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Xerardo Garcia-Mera

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Articles 70
Citations 345
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Recent Articles
1.
Silva-Reis S, Costa V, da Silva D, Pereira D, Correia X, Garcia-Mera X, et al.
RSC Med Chem . 2024 Sep; PMID: 39290380
Neurodegenerative disorders comprise a series of heterogeneous conditions that affect millions of people worldwide, representing a significant health burden in both developed and developing countries. Without disease-modifying treatments currently available,...
2.
Prieto-Diaz R, Fojo-Carballo H, Majellaro M, Tandaric T, Azuaje J, Brea J, et al.
Biomed Pharmacother . 2024 Mar; 173:116345. PMID: 38442670
Antagonists of the A adenosine receptor have recently emerged as targeted anticancer agents and immune checkpoint inhibitors within the realm of cancer immunotherapy. This study presents a comprehensive evaluation of...
3.
Silva-Reis S, Costa V, da Silva D, Pereira D, Correia X, Costa-Almeida H, et al.
Eur J Med Chem . 2024 Feb; 267:116174. PMID: 38306884
Neurodegenerative disorders of the central nervous system (CNS) such as Alzheimer's and Parkinson's diseases, afflict millions globally, posing a significant public health challenge. Despite extensive research, a critical hurdle in...
4.
Silva-Reis S, Correia X, Costa-Almeida H, Pires-Lima B, Maronde D, Costa V, et al.
ACS Med Chem Lett . 2023 Dec; 14(12):1656-1663. PMID: 38116429
This work describes the synthesis and pharmacological and toxicological evaluation of melanostatin (MIF-1) bioconjugates with amantadine (Am) via a peptide linkage. The data from the functional assays at human dopamine...
5.
Gioe-Gallo C, Ortigueira S, Brea J, Raich I, Azuaje J, Rita Paleo M, et al.
Biomed Pharmacother . 2023 May; 164:114934. PMID: 37236027
Synthetic cannabinoid receptor agonists (SCRAs) constitute the largest and most defiant group of abuse designer drugs. These new psychoactive substances (NPS), developed as unregulated alternatives to cannabis, have potent cannabimimetic...
6.
Silva-Reis S, Sampaio-Dias I, Costa V, Correia X, Costa-Almeida H, Garcia-Mera X, et al.
ACS Chem Neurosci . 2023 Feb; 14(4):554-572. PMID: 36735764
Neurodegenerative diseases of the central nervous system (CNS) pose a serious health concern worldwide, with a particular incidence in developed countries as a result of life expectancy increase and the...
7.
Prieto-Diaz R, Gonzalez-Gomez M, Fojo-Carballo H, Azuaje J, El Maatougui A, Majellaro M, et al.
J Med Chem . 2022 Dec; 66(1):890-912. PMID: 36517209
The modulation of the A adenosine receptor is a promising strategy in cancer (immuno) therapy, with AAR antagonists emerging as immune checkpoint inhibitors. Herein, we report a systematic assessment of...
8.
Tay A, Prieto-Diaz R, Neo S, Tong L, Chen X, Carannante V, et al.
J Immunother Cancer . 2022 May; 10(5). PMID: 35580926
Background: Adenosine is a metabolite that suppresses antitumor immune response of T and NK cells via extracellular binding to the two subtypes of adenosine-2 receptors, AARs. While blockade of the...
9.
Miranda-Pastoriza D, Bernardez R, Azuaje J, Prieto-Diaz R, Majellaro M, Tamhankar A, et al.
ACS Med Chem Lett . 2022 Feb; 13(2):243-249. PMID: 35178181
A library of potent and highly AAR selective pyrimidine-based compounds was designed to explore non-orthosteric interactions within this receptor. Starting from a prototypical orthosteric AAR antagonist (ISVY130), the structure-based design...
10.
Val C, Rodriguez-Garcia C, Prieto-Diaz R, Crespo A, Azuaje J, Carbajales C, et al.
J Med Chem . 2022 Jan; 65(3):2091-2106. PMID: 35068155
We herein document a large collection of 108 2-amino-4,6-disubstituted-pyrimidine derivatives as potent, structurally simple, and highly selective AAR ligands. The most attractive ligands were confirmed as antagonists of the canonical...