Exploration of Medicine

From: Lactate metabolic pathway regulates tumor cell metastasis and its use as a new therapeutic target

Table 1. List of information on LDHA inhibitors

LDHA inhibitors	Competitive sites	LDHA (K_i value)	Shortcomings	References
Oxamate	Pyruvate	136.3 μM	High polarity, low exocytosis across cell membranes, high dosing concentration	[71–75]
(R)-(–)-gossypol	NADH	1.9 μM	Non-specific toxicity	[76–78, 84, 85]
FX11	NADH	8 μM	Not yet used in clinical trials	[76, 78]
Quinoline 3-sulfonamides	NADH	4–6 nM	Low clearance in vivo	[88]
GF	Pyruvate	5.46 μM	Possible inhibition of RNA synthesis rather than blockage of glycolysis	[89, 92]
GF	NADH	56 μM		[89, 92]
NHI	Pyruvate, NADH	8.9 μM	Novel inhibitors to be studied	[15, 93]
GNE-140	NADH	-	Novel inhibitors to be studied	[96]

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GF: galloflavin. K_i: inhibition constant; -: no literature has demonstrated it

Declarations

Author contributions

WX, XL, and YZ: Writing—original draft. MZ and ML: Writing—review & editing, Supervision.

Conflicts of interest

The authors declare that they have no conflicts of interest.

Ethical approval

Not applicable.

Consent to participate

Not applicable.

Consent to publication

Not applicable.

Availability of data and materials

Not applicable.

Funding

This work is supported by the National Natural Science Foundation of China [81960519, 81660463, 82060514], the Natural Science Foundation of Hainan Province [2019CXTD406], and Hainan Province Science and Technology Special Fund [ZDYF2021SHFZ222]. The funders had no role in study design, data collection and analysis, decision to publish, or preparation of the manuscript.

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