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Scheinpflug R, Czodrowski P, Janning P, Depta L, Quambusch L, Müller MP, Engels B, Rauh
D (2019) Structural and chemical insights into the covalent-allosteric inhibition of the protein
kinase Akt. Chem Sci 10:3573–3585. https://doi.org/10.1039/C8SC05212C
136. Craven GB, Affron DP, Allen CE, Matthies S, Greener JG, Morgan RML, Tate EW,
Armstrong A, Mann DJ High-throughput kinetic analysis for target-directed covalent ligand
discovery. Angew Chem Int Ed 57:5257–5261. https://doi.org/10.1002/anie.201711825
137. Bührmann M, Hardick J, Weisner J, Quambusch L, Rauh D (2017) Covalent lipid pocket
ligands targeting p38α MAPK mutants. Angew Chem Int Ed 56:13232–13236. https://doi.org/
10.1002/anie.201706345
138. Dalton SE, Dittus L, Thomas DA, Convery MA, Nunes J, Bush JT, Evans JP, Werner T,
Bantscheff M, Murphy JA, Campos S (2018) Selectively targeting the Kinome-conserved
lysine of PI3Kδ as a general approach to covalent kinase inhibition. J Am Chem Soc
140:932–939. https://doi.org/10.1021/jacs.7b08979
139. Anscombe E, Meschini E, Mora-Vidal R, Martin MP, Staunton D, Geitmann M, Danielson
UH, Stanley WA, Wang LZ, Reuillon T, Golding BT, Cano C, Newell DR, Noble MEM,
Wedge SR, Endicott JA, Griffin RJ (2015) Identification and characterization of an irreversible
inhibitor of CDK2. Cell Chem Biol 22:1159–1164. https://doi.org/10.1016/j.chembiol.2015.
07.018
140. Dahal UP, Gilbert AM, Obach RS, Flanagan ME, Chen JM, Garcia-Irizarry C, Starr JT,
Schuff B, Uccello DP, Young JA (2016) Intrinsic reactivity profile of electrophilic moieties
to guide covalent drug design: N-α-acetyl-L-lysine as an amine nucleophile. Med Chem
Commun 7:864–872. https://doi.org/10.1039/C6MD00017G
141. Zhao Q, Ouyang X, Wan X, Gajiwala KS, Kath JC, Jones LH, Burlingame AL, Taunton J
(2017) Broad-Spectrum kinase profiling in live cells with lysine-targeted Sulfonyl fluoride
probes. J Am Chem Soc 139:680–685. https://doi.org/10.1021/jacs.6b08536
142. Hatcher JM, Wu G, Zeng C, Zhu J, Meng F, Patel S, Wang W, Ficarro SB, Leggett AL, Powell
CE, Marto JA, Zhang K, Ngo JCK, Fu X-D, Zhang T, Gray NS (2018) SRPKIN-1: a covalent
SRPK1/2 inhibitor that potently converts VEGF from pro-angiogenic to anti-angiogenic
isoform. Cell Chem Biol 25:460–470.e6. https://doi.org/10.1016/j.chembiol.2018.01.013
94
M. Gehringer