Synthesis and pharmacological evaluation of carboxycoumarins as a new antitumor treatment targeting lactate transport in cancer cells

Draoui, Nihed; Schicke, Olivier; Fernandes, Antony E.; Drozak, Xavier; Nahra, Fady; Dumont, Amélie; Douxfils, Jonathan; Hermans, Emmanuel; Dogné, Jean‐Michel; Corbau, Romuald; Marchand, Arnaud; Chaltin, Patrick; Sonveaux, Pierre; Feron, Olivier; Riant, Olivier

doi:10.1016/j.bmc.2013.09.010

Cited by 59 publications

(64 citation statements)

References 31 publications

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“…Alternatively, oxidative cancer cells can metabolically exploit host cells. Targeting PKM2, 160 glutaminolysis, 8 and the oxidative pathway of lactate 111,[161][162][163] would therefore constitute interesting anticancer options.…”

Section: Discussionmentioning

confidence: 99%

Common Responses of Tumors and Wounds to Hypoxia

Payen

Brisson

Dewhirst³

et al. 2015

The Cancer Journal

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Hypoxia is a characteristic of tumors and wounds. Hypoxic cells develop 2 common strategies to face hypoxia: the glycolytic switch and the angiogenic switch. At the onset of hypoxia, alleviation of the Pasteur effect ensures short-term cell survival. Long-term hypoxic cell survival requires a further acceleration of the glycolytic flux under the control of hypoxia-inducible factor 1 that stimulates the expression of most glycolytic transporters and enzymes, uncouples glycolysis from the TCA cycle, and rewires glycolysis to lactic fermentation. Hypoxic cells also trigger angiogenesis, a process that aims to restore normal microenvironmental conditions. Transcription factors (hypoxia-inducible factor 1, nuclear factor κB, activator protein 1) and lactate cooperate to stimulate the expression of proangiogenic agents. Cancer cells differ from normal hypoxic cells by their proliferative agenda and by a high metabolic heterogeneity. These effects in tumor account for further molecular and metabolic changes and for a persistent stimulation of angiogenesis.

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Section: Discussionmentioning

confidence: 99%

Common Responses of Tumors and Wounds to Hypoxia

Payen

Brisson

Dewhirst³

et al. 2015

The Cancer Journal

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“…The re mark able de pen dency for sur vival of hy poxic/ gly colytic can cer cells on the meta bolic pref er ences of nor moxic/ ox ida tive ones mo ti vated the de vel op ment of strate gies aimed to in ter fere with the ex change of lac tate. Ther a peu tic in ter ven tions could be aimed at in hibit ing MCT4 in hy poxic can cer cell com part ments [86], in hibit ing MCT1 [5,[87][88][89] and lac tate up take [90,91] in oxy genated/ ox ida tive can cer cells, in hibit ing LDHB [76,92] or, pos si bly, in hibit ing the mi to chon dr ial pyru vate car rier in ox ida tive can cer cells [93]. In our opin ion, fu ture ther a peu tic de vel op ments should aim at tar get ing the ox ida tive path way of lac tate in can cer cells that re side close to drug de liv er ing blood ves sels.…”

Section: Metabolic Cooperation In Cancermentioning

confidence: 99%

Cancer metabolism in space and time: Beyond the Warburg effect

Danhier

Bański

Payen

et al. 2017

Biochimica et Biophysica Acta (BBA) - Bioenergetics

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178

139

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Available online xxx Keywords:Can cer Me tab o lism Mi to chon dria Het ero gene ity Metas ta sis A B S T R A C T Al tered me tab o lism in can cer cells is piv otal for tu mor growth, most no tably by pro vid ing en ergy, re duc ing equiv a lents and build ing blocks while sev eral metabo lites ex ert a sig nal ing func tion pro mot ing tu mor growth and pro gres sion. A can cer tis sue can not be sim ply re duced to a bulk of pro lif er at ing cells. Tu mors are in deed com plex and dy namic struc tures where sin gle cells can het ero ge neously per form var i ous bi o log i cal ac tiv i ties with dif fer ent meta bolic re quire ments. Be cause tu mors are com posed of dif fer ent types of cells with meta bolic ac tiv i ties af fected by dif fer ent spa tial and tem po ral con texts, it is im por tant to ad dress me tab o lism tak ing into ac count cel lu lar and bi o log i cal het ero gene ity. In this re view, we de scribe this het ero gene ity also in meta bolic fluxes, thus show ing the rel a tive con tri bu tion of dif fer ent meta bolic ac tiv i ties to tu mor pro gres sion ac cord ing to the cel lu lar con text. This ar ti cle is part of a Spe cial Is sue en ti tled Res pi ra tory com plex I, edited by Giuseppe Gas parre, Ro drigue Rossig nol and Pierre Son veaux. Abbreviations: ACL, ATP cit rate lyase; AMPK, adeno sine monophos phate ki nase; ARG1, L argi nine me tab o liz ing en zyme arginase 1; BCAA, branched chain amino acid; Bcl2, B cell lym phoma 2; CAF, can cer as so ci ated fi brob last; CIC, can cer ini ti at ing cell; COX2, cy tochrome ox i dase; CSC, can cer stem cell; CREB, cyclic adeno sine monophos phate re sponse el e ment bind ing pro tein; DEC1, dif fer en tially ex pressed in chon dro cytes 1; EMT, ep ithe lial to mes enchy mal tran si tion; FAK, fo cal ad he sion ki nase; FAS, fatty acid syn thase; FBP, fruc tose 1,6 bis pho s phate; FDG PET, [ F] flu o rodeoxyglu cose positron emis sion to mog ra phy; GAPDH, glyc er alde hyde 3 phos phate de hy dro ge nase; HIF 1, hy poxia ac ti vated fac tor 1; HK2, hex ok i nase 2; HMGB1, high mo bil ity group box 1; HU VEC, hu man um bil i cal vein en dothe lial cell; IFN γ, in ter feron gamma; LDH, lac tate de hy dro ge nase; MEF, murine em bry onic fi brob last; MET, mes enchy mal to ep ithe lial tran si tion; MRI, mag netic res o nance imag ing; mTORC1, mam malian tar get of ra pamycin com plex 1; NSCLC, non small cell lung can cer; OX PHOS, ox ida tive phos pho ry la tion; PDAC, pan cre atic duc tal ade no car ci noma; PHD, pro lyl hy drox y lase; pHe, ex tra cel lu lar pH; pHi, in tra cel lu lar pH; PK, pyru vate ki nase; PPP, pen tose phos phate path way; REDD1, reg u lated in de vel op ment and DNA dam age re sponse 1; RhoA, Ras ho molog gene fam ily, mem ber A; ROS, re ac tive oxy gen species; SASP, senes cence as so ci ated se cre tory phe no type; SCO2, syn the sis of cy tochrome ox i dase 2; SGK 1, serum and glu co cor ti coid reg u lated ki nase 1 Sirt1, sir tuin 1; TAM, tu mor as so ci ated macrophage; TIGAR, TP53 in duced gly col y ...

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“…Compound 65 ( Fig. 18) with Nmethylbenzyl moiety at the C-7 position was found to be the more active compound compared to the compound 64 as parent compound [117].…”

Section: Diverse 7-substituted Coumarinsmentioning

confidence: 92%