Skip to main content
. Author manuscript; available in PMC: 2024 May 1.
Published in final edited form as: Trends Cancer. 2023 Feb 18;9(5):410–420. doi: 10.1016/j.trecan.2023.01.005

Table 1.

List of inhibitors for glycation repair and detoxification systems with possible cancer applications

Target Entry number Inhibitor Cancer applications Refs
GLO1 1 S-p-Bromobenzylglutathione cyclopentyl diester
graphic file with name nihms-1868689-t0001.jpg
  • Induced MGO accumulation to inhibit cancer cell growth and promote cancer cell apoptosis

  • Active against breast, brain, lung, colon, leukemia, melanoma, ovarian, renal, prostate cancer cell lines

  • Active against glioblastoma tumors in mice

[7983]
2 Methotrexate
graphic file with name nihms-1868689-t0002.jpg
  • Inhibited MGO metabolism in patients with lymphoid leukemia

  • FDA-approved chemotherapeutic drug

[84]
3 Curcumin and derivatives
graphic file with name nihms-1868689-t0003.jpg
  • Potent competitive GLO1 inhibitor

  • Active against breast, prostate and brain cancer cell lines

[85, 86]
4 Tetrahydropyridoindole-thiourea scaffold
graphic file with name nihms-1868689-t0004.jpg
  • Increased intracellular MGO level in lung cancer cells

  • Suppressed osteoclast formation in mouse macrophage cells

[87]
PAD4 5 F-amidine
graphic file with name nihms-1868689-t0005.jpg
  • Covalent inhibitor that targets the active site cysteine

[88]
6 GSK484
graphic file with name nihms-1868689-t0006.jpg
  • Reversible covalent inhibitor

  • Blocked the formation of mouse neutrophil extracellular traps (NETs)

  • Facilitated apoptosis of triple-negative breast cancer (TNBC) cells

  • Sensitized irradiation-induced inhibition of TNBC

[89]
7 BMS-P5
graphic file with name nihms-1868689-t0007.jpg
  • More potent than GSK484

  • Blocked NETs formation and hindered the progression of multiple myeloma in mice

[92]
8 JBI-589
graphic file with name nihms-1868689-t0008.jpg
  • Blocked the formation of NETs, reduced both primary tumor growth and lung metastases in mice

[93]
DJ-1 9 Amino-epoxycyclohexenone
graphic file with name nihms-1868689-t0009.jpg
  • Irreversible covalent inhibitor targeting the active site cysteine

[94]
10 Isatin-based analogs
graphic file with name nihms-1868689-t0010.jpg
  • Reversible covalent inhibitor targeting the active site cysteine

[95]