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. 2022 Mar 31;12(9):3548–3566. doi: 10.1016/j.apsb.2022.03.019

Table 1.

The discovery strategies of molecular glues and the specific techniques exploited within these studies.

Target protein Molecular glues Discovery strategy Techniques Refs.
PD-L1 BMS-202 Serendipity NMR, DSF, crystal 32
REV1 JH-RE-06 Serendipity Crystal, SDS-PAGE 40
MDMX RO-2443, RO-5986 Serendipity NMR, SEC-SLS, crystal, TR-FRET 46
BCL6 BI-3802 Serendipity IF, Cryo-EM, WB, TR-FRET 53
CCT369260 Serendipity Nano-BRET, IF, MSD 54
MERS-CoV P3 Virtual screening SAXS, IF, crystal, thermostability 61
DDB1CRBN–substrate Thalidomide, lenalidomide, pomalidomide Serendipity Proteomic, LC‒MS/MS, crystal, TR-FRET 62,63
CC-122, CC-220 Rational design Crystal, WB, TR-FRET 64,65
CC-885 Rational design IP, crystal, pull-down, IF, LC‒MS/MS, SPPIER 67
CC-90009 Rational design WB, proteomic, crystal 69
SJ6986 Rational design WB, MD simulation 68
DDB1DCAF15–RBM39 Indisulam, E7820 Serendipity IP, LC‒MS/MS, CRISPR/Cas9, pull-down, Cryo-EM, TR-FRET 77,78
DDB1–CDK12/cyclinK dCeMM2, dCeMM3, dCeMM4 Chemical screening WB, CRISPR/Cas9, pull-down 83
(R)-CR8 Data mining Co-IP, ITC, crystal, TR-FRET, nano-BRET 85
HQ461 HTS CRISPR/Cas9, Co-IP, WB, pull-down, CXMS, LC‒MS/MS, DSF, thermostability 84
SCFβ-TrCPβ-catenin NRX-252114, NRX-252262, NRX-103094 HTS, rational design FP, crystal, TR-FRET, pull-down 89
LC3-mHTT 10O5, 8F20, AN1, AN2 HTS SMM, OI-RD, HTRF, MST, pull-down, IF 93
GLP-1–GLP-1R LSN3160440 HTS, rational design Crystal, MD simulation, IF 101