Pre-prints
Jung S, Zheng Q, Shokat KM. Single-sequence deep learning delivers crystal-quality models of covalent K-Ras G12 hotspot complexes. bioRxiv 2025.09.16.676163. doi: 10.1101/2025.09.16.676163.
Wang C, Hou Y, Zak J, Zheng Q, McCord KA, Wu M, Zhang D, Chung S, Shi Y, Ye J, Zhao Y, Hajjar S, Wilson IA, Paulson JC, Teijaro JR, Zhou X, Sharpless KB, Macauley MS, Wu P. Reshaping the tumor microenvironment by degrading glycoimmune checkpoints Siglec-7 and -9. bioRxiv 2024.10.11.617879. doi: 10.1101/2024.10.11.617879.
Research Articles
Budai B, Vaupel A, Dickson CJ, Beyer KS, Guthy DA, Ostermann N, McGregor LM, De Kanter R, Weiss A, Linder M, Sager E, Bomio-Confaglia C, Proctor R, Leblanc C, Yuan J, Cotesta S, Wilcken R, Danilack AD, Garcia F, Rogemoser P, Kazic-Legueux M, Zhang Z, Zheng Q, Shokat KM, Brachmann SM, Ehmke V. Promise and Challenge of β-Lactone Electrophiles to Target Aspartate 12 of Mutant KRASG12D. J Med Chem. 2025;68(14):15050-15064. PMID: 40635203.
Distal covalent targeting suppresses signaling of oncogenic K-Ras(G13C) in cancer cells
Zheng Q*, Shen T**, Pampel J, Shokat KM.
ACS Chem Biol. 2025;20(7):1696-1706. PMID: 40629868.
Denitrogenative Alkylation of K-Ras(G12D) Inhibits Oncogenic Signaling in Cancer Cells
Zheng Q, Shokat KM.
J Am Chem Soc. 2025;147(28):24785-24792. PMID: 40587607.
Strain-release alkylation of Asp12 enables mutant selective targeting of K-Ras-G12D
Zheng Q*, Zhang Z*, Guiley KZ, Shokat KM
Nat Chem Biol. 2024;20(9):1114-1122. PMID: 38443470.
Liu Y, Wang R, Zheng Q, Hu X, Liu F, Yan N. Modular synthesis of conjugated enamidines and cascade annulation toward benzofuran-3-oxoacetate. Organic Chemistry Frontiers. 2024;11(7):2047-53.
Malakoutikhah M, Mahran R, Gooran N, Masoumi A, Lundell K, Liljeblad A, Guiley K, Dai S, Zheng Q, Zhu L, Shokat KM, Kopra K, Härmä H. Nanomolar Protein Thermal Profiling with Modified Cyanine Dyes. Anal Chem. 2023;95(50):18344-18351. PMID: 38060502.
Wu Q, Xue Q, Li J, Zheng Q, Zhao X, Li W, et al. Identification of Styryl Sulfonyl Fluoride as a Near-Perfect Michael Acceptor for Diversified Protein Bioconjugations. CCS Chemistry. 2023;5(10):2251-63.
KRAS is vulnerable to reversible switch-II pocket engagement in cells
Vasta JD*, Peacock DM*, Zheng Q*, Walker JA, Zhang Z, Zimprich CA, Thomas MR, Beck MT, Binkowski BF, Corona CR, Robers MB, Shokat KM
Nat Chem Biol. 2022;18(6):596-604. PMID: 35314814.
Garnar-Wortzel L, Bishop TR, Kitamura S, Milosevich N, Asiaban JN, Zhang X, Zheng Q, Chen E, Ramos AR, Ackerman CJ, Hampton EN, Chatterjee AK, Young TS, Hull MV, Sharpless KB, Cravatt BF, Wolan DW, Erb MA. Chemical Inhibition of ENL/AF9 YEATS Domains in Acute Leukemia. ACS Cent Sci. 2021;7(5):815-830. PMID: 34079898.
Sulfur [18F]Fluoride Exchange Click Chemistry Enabled Ultrafast Late-Stage Radiosynthesis
Zheng Q*, Xu H*, Wang H, Du WH, Wang N, Xiong H, Gu Y, Noodleman L, Sharpless KB, Yang G, Wu P
J Am Chem Soc. 2021;143(10):3753-3763. PMID: 33630577.
Sulfur(VI) Fluoride Exchange (SuFEx)-Enabled High-Throughput Medicinal Chemistry
Kitamura S*, Zheng Q*, Woehl JL, Solania A, Chen E, Dillon N, Hull MV, Kotaniguchi M, Cappiello JR, Kitamura S, Nizet V, Sharpless KB, Wolan DW
J Am Chem Soc. 2020;142(25):10899-10904. PMID: 32479075.
SuFEx-enabled, agnostic discovery of covalent inhibitors of human neutrophil elastase
Zheng Q*, Woehl JL*, Kitamura S, Santos-Martins D, Smedley CJ, Li G, Forli S, Moses JE, Wolan DW, Sharpless KB
Proc Natl Acad Sci U S A. 2019;116(38):18808-18814. PMID: 31484779.
Smedley CJ, Zheng Q, Gao B, Li S, Molino A, Duivenvoorden HM, Parker BS, Wilson DJD, Sharpless KB, Moses JE. Bifluoride Ion Mediated SuFEx Trifluoromethylation of Sulfonyl Fluorides and Iminosulfur Oxydifluorides. Angew Chem Int Ed Engl. 2019;58(14):4552-4556. PMID: 30740848.
Gahtory D, Sen R, Pujari S, Li S, Zheng Q, Moses JE, Sharpless KB, Zuilhof H. Quantitative and Orthogonal Formation and Reactivity of SuFEx Platforms. Chemistry. 2018;24(41):10550-10556. PMID: 29949211.
Gao B, Zhang L, Zheng Q, Zhou F, Klivansky LM, Lu J, Liu Y, Dong JJ, Wu P, Sharpless KB. Bifluoride-catalysed sulfur(VI) fluoride exchange reaction for the synthesis of polysulfates and polysulfonates. Nat Chem. 2017;9(11):1083-8. PMID: 29064495.
Wang H, Zhou F, Ren G, Zheng Q, Chen H, Gao B, Klivansky L, Liu Y, Wu B, Xu Q, Lu J, Sharpless KB, Wu P. SuFEx-Based Polysulfonate Formation from Ethenesulfonyl Fluoride-Amine Adducts. Angew Chem Int Ed Engl. 2017;56(37):11203-11208. PMID: 28792119.
Zha GF*, Zheng Q*, Leng J, Wu P, Qin HL, Sharpless KB. Palladium-Catalyzed Fluorosulfonylvinylation of Organic Iodides. Angew Chem Int Ed Engl. 2017;56(17):4849-4852. PMID: 28370917.
Ren G, Zheng Q*, Wang H*. Aryl Fluorosulfate Trapped Staudinger Reduction. Org Lett. 2017;19(7):1582-1585. PMID: 28332844.
Ethenesulfonyl Fluoride (ESF): An On-Water Procedure for the Kilogram-Scale Preparation
Zheng Q, Dong J, Sharpless KB
J Org Chem. 2016 Nov 18;81(22):11360-11362. PMID: 27764941.
Qin HL*, Zheng Q*, Bare GA, Wu P, Sharpless KB. A Heck-Matsuda Process for the Synthesis of β-Arylethenesulfonyl Fluorides: Selectively Addressable Bis-electrophiles for SuFEx Click Chemistry. Angew Chem Int Ed Engl. 2016;55(45):14155-14158. PMID: 27723200.
Zheng Q, Meng W, Jiang GJ, Yu ZX. CuI-catalyzed C1-alkynylation of tetrahydroisoquinolines (THIQs) by A3 reaction with tunable iminium ions. Org Lett. 2013;15(23):5928-31. PMID: 24237286.
Jiang GJ*, Zheng Q*, Dou M, Zhuo LG, Meng W, Yu ZX. Mild-condition synthesis of allenes from alkynes and aldehydes mediated by tetrahydroisoquinoline (THIQ). J Org Chem. 2013;78(23):11783-93. PMID: 24266693.
Review and Viewpoint Articles
Homer JA, Xu L, Kayambu N, Zheng Q, Choi EJ, Kim BM, Sharpless KB, Zuilhof H, Dong J, Moses JE. Sulfur fluoride exchange. Nat Rev Methods Primers. 2023;3:58. PMID: 38873592.
Zheng Q*, Peacock DM*, Shokat KM. Drugging the Next Undruggable KRAS Allele-Gly12Asp. J Med Chem. 2022;65(4):3119-3122. PMID: 35167298.
Barrow AS, Smedley CJ, Zheng Q, Li S, Dong J, Moses JE. The growing applications of SuFEx click chemistry. Chem Soc Rev. 2019;48(17):4731-4758. PMID: 31364998.