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Biology subjects

Pinheiro, L. C.

Publications and source records attributed to Pinheiro, L. C..

2 recordsLinked to original sources

Absolute quantitative proteomics guides patient-stratified drug repurposing in clear cell and papillary renal cell carcinoma.

BackgroundRenal cell carcinoma (RCC) is a highly heterogeneous disease in which distinct molecular subtypes exhibit characteristic genomic, metabolic, and microenvironmental features that influence therapeutic response. Substantial inter-patient variability exists within each subtype, resulting in markedly different clinical outcomes even among tumours of the same histological category. Proteomics provides a direct readout of tumour biology and pathway activity, complementing genomic information and enabling the identification of patient-specific actionable vulnerabilities. We applied a Total Protein Approach (TPA)-based prescriptomics framework that integrates absolute quantitative proteomics with curated drug-target knowledge to nominate patient-specific drug-repurposing options, positioned as coadjuvants to the prevailing standard of care. MethodsSeventeen human kidney tissue specimens, seven clear cell RCC (ccRCC), five papillary RCC (pRCC), and five normal adjacent tissues (NAT), were retrieved from the publicly available PRIDE repository (PXD023296) and reanalysed by TPA-based absolute quantification applied to previously acquired label-free LC-MS/MS data. Differential expression analysis between each tumour subtype and NAT identified subtype-specific upregulated proteins, wich were intersected with Therapeutic Target Database (TTD) to nominate FDA-approved drugs targeting dysregulated proteins as candidate repurposing strategies. ResultsccRCC and pRCC produced distinct proteome-wide upregulation profiles consistent with their known biological drivers. TPA index stratification nominated bempedoic acid (ACLY inhibitor) and tipiracil hydrochloride (TYMP inhibitor) as patient-stratified candidates for ccRCC, and auranofin (TXNRD1 inhibitor), bempedoic acid, and mipomersen (APOB-directed antisense oligonucleotide) for pRCC. ACLY was the only top-priority target shared across both subtypes, pointing to a candidate cross-subtype metabolic vulnerability. Secondary candidates emerged from protein-protein interaction network analysis in both subtypes.. ConclusionsThis study presents a quantitative proteomics framework for translating individual-patient proteomic dysregulation into coadjuvant drug-repurposing hypotheses across the principal RCC subtypes. By combining the TPA for absolute protein quantification with prescriptomics-guided drug-target mapping, we show that ccRCC and pRCC harbour distinct, individually stratifiable therapeutic vulnerabilities. These findings provide a proof-of-concept for proteomics-based treatment stratification in RCC and establish a scalable framework that, pending functional validation, could inform personalised therapeutic decision-making across RCC subtypes.

biochemistry↗

Activation of the TRKB receptor mediates the panicolytic-like effect of NOS inhibitor aminoguanidine

Nitric oxide (NO) triggers escape reactions in the dorsal periaqueductal gray matter (dPAG), a core structure mediating panic-associated responses, and decreases the release of BDNF in vitro. BDNF mediates the panicolytic effect induced by antidepressant drugs and produces these effects per se when injected into the dPAG. Based on these findings, we hypothesize that nitric oxide synthase (NOS) inhibitors would have panicolytic properties associated with increased BDNF signaling in the dPAG. We observed that the repeated (7 days), but not acute (1day), systemic administration of the NOS inhibitor aminoguanidine (AMG; 15 mg/kg/day) increased the latency to escape from the open arm of the elevated T-maze (ETM) and inhibited the number of jumps in hypoxia-induced escape reaction in rats, suggesting a panicolytic-like effect. Repeated, but not acute, AMG administration (15mg/kg) also decreased nitrite levels and increased TRKB phosphorylation at residues Y706/7 in the dPAG. Notwithstanding the lack of AMG effect on total BDNF levels in that structure, the microinjection of the TRK antagonist K252a into the dPAG blocked the anti-escape effect of this drug in the ETM. Taken together our data suggest that the inhibition of NO production by AMG increased the levels of pTRKB, which is required for the panicolytic-like effect observed.

neuroscience↗