Cell Death Discovery

Table 2 Summary of Lipoylation Pathway Targeting in Cancer Therapies.

From: Protein lipoylation in cancer: metabolic reprogramming and therapeutic potential

Lipoylated protein	Cancers or caner cells	Targeted metabolic type	Mechanism	Targeting strategies	Ref.
DLAT	HCC	leucine decomposition	DLAT Acetylat AUH inhibits leucine decomposition	AUH^K109R-mRNA lipid nanoparticles	[154]
DLAT	HCC	OXPHOS	Stabilizes mitochondrial function	Elesclomol	[182]
PDH, KGDH	Triple-negative cancer cells	OXPHOS	Increase lipoylated DLAT to improve mitochondrial respiration	Polymerase-δ Interacting protein 2	[121]
DLST	TNBC	OXPHOS	Inhibits TCA cycling	DLST depletion or CPI-613	[69]
DLST	T-ALL	OXPHOS	Disrupts the biochemical conversion of α-KG to succinyl-CoA	DLST knockdown	[70]
DLST	High-risk neuroblastoma	OXPHOS	Inhibits OXPHOS and reduces NADH levels	DLST depletion or complex I inhibitor IACS-010759	[162]
DLST	Cancer cell lines with DLST amplification or high mRNA levels	OXPHOS	Inhibits cellular OXPHOS	Obatoclax mesylate	[163]
DLST, DLAT	AML	OXPHOS	Blocks glucose or glutamine-derived carbon from entering the TCA cycle and promotes PDH phosphorylation	CPI-613	[150]
OGDH	AML	TCA cycle	Impairs the production of aspartic acid	OGDH inhibition	[164]
KGDH	AML	OXPHOS	Targets KGDH to block the TCA cycle	Imipridone ONC213	[165]
BCAA	Ovarian and breast cancer cell lines	BCAA metabolism	Inhibition of BCKDK to decrease intracellular BCAA levels	3,6-dichlorobenzothiophene-2-carboxylic acid (BT2/DCBC) or (S)-2-chloro-4-methylvaleric acid (CMVA)	[166]
BCKDH	HCC	BCAA metabolism	Phosphorylation of the BCKDHA subunit and activation of the mTORC1 signaling pathway	BCKDK inhibitor BT2 or BCAA dietary restriction	[86]
GCSH	Breast cancer cells	Glycine metabolism	Limit GCSH translations	Transcript variants	[168]
GCS	HCC	Glycine metabolism	Inhibits the lipoylation complex	GLDC silence	116]

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