Lactate dehydrogenase inhibitor polypeptides for treatment of cancer

A lactate dehydrogenase and cyclic polypeptide technology, which is applied in the field of polypeptides that regulate the activity of natural tetramer lactate dehydrogenase, can solve the problem of low clinical value

Pending Publication Date: 2022-05-06
ЮНІВЕРСИТЕ КАТОЛІК ДЕ ЛУВЕН
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  • Abstract
  • Description
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Problems solved by technology

On the other hand, high polarity often prevents molecules from effectively interacting with the catalytic sites of LDH1 or LDH5, and thus non-"drug-like" features often lead to lower clinical value (Ward et al. (2012); Kohlmann et al. (2013))
In conclusion, although LDH remains a very promising and effective target, LDH inhibitors have not demonstrated their potential in clinical trials

Method used

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  • Lactate dehydrogenase inhibitor polypeptides for treatment of cancer
  • Lactate dehydrogenase inhibitor polypeptides for treatment of cancer
  • Lactate dehydrogenase inhibitor polypeptides for treatment of cancer

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Embodiment Construction

[0045] To establish a new way to inhibit LDH, the focus is on unraveling LDH allosteric sites, the targeting of which could lead to unprecedented approaches to this problem. Given that tetramer is the smallest functional unit, the activity of LDH depends on its catalytic site and oligomerization state. With regard to LDHs, since their N-terminal arms extend from one subunit and wrap around two adjacent subunits, the subunits are held together, thereby promoting cohesion of the overall tetramer. Interestingly, the 32 N-terminal amino acid fragment of LDH is known to interfere with LDH tetramerization in vitro ( et al. (1987)). Taken together, these observations prompted the inventors to evaluate this N-terminal arm as a starting point for the design and development of molecules that interfere with LDH tetramerization.

[0046] The present invention relates to polypeptides that modulate the activity of at least one isoform of native tetrameric lactate dehydrogenase.

[0047]...

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Abstract

The present invention relates to polypeptides that modulate the activity of at least one subtype of natural tetramer lactic dehydrogenase and their use as medicaments for the treatment of cancer. More specifically, the present invention relates to linear and cyclic polypeptides that inhibit tetramerization of lactic dehydrogenase subunits.

Description

technical field [0001] The present invention relates to a polypeptide that modulates the activity of natural tetrameric lactate dehydrogenase and its use as a drug for the treatment of cancer. More specifically, the present invention relates to linear and cyclic polypeptides that inhibit the tetramerization of lactate dehydrogenase subunits. Background technique [0002] Cancer cells undergo enormous metabolic adaptations to sustain their anabolic growth and proliferative processes. The most striking feature of this metabolic plasticity is the amplification of glycolytic activity and lactate production, regardless of oxygen availability. This enhancement of glycolysis, known as the Warburg effect, allows cancer cells to divert a portion of carbohydrates from energy production to anabolic pathways, thereby enhancing cell proliferation. On the other hand, elevated intracellular and extracellular lactate, the end product of glycolysis, drives pathogenesis by promoting several...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C12N9/04C07K7/06C07K7/08
CPCC07K7/06A61P35/00A61K38/00A01H5/02C12N9/0006C12Y101/01027
Inventor 皮埃尔·索沃克斯拉斐尔·弗雷德里克利奥波德·塔博露西·布里松塔玛拉·科佩蒂
Owner ЮНІВЕРСИТЕ КАТОЛІК ДЕ ЛУВЕН
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