Complete list of Publications on PubMed can be found here.
Journal Articles
86.
Jiang X, Lynch EM, Lyu C, Wilson CN, Salay LE, Hess HT, Lyons SN, Lu MJ, Luo S, Kim G, Chan HR, Wolfe WJ, Zacharias LG, Mathews TP, Lin YC, Webb BA, Kollman JM, Cambronne XA, Hsu KL. A covalent PFKL activator suppresses tumor growth. Nat Chem Biol. 2026. [online ahead of print]
85.
Li Z, Tsai HK, Libby AH, Founds MW, Murtagh OL, Ware ML, Leace DM, Wolfe WJ, Gingrich PW, Al-Lazikani B, Chang CY, Hsu KL. A chemoproteomic atlas of the human purine interactome for regioselective ligand discovery Nature Communications. 2026; 17(1).
84.
Murtagh O, Lowrey PE, Hsu KL. Ultrasensitive Detection of Tissue Lipids at the Femtomole Scale Using Low-Microflow Targeted Lipidomics. Anal Chem. 2026; 98(7): 5250–5260.
83.
Grams RJ, Murtagh O, Ware ML, Vasylevskyi S, Hsu KL. Re-Engineering P(V) Chemical Warfare: Harnessing Stereogenic Phosphorous-Azoles for Protein Ligand Discovery In Vivo. bioRxiv. 2026. [preprint]
82.
Ware ML, Leace DM, Qu Z, Schaefer Q, Vaidya SD, Horvath ML, Li Z, Bai Y, Zhang Z, Hsu KL. Protein tyrosine phosphatase inactivation by electrophilic tyrosine modification. Chemical Science. 2026; 17: 5163–5171.
81.
Leace DM, Ware ML, Murtagh O, Tsai HK, Chang CY, Hsu KL. A Glutathione S-Transferase Pi Molecular Glue Tethers Splicing Factors and Remodels Cell Metabolism. JACS. 2025; 147(40): 36170–36179.
80.
Kim G, Grams RJ, Hsu KL. Advancing Covalent Ligand and Drug Discovery beyond Cysteine. Chem Rev. 2025; 125(14): 6654–6684.
79.
Founds MW, Murtagh OL, Grams RJ, Li Z, Ciancone AM, Seal RJ, Hsu KL. Human PTGR2 Inactivation Alters Eicosanoid Metabolism and Cytokine Response of Inflammatory Macrophages. ACS Chem Bio. 2025; 20(6): 1426–1434.
78.
Grams RJ, Wolfe WJ, Seal RJ, Veccia J, Hsu KL. Discovery and Optimization of a Covalent AKR1C3 Inhibitor. J Med Chem. 2025; 68(9): 9465–9478.
77.
Edwards AN, Hsu KL. Emerging opportunities for intact and native protein analysis using chemical proteomics. Analytica Chimica Acta. 2025; 1338: 343551.
76.
Grams RJ, Yuan K, Founds MW, Ware ML, Pilar MG, Hsu KL. Imidazoles are Tunable Nucleofuges for Developing Tyrosine-Reactive Electrophiles. ChemBioChem. 2024; 25(16): e202400382.
75.
Hsu KL, Schumann B, Sletten E, Vinogradova E, Zou P. Voices: Challenges and opportunities for bioorthogonal chemistry. Cell Chem Bio. 2024; 31(3): 380–382.
74.
Chen M, Shin M, Ware TB, Donvito G, Muchhala KH, Mischel R, Mustafa MA, Serbulea V, Upchurch CM, Leitinger N, Akbarali HI, Lichtman AH, and Hsu KL. Endocannabinoid biosynthetic enzymes regulate pain response via LKB1-AMPK signaling. PNAS. 2023; 120(52): e2304900120.
73.
Heindel AJ, Brulet JW, Wang X, Founds MW, Libby AH, Bai DL, Lemke MC, Leace DM, Harris TE, Hafner M, and Hsu KL. Chemoproteomic capture of RNA binding activity in living cells. Nat Comm. 14, 6282 (2023).
72.
Mendez R, Shaikh MS, Lemke MC, Yuan K, Libby AH, Bai DL, Ross MM, Harris TE, and Hsu KL. Predicting small molecule binding pockets on diacylglycerol kinases using chemoproteomics and AlphaFold. RSC Chem Biol. 4, 422–430 (2023).
71.
Ciancone AM*, Seo KW*, Chen M*, Borne AL, Libby AH, Bai DL, Kleiner RE*, and Hsu KL*. Global discovery of covalent modulators of ribonucleoprotein granules. J Am Chem Soc. 145, 11056–11066 (2023).
70.
Brulet JW*, Ciancone AM*, Yuan K*, and Hsu KL. Advances in activity-based protein profiling of functional tyrosines in proteomes. Isr J Chem. 2023; 63: e202300001.
69.
Ciancone AM, Hosseinibarkooie S, Bai DL, Borne AL, and Hsu KL. Global profiling identifies a stress-responsive tyrosine site on EDC3 regulating biomolecular condensate formation. Cell Chem Biol. 2022; 29: 1709–1720.
68.
Grams RJ and Hsu KL. Catch your breath. Nat Chem Biol. 2022; 18: 686–687.
67.
Ozturk H, et al.; Hsu KL; et al. ISL2 is a putative tumor suppressor whose epigenetic silencing reprograms the metabolism of pancreatic cancer. Dev Cell. 2022; 57: 1331–1346.
66.
Grams RJ and Hsu KL. Reactive chemistry for covalent probe development and therapeutic discovery. Trends Pharmacol Sci. 2022; 43: 249–262.
65.
McCloud RL, Yuan K, Mahoney KE, Bai DL, Shabanowitz J, Ross MM, Hunt DF, and Hsu KL. Direct target site identification of a sulfonyl-triazole covalent kinase probe by LC-MS chemical proteomics. Anal Chem. 2021; 93: 11946–11955.
64.
Hussain SS, Tran T, Ware TB, Luse MA, Prevost CT, Ferguson AN, Kashatus JA, Hsu KL, and Kashatus DF. RalA and PLD1 promote lipid droplet growth in response to nutrient withdrawal. Cell Rep. 2021; 36: 109451.
63.
Ware TB and Hsu KL. Advances in chemical proteomic evaluation of lipid kinases – DAG kinases as a case study. Curr Opin Chem Biol. 2021; 65: 101–108.
62.
Nass SR, Steele FF, Ware TB, Libby AH, Hsu KL, and Kinsey SG. Monoacylglycerol lipase inhibition using JZL184 attenuates paw inflammation and functional deficits in a mouse model of inflammatory arthritis. Cannabis Cannabinoid Res. 2021; 6: 233–241.
61.
Cao JK, Viray K, Shin M, Hsu KL, Mackie K, Westenbroek R, and Stella N. ABHD6 inhibition rescues a sex-dependent deficit in motor coordination in the HdhQ200/200 mouse model of Huntington's disease. J Neurol Neurol Disord. 2021; 7: 1–16.
60.
Toroitich EK, Ciancone AM, Hahm HS, Brodowski SM, Libby AH, and Hsu KL. Discovery of a cell-active SuTEx ligand of prostaglandin reductase 2. ChemBioChem. 2021; 22: 2134–2139.
59.
Hsu KL. Shining a light on phenotypic drug discovery. Cell Chem Biol. 2021; 28: 115–117.
58.
Huang T, Borne AL, Brulet JW, and Hsu KL. Chemoproteomic profiling of kinases in live cells using electrophilic sulfonyl triazole probes. Chem Sci. 2021; 12: 3295–3307.
57.
Borne AL, Brulet JW, Yuan K, and Hsu KL. Development and biological applications of sulfur-triazole exchange (SuTEx) chemistry. RSC Chem Biol. 2021; 2: 322–337.
56.
Georgiev GA, et al.; Hsu KL; et al. Lacritin proteoforms promote and restore stability of the tear lipid layer. J Biol Chem. 2021; 296: 100070.
55.
Seki SM, et al.; Hsu KL; et al. Modulation of PKM activity controls differentiation of Th17 cells. Sci Signal. 2020; 13: eaay9217.
54.
Brulet JW, Borne AL, Yuan K, Libby AH, and Hsu KL. Liganding functional tyrosine sites on proteins using sulfur-triazole exchange chemistry. J Am Chem Soc. 2020; 142: 8270–8280.
53.
Shin M, Ware TB, and Hsu KL. DAGL-beta functions as a PUFA-specific triacylglycerol lipase in macrophages. Cell Chem Biol. 2020; 27: 314–321.
52.
Ware TB, Franks CE, Granade ME, Zhang M, Kim KB, Park KS, Gahlmann A, Harris TE, and Hsu KL. Reprogramming fatty acyl specificity of lipid kinases via C1 domain engineering. Nat Chem Biol. 2020; 16: 170–178.
51.
Yin B, Mendez R, Zhao X, Rakhit R, Hsu KL, and Ewald S. Automated spatially targeted optical micro proteomics (autoSTOMP) to determine protein complexity of subcellular structures. Anal Chem. 2020; 92: 2005–2010.
50.
Hahm HS*, Toroitich EK, Borne AL, Brulet JW, Libby AH, Yuan K, Ware TB, McCloud RL, Ciancone AM, and Hsu KL. Global targeting of functional tyrosines using sulfur triazole exchange chemistry. Nat Chem Biol. 2020; 16: 150–159.
49.
Lazo JS, et al.; Hsu KL; et al. Next-generation cell-active inhibitors of the undrugged oncogenic PTP4A3 phosphatase. J Pharmacol Exp Ther. 2019; 371: 652–662.
48.
Franks CE and Hsu KL. Activity-Based Kinome Profiling using Chemical Proteomics and ATP Acyl Phosphates. Curr Protoc Chem Biol. 2019; 11: e72.
47.
Ware TB, Shin M, and Hsu KL. Metabolomics analysis of lipid metabolizing enzyme activity. Methods Enzymol. 2019, 626: 407–428.
46.
Shin M, Buckner A, Prince J, Bullock TNJ, and Hsu KL. Diacylglycerol lipase-beta is required for TNF-alpha response but not CD8+ T cell priming capacity of dendritic cells. Cell Chem Biol. 2019; 26: 1036–1041.
45.
Borne AL, Huang T, McCloud RL, Pachaiyappan B, Bullock TN, and Hsu KL. Deciphering T cell immunometabolism with activity-based protein profiling. Curr Top Microbiol Immunol. 2019; 420: 175–210.
44.
Shin M, Ware TB, Lee HC, and Hsu KL. Lipid-metabolizing serine hydrolases in the mammalian central nervous system: endocannabinoids and beyond. Biochim Biophys Acta. 2019; 1864: 907–921.
43.
Campbell ST, Franks CE, Borne AL, Shin M, Zhang L, and Hsu KL. Chemoproteomic discovery of a ritanserin-targeted kinase network mediating apoptotic cell death of lung tumor cells. Mol Pharmacol. 2018; 94: 1246–1255.
42.
Manterola A, et al.; Hsu KL; et al. Re-examining the potential of targeting ABHD6 in multiple sclerosis. Neuropharmacology. 2018; 141: 181–191.
41.
Manterola A, et al.; Hsu KL; et al. Deregulation of the endocannabinoid system and therapeutic potential of ABHD6 blockade in the cuprizone model of demyelination. Biochem Pharmacol. 2018; 157: 189–201.
40.
Curry Z, et al.; Hsu KL; et al. Monoacylglycerol lipase inhibitors reverse paclitaxel-induced nociceptive behavior in a mouse model of chemotherapy-induced neuropathy. J Pharmacol Exp Ther. 2018; 366: 169–183.
39.
Wilkerson JL, et al.; Hsu KL; et al. Evaluation of different drug classes on transient sciatic nerve injury-depressed marble burying in mice. Pain. 2018; 159: 1155–1165.
38.
Shin M, Franks CE, and Hsu KL. Isoform-selective activity-based profiling of ERK signaling. Chem Sci. 2018; 9: 2419–2431. Featured as a 2018 Chemical Science HOT Article.
37.
McCloud RL, Franks CE, Campbell ST, Purow BW, Harris TE, and Hsu KL. Deconstructing lipid kinase inhibitors by chemical proteomics. Biochemistry. 2018; 57: 231–236. Highlighted in Future of Biochemistry special issue.
36.
Shin M, et al.; Hsu KL; et al. Liposomal Delivery of Diacylglycerol Lipase-Beta Inhibitors to Macrophages Dramatically Enhances Selectivity and Efficacy In Vivo. Mol Pharm. 2018; 15: 721–728.
35.
Franks CE, Campbell ST, Purow BW, Harris TE, and Hsu KL. The Ligand Binding Landscape of Diacylglycerol Kinases. Cell Chem Biol. 2017; 24: 870–880.
34.
Yun B, et al.; Hsu KL; et al. Regulation of calcium release from the endoplasmic reticulum by the serine hydrolase ABHD2. Biochem Biophys Res Commun. 2017; 490: 1226–1231.
33.
Chang JW, et al.; Hsu KL*; Cravatt BF*. Selective inhibitor of platelet-activating factor acetylhydrolases 1b2 and 1b3 that impairs cancer cell survival. ACS Chem Biol. 2015; 10: 925. *co-corresponding authors
Graduate and Postdoctoral Work
32.
Wilkerson JL, et al.; Hsu KL; et al. Diacylglycerol lipase beta inhibition reverses nociceptive behavior in mouse models of inflammatory and neuropathic pain. Br J Pharmacol. 2016; 173: 1678–1692.
31.
Buczynski MW, et al.; Hsu KL; et al. Diacylglycerol lipase disinhibits VTA DA neurons during chronic nicotine exposure. PNAS. 2016; 113: 1086–1091.
30.
Baggelaar MP, et al.; Hsu KL; et al. A highly selective, reversible inhibitor identified by comparative chemoproteomics modulates diacylglycerol lipase activity in neurons. J Am Chem Soc. 2015; 137: 8851–8857.
29.
Kohnz RA, et al.; Hsu KL; et al. Activity-based protein profiling of oncogene-driven changes in metabolism reveals broad dysregulation of PAFAH1B2 and 1B3 in cancer. ACS Chem Biol. 2015; 10: 1624–1630.
28.
Manna JD, Wepy JA, Hsu KL, Chang JW, Cravatt BF, and Marnett LJ. Identification of the major prostaglandin glycerol ester hydrolase in human cancer cells. J Biol Chem. 2014; 289: 33741–33753.
27.
Inloes J, Hsu KL, Dix MM, Viader A, Masuda K, Takei T, Wood MR, and Cravatt BF. The hereditary spastic paraplegia-related enzyme DDHD2 is a principal brain triglyceride lipase. Proc Natl Acad Sci. 2014; 111: 14924–14929.
26.
Grim TW, et al.; Hsu KL; et al. Combined inhibition of FAAH and COX produces enhanced anti-allodynic effects in mouse neuropathic and inflammatory pain models. Pharmacol Biochem Behav. 2014; 124: 405–411.
25.
Naydenov AV, et al.; Hsu KL; et al. ABHD6 Blockade Exerts Antiepileptic Activity in PTZ-Induced Seizures and in Spontaneous Seizures in R6/2 Mice. Neuron. 2014; 83: 361–371.
24.
Agrawal P, et al.; Hsu KL; et al. Mapping posttranscriptional regulation of the human glycome uncovers microRNA defining the glycocode. Proc Natl Acad Sci. 2014; 111: 4338–4343.
23.
Dominguez E, et al.; Hsu KL; et al. Integrated phenotypic and activity-based profiling links Ces3 to obesity and diabetes. Nat Chem Biol. 2014; 10: 113–121.
22.
Yun B, et al.; Hsu KL; et al. Serine hydrolase inhibitors block necrotic cell death by preventing calcium overload of the mitochondria and permeability transition pore formation. J Biol Chem. 2014; 289: 1491–1504.
21.
Hsu KL*, Tsuboi K, Chang JW, Whitby LR, Speers AE, Pugh H, Cravatt BF*. Discovery and optimization of piperidyl-1,2,3-triazole ureas as potent, selective, and in vivo-active inhibitors of α/β-hydrolase domain containing 6 (ABHD6). J Med Chem. 2013; 56: 8270–8279.
20.
Hsu KL*, Tsuboi K, Whitby LR, Speers AE, Pugh H, Inloes J, Cravatt BF*. Development and optimization of piperidyl-1,2,3-triazole ureas as selective chemical probes of endocannabinoid biosynthesis. J Med Chem. 2013; 56: 8257–8269.
19.
Nagano JM, Hsu KL, et al. Selective inhibitors and tailored activity probes for lipoprotein-associated phospholipase A(2). Bioorg Med Chem Lett. 2013; 23: 839–843.
18.
Hsu KL, Tsuboi K, Adibekian A, Pugh H, Masuda K, Cravatt BF. DAGLβ inhibition perturbs a lipid network involved in macrophage inflammatory responses. Nat Chem Biol. 2012; 8: 999–1007.
17.
Adibekian A, et al.; Hsu KL; et al. Confirming target engagement for reversible inhibitors in vivo by kinetically tuned activity-based probes. J Am Chem Soc. 2012; 134: 10345–10348.
16.
Zuhl AM, et al.; Hsu KL; et al. Competitive activity-based protein profiling identifies aza-β-lactams as a versatile chemotype for serine hydrolase inhibition. J Am Chem Soc. 2012; 134: 5068–5071.
15.
Adibekian A, et al.; Hsu KL; et al. Click-generated triazole ureas as ultrapotent in vivo-active serine hydrolase inhibitors. Nat Chem Biol. 2011; 7: 469–478.
14.
Propheter DC, Hsu KL, Mahal LK. Recombinant lectin microarrays for glycomic analysis. Methods Mol Biol. 2011; 723: 67–77.
13.
Hsu KL, Pilobello K, Krishnamoorthy L, Mahal LK. Ratiometric lectin microarray analysis of the mammalian cell surface glycome. Methods Mol Biol. 2011; 671: 117–131.
12.
Propheter DC, Hsu KL, Mahal LK. Fabrication of an oriented lectin microarray. Chembiochem. 2010; 11: 1203–1207.
11.
Hsu KL, Mahal LK. Sweet tasting chips: microarray-based analysis of glycans. Curr Opin Chem Biol. 2009; 13: 427–432.
10.
Hsu KL, Gildersleeve JC, Mahal LK. A simple strategy for the creation of a recombinant lectin microarray. Mol Biosyst. 2008; 4: 654–662.
9.
Hsu KL, Mahal LK. A lectin microarray approach for the rapid analysis of bacterial glycans. Nat Protoc. 2006; 1: 543–549.
8.
Hsu KL, Pilobello KT, Mahal LK. Analyzing the dynamic bacterial glycome with a lectin microarray approach. Nat Chem Biol. 2006; 2: 153–157.
Books & Chapters
7.
Adibekian A, et al.; Hsu KL; et al. Characterization of a Selective, Reversible Inhibitor of Lysophospholipase 2 (LYPLA2). Probe Reports from the NIH Molecular Libraries Program. 2013.
6.
Adibekian A, et al.; Hsu KL; et al. Characterization of a Selective, Reversible Inhibitor of Lysophospholipase 1 (LYPLA1). Probe Reports from the NIH Molecular Libraries Program. 2013.
5.
Hsu KL, et al. Optimization and characterization of triazole urea inhibitors for abhydrolase domain containing protein 6 (ABHD6). Probe Reports from the NIH Molecular Libraries Program. 2012.
4.
Adibekian A, Hsu KL, et al. Optimization and characterization of a triazole urea inhibitor for platelet-activating factor acetylhydrolase type 2 (PAFAH2). Probe Reports from the NIH Molecular Libraries Program. 2011.
3.
Adibekian A, Hsu KL, et al. Optimization and characterization of a triazole urea inhibitor for alpha/beta hydrolase domain-containing protein 11 (ABHD11). Probe Reports from the NIH Molecular Libraries Program. 2011.
2.
Nagano JMG, Hsu KL, et al. Optimization and characterization of a carbamate inhibitor for plasma platelet-activating factor acetylhydrolase (pPAFAH). Probe Reports from the NIH Molecular Libraries Program. 2011.
1.
Hsu KL, et al. Optimization and characterization of a triazole urea inhibitor for diacylglycerol lipase beta (DAGL-β). Probe Reports from the NIH Molecular Libraries Program. 2012.