Saul, Shirit Einav,* Christopher R. M. Asquith*
Synthesis and evaluation of novel 1,2,6-thiadiazinones as kinase inhibitors of solid tumors Link
Molecules 2021, 26, (19), 5911
Andreas S. Kalogirou,* Michael P. East, Tuomo Laitinen, Chad D. Torrice, Kaitlyn A. Maffuid, David H. Drewry, Panayiotis A. Koutentis, Gary L. Johnson, Daniel J. Crona, Christopher R. M. Asquith*
Identification and evaluation of 4-anilinoquin(az)olines as potent inhibitors of both of Venezuelan equine encephalitis virus (VEEV) and dengue virus (DENV) Link
Bioorganic & Medicinal Chemistry Letters 2021, 52, 128407
Sirle Saul, Pei-Tzu Huang, Shirit Einav,* Christopher R. M. Asquith*
PIKfyve: a lipid kinase target for COVID-19, cancer and neurodegenerative disorders Link
Nature Reviews Drug Discovery 2021, 20, (10), 730
Pei-Tzu Huang, Shirit Einav, Christopher R. M. Asquith*
Hinge Binder Scaffold Hopping Identifies Potent Calcium/Calmodulin-Dependent Protein Kinase Kinase 2 (CAMKK2) Inhibitor Chemotypes Link
Journal of Medicinal Chemistry 2021, 64, (15), 10849
Benjamin J. Eduful, Sean N. O’Byrne, Louisa Temme, Christopher R. M. Asquith, Yi Liang, Alfredo Picado, Joseph R. Pilotte..., Timothy M. Willson, Daniel E. Frigo, John W. Scott,* David H. Drewry*
eEF2K: an atypical kinase target for cancer Link
Nature Reviews Drug Discovery 2021, 20, (8), 577
Louisa Temme* & Christopher R. M. Asquith*
BCKDK: an emerging kinase target for metabolic diseases and cancer Link
Nature Reviews Drug Discovery 2021, 20, (7), 498
Michael P. East, Tuomo Laitinen, Christopher R. M. Asquith*
Design and evaluation of 1,2,3-dithiazoles and fused 1,2,4-dithiazines as anti-cancer agents Link
Bioorganic & Medicinal Chemistry Letters 2021, 43, 128078
Kaitlyn A. Maffuid, Maria Koyioni, Chad D. Torrice, William A. Murphy, Heemaja K. Mewada, Panayiotis A. Koutentis, Daniel J. Crona, Christopher R. M. Asquith*
CDC42BPA: A new therapeutic target for high-grade serous ovarian carcinoma and skin cancer Link
Nature Reviews Drug Discovery 2021, 20, (3), 167
Michael P. East, Christopher R. M. Asquith*
The Kinase Chemogenomic Set (KCGS): An open science resource for kinase vulnerability identification Link
International Journal of Molecular Sciences 2021, 22, (2), 566
Carrow I. Wells, Hassan Al-Ali, David M. Andrews, Christopher R. M. Asquith, Alison D. Axtman, Ivan Dikic, Daniel Ebner, Peter Ettmayer, Christian Fischer …, David H. Drewry*
2020
WNK kinases: an untapped opportunity to modulate ion transport Link
Nature Reviews Drug Discovery 2020, 19, (12), 828
Michael P. East, Tuomo Laitinen, Christopher R. M. Asquith*
6-Bromo-N-(3-(difluoromethyl)phenyl)quinolin-4-amine Link
Molbank 2020, 2020, (4), M1161
Christopher R. M. Asquith* & Graham J. Tizzard
Antimicrobial and Antifungal Activity of Rare Substituted 1,2,3-Thiaselenazoles and Corresponding Matched Pair 1,2,3-Dithiazoles Link
Antibiotics (Basel) 2020, 9, (7), 369
Tuomo Laitinen, Ilia V. Baranovsky, Lidia S. Konstantinova, Antti Poso, Oleg A. Rakitin, Christopher R. M. Asquith*
STK19: a new target for NRAS-driven cancer Link
Nature Reviews Drug Discovery 2020, 19, (9) 579
Christopher R. M. Asquith,* Louisa Temme*
Potent antiviral activity of novel multi-substituted 4-anilinoquin(az)olines Link
Bioorganic & Medicinal Chemistry Letters 2020, 30, (16), 127284
Sirle Saul, Szu-Yuan Pu, William J. Zuercher, Shirit Einav,* Christopher R. M. Asquith*
Synthesis of (R) and (S)-3-Chloro-5-(2,4-dimethylpiperazin-1-yl)-4H-1,2,6-thiadiazin-4-ones Link
Molbank 2020, 2020, (2), M1139
Andreas S. Kalogirou,* Christopher R. M. Asquith, Panayiotis A. Koutentis
Targeting the water network in cyclin G associated kinase (GAK) with 4-anilino-quin(az)oline inhibitors Link
ChemMedChem 2020, 15, (13), 1200-1215
Christopher R. M. Asquith,* Graham J. Tizzard, James M. Bennett, Carrow I. Wells, Jonathan M. Elkins, Prof. Timothy M. Willson, Antti Poso, Tuomo Laitinen
Synthesis of (R) and (S)-3-Chloro-5-(3-methylmorpholino)-4H-1,2,6-thiadiazin-4-ones Link
Molbank 2020, 2020, (2), M1128
Andreas S. Kalogirou,* Christopher R. M. Asquith, Panayiotis A. Koutentis
PIP5K1A: a potential target for cancers with mutations in KRAS or p53 Link
Nature Reviews Drug Discovery 2020, 19, (7), 436
Michael P. East, Tuomo Laitinen, Christopher R. M. Asquith*
New insights into 4-anilinoquinazolines as inhibitors of cardiac troponin I–interacting kinase (TNNi3K) Link
Molecules 2020, 25, (7), 1697
Christopher R. M. Asquith,* Tuomo Laitinen, Carrow I. Wells, Graham J. Tizzard, William J. Zuercher
PKMYT1: forgotten member of the Wee1 family Link
Nature Reviews Drug Discovery 2020, 19, (3), 157
Christopher R. M. Asquith, Tuomo Laitinen, Michael P. East*
Design and Analysis of the 4-Anilinoquin(az)oline Kinase Inhibition Profiles of GAK/SLK/STK10 Using Quantitative Structure-Activity Relationships Link
ChemMedChem 2020, 15, (1), 26
Christopher R. M. Asquith,* Tuomo Laitinen, James M. Bennett, Carrow I. Wells, Jonathan M. Elkins, William J. Zuercher, Graham J. Tizzard, Antti Poso