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Carbonic Anhydrase Inhibitors Targeting Metabolism and Tumor Microenvironment

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dc.contributor.authorAngeli, Andrea
dc.contributor.authorCarta, Fabrizio
dc.contributor.authorNocentini, Alessio
dc.contributor.authorWinum, Jean-Yves
dc.contributor.authorZalubovskis, Raivis
dc.contributor.authorAKDEMİR, ATİLLA
dc.contributor.authorOnnis, Valentina
dc.contributor.authorEldehna, Wagdy M.
dc.contributor.authorCapasso, Clemente
dc.contributor.authorDe Simone, Giuseppina
dc.contributor.authorMonti, Simona Maria
dc.contributor.authorCarradori, Simone
dc.contributor.authorDonald, William A.
dc.contributor.authorDedhar, Shoukat
dc.contributor.authorSupuran, Claudiu T.
dc.contributor.institutionauthorAKDEMİR, ATİLLA
dc.date.accessioned2020-11-24T20:59:07Z
dc.date.available2020-11-24T20:59:07Z
dc.date.issued2020-10-01T00:00:00Z
dc.description.abstractThe tumor microenvironment is crucial for the growth of cancer cells, triggering particular biochemical and physiological changes, which frequently influence the outcome of anticancer therapies. The biochemical rationale behind many of these phenomena resides in the activation of transcription factors such as hypoxia-inducible factor 1 and 2 (HIF-1/2). In turn, the HIF pathway activates a number of genes including those involved in glucose metabolism, angiogenesis, and pH regulation. Several carbonic anhydrase (CA, EC 4.2.1.1) isoforms, such as CA IX and XII, actively participate in these processes and were validated as antitumor/antimetastatic drug targets. Here, we review the field of CA inhibitors (CAIs), which selectively inhibit the cancer-associated CA isoforms. Particular focus was on the identification of lead compounds and various inhibitor classes, and the measurement of CA inhibitory on-/off-target effects. In addition, the preclinical data that resulted in the identification of SLC-0111, a sulfonamide in Phase Ib/II clinical trials for the treatment of hypoxic, advanced solid tumors, are detailed.
dc.identifier.citationAngeli A., Carta F., Nocentini A., Winum J., Zalubovskis R., AKDEMİR A., Onnis V., Eldehna W. M. , Capasso C., De Simone G., et al., -Carbonic Anhydrase Inhibitors Targeting Metabolism and Tumor Microenvironment-, METABOLITES, cilt.10, 2020
dc.identifier.doi10.3390/metabo10100412
dc.identifier.pubmed33066524
dc.identifier.scopus85094191127
dc.identifier.urihttp://hdl.handle.net/20.500.12645/27425
dc.identifier.wosWOS:000585082100001
dc.titleCarbonic Anhydrase Inhibitors Targeting Metabolism and Tumor Microenvironment
dc.typeArticle
dspace.entity.typePublication
local.avesis.id09520cde-6366-497e-989f-62c85e99d5dc
local.publication.goal03 - Sağlık ve Kaliteli Yaşam
local.publication.isinternational1
relation.isAuthorOfPublication19bc513a-c695-4e72-ba1d-83b8d6c574c8
relation.isAuthorOfPublication.latestForDiscovery19bc513a-c695-4e72-ba1d-83b8d6c574c8
relation.isGoalOfPublication9c198c48-b603-4e2f-8366-04edcfc1224c
relation.isGoalOfPublication.latestForDiscovery9c198c48-b603-4e2f-8366-04edcfc1224c
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