Chemical Biology & Drug Discovery Lab

*Vasquez D, *Lagos CF, Mella-Raipan J, Gonzalez L, Ebensperger R, Alvarez-Figueroa MJ, Saez E, Pessoa-Mahana H, Araya-Secchi R, Gonzalez-Wong A, Perez-Acle T, Pessoa-Mahana CD. 1-benzoyl-2-(2-nitrophenyl)-1H-benzimidazole derivatives: A novel approach to the development of new HIV-1 reverse transcriptase inhibitors. J Chil Chem Soc 2007, 52, 1281-1287. *Equally contributor authors

Colombres, M; Garate, JA; Lagos CF; Araya-Secchi R; Norambuena P, Quiroz S, Larrondo L, Perez-Acle T, Eyzaguirre J. An eleven amino acid residue deletion expands the substrate specificity of acetyl xylan esterase II (AXE II) from Penicillium purpurogenum. J Comput Aid Mol Des 2008, 22, 19-28.

Gonzalez, A; Duran, LS; Araya-Secchi, R; Garate, JA; Pessoa-Mahana, CD; Lagos, CF; Perez-Acle, T. Computational modeling study of functional microdomains in cannabinoid receptor type 1. Bioorgan Med Chem 2008, 16, 4378-89.

*Lagos CF, *Caballero J, Gonzalez-Nilo FD, Pessoa-Mahana CD, Perez-Acle T. Docking and quantitative structure-activity relationship studies for the bisphenylbenzimidazole family of non-nucleoside inhibitors of HIV-1 reverse transcriptase. Chem Biol Drug Des 2008, 72, 360-9. *Equally contributor authors

*Lizama C, *Lagos CF, *Lagos-Cabre R, Cantuarias L, Rivera F, Huenchunir P, Perez-Acle T, Carrion F, Moreno RD. Calpain inhibitors prevent p38 MAPK activation and germ cell apoptosis after heat stress in pubertal rat testes. J Cell Physiol 2009, 221:296-305. *Equally contributor authors

Chávez FP, Lagos CF, Reyes-Parada M, Guiliani N, Jerez CA. Polyphosphate Synthesis as a Target for Novel Antibiotics. Curr Enzym Inhib 2011 7(3): 163-168.

*Lagos CF, *Araya-Secchi R, Thomas P, Pérez-Acle T, Tapia RA, Salas CO. Molecular Modeling of Trypanosoma cruzi Glutamate Cysteine Ligase and Investigation of its Interactions with Glutathione. J Mol Model 2012 18(5):2055-2064. *Equally contributor authors

Carvajal CA, Campino C, Martinez-Aguayo A, Tichauer JE, Bancalari R, Trejo P, Aglony M, Baudrand R, Lagos CF, Mellado C, Garcia H, Fardella CE. A new presentation of the chimeric CYP11B1/CYP11B2 gene with low prevalence of primary aldosteronism and atypical gene segregation pattern. Hypertension 2012 59(1): 85-91.

Campino C, Quinteros H, Owen GI, Carvajal CA, Morales M, Olivieri O, Guidi G, Faccini G, Pasini F, Baudrand R, Padilla O, Valdivia C, Tichauer J, Lagos CF, Kalergis AM, Fardella CE. 11β-hydroxysteroid dehydrogenase type 2 polymorphisms and activity in a Chilean 2 essential hypertensive and normotensive cohort. Am J Hypert 2012 25(5):597-603.

Jara O, Acuña R, García I, Maripillán J, Figueroa V, Sáez JC, Araya-Secchi R, Lagos CF, Pérez-Acle T, Berthoud VM, Beyer EC, Martínez AD. Critical role of the first transmembrane domain of Cx26 in regulating oligomerization, function and permeability Mol Biol Cell 2012 23, 3299-3311.

Dussaillant C, Serrano V, Eyheramendi S, Smalley SV, Maiz A, Chavez M, Martinez JA, Cataldo LR, Lagos CF, Santos JL. APOA5 Q97x Mutation Identified through homozygosity mapping causes severe hypertriglyceridemia in a Chilean consanguineous family. BMC Med Genet 2012 13, 106.

Blanco EH, Lagos CF, Andrés ME, Gysling K. An Amphipathic Alpha-helix in the Prodomain of Cocaine and Amphetamine Regulated Transcript Peptide Precursor Serves as its Sorting Signal to the Regulated Secretory Pathway. Plos One 2013 8(3):e59695.

Mella-Raipán J, Lagos CF, Recabarren-Gajardo G, Espinosa-Bustos C, Romero-Parra J, Pessoa-Mahana H, Iturriaga-Vásquez P, Pessoa-Mahana CD. Design, Synthesis, Binding and Docking-Based 3D-QSAR Studies of 2-Pyridylbenzimidazoles-A New Family of High Affinity CB1 Cannabinoid Ligands. Molecules 2013 18(4):3972-4001.

Vecchiola A, Lagos CF, Fuentes CA, Allende F, Campino C, Valdivia C, Tapia A, Ogishima T, Mukai K, Owen GI, Solari S, Carvajal CA, Fardella CE. Inhibitory effects of sex steroids on chimeric and wild type aldosterone synthase in vitro. Reprod Biol Endocrin 2013 11:76.

Allende, F.; Solari, S; Campino, C; Carvajal, CA; Lagos, CF; Vecchiola, A; Valdivia, C; Baudrand, R; Owen, GI; Fardella, CE. LC–MS/MS Method for the Simultaneous Determination of Free Urinary Steroids. Chromatographia 2014, 77:637-642.

Ocaranza MP, Michea L, Chiong M, Lagos CF, Lavandero S, Jalil JE. Recent insights and therapeutic perspectives of angiotensin-(1-9) in the cardiovascular system. Clinical Science 2014, 127(9): 549-557.

Cortes, VA; Smalley, SV; Goldenberg, D; Lagos, CF; Hodgson, MI; Santos, JL. Divergent Metabolic Phenotype between Two Sisters with Congenital Generalized Lipodystrophy Due to Double AGPAT2 Homozygous Mutations. A Clinical, Genetic and In Silico Study. PLoS One 2014, 9, e87173.

González, PM; Lagos, CF; Ward, WC; Polli, JE. Structural requirements of the human sodium-dependent bile acid transporter (hASBT): Role of 3- and 7-OH moieties on binding and translocation of bile acids. Mol Pharm 2014, 11 (2): 588-598.

Tapia-Castillo, A; Carvajal, CA; Campino, C; Vecchiola, A; Allende, F; Solari, S; Garcia, L; Lavanderos, S; Valdivia, C; Fuentes, C; Lagos, CF; Martinez-Aguayo, A; Baudrand, R; Aglony, M; Garcia, H; Fardella, CE. Polymorphisms in the RAC1 Gene Are Associated With Hypertension Risk Factors in a Chilean Pediatric Population. Am J Hypertens 2014, 27, 299-307.

Lagos, CF; Vecchiola, A; Allende, F; Fuentes, CA; Tichauer, JE; Solari, S; Campino, C; Tapia-Castillo, A; Baudrand, R; Villarroel, P; Cifuentes, M; Owen, GI; Carvajal, CA; Fardella, CE. Identification of novel 11beta-HSD1 inhibitors by combined ligand- and structure-based virtual screening. Mol Cell Endocrinol 2014, 384: 71-82.

Tapia-Castillo, A.; Carvajal, C. A.; Campino, C.; Hill, C.; Allende, F.; Vecchiola, A.; Carrasco, C.; Bancalari, R.; Valdivia, C.; Lagos, CF; Martinez-Aguayo, A.; Garcia, H.; Aglony, M.; Baudrand, R. F.; Kalergis, A. M.; Michea, L. F.; Riedel, C. A.; Fardella, C. E. The Expression of RAC1 and Mineralocorticoid Pathway-Dependent Genes are Associated With Different Responses to Salt Intake. Am J Hypertens 2015 28(6): 722-728.

. Campino C, Trejo P, Carvajal CA, Vecchiola A, Valdivia C, Fuentes CA, Delgado JF, Lagos CF, Aglony M, Carrasco C, Martinez-Aguayo A, García H, Loureiro C, Fardella CE. Pregnancy normalized familial hyperaldosteronism type I: a novel role for progesterone? J Hum Hypertens. 2015, 29 (2), 138-9.

Espinosa-Bustos, C; Lagos, CF; Romero-Parra, J; Zárate A. M.; Mella-Raipán, J.; Recabarren-Gajardo, G.; Pessoa-Mahana, H.; Iturriaga-Vásquez, P.; Tapia, R. A.; Pessoa-Mahana, CD. Design, synthesis, biological evaluation and binding mode modeling of benzimidazole derivatives targeting Cannabinoid Receptor Type 1. Arch. Pharm. Chem. Life Sci. 2015, 348, 81-88.

De la Fuente-Ortega, E; Gravotta, D; Bay, AP; Benedicto, I; Carvajal-Gonzalez, JM; Lehmann, G; Lagos, CF & Rodríguez-Boulan, E. Basolateral Sorting of Chloride Channel 2 is Mediated by Interactions Between a Dileucine Motif and the Clathrin Adaptor AP-1. Mol Biol Cell 2015, 26, 1728-1742. *Portada de Revista.

Smalley, SV; Preiss, Y; Suazo, J; Vega, JA; Angellotti, I; Lagos, CF; Rivera, E; Kleinsteuber, K; Campion, J; Martínez, JA; Maiz, A & Santos, JL. Novel splice-affecting variants in CYP27A1 gene in two Chilean patients with Cerebrotendinous Xanthomatosis. Genetics and Molecular Biology 2015, 38, 30-36. *Portada de Revista.

Valdivia-Pizarro, C; Carvajal, CA; Campino, C; Allende, F; Martinez-Aguayo, A; Baudrand, RF; Vecchiola, A; Lagos, CF; Tapia-Castillo, A; Fuentes, CA; Aglony, M; Solari, S; Kalergis, AM; Garcia, H; Fardella, CE. Citosine-Adenine repeat microsatellite of HSD11B2 gene in hypertensive children. Am J Hypertens 2016, 29, 25-32.

Vecchiola, A; Lagos, CF; Carvajal, CA; Baudrand, R & Fardella, CE. Aldosterone production and signaling dysregulation in obesity. Current Hypertension Reports 2016, 18, 20-29.

Vecchiola A, Fuentes, CA; Muñoz-Durango, N; Tapia-Castillo, A; González-Gómez, LM; Baudrand, R; Carvajal CA; Campino, C; Kalergis, AM; Lagos, CF & Fardella, CE. Aldosterone and IL-17 in the genesis of mineralocorticoid arterial hypertension: an ex vivo study. Rev Chil Endocrinol Diabetes 2016, 9(1):19-26.

Bravo-Toncio, C.; Alvarez, JA; Campos, F; Ortíz-Severín, J; Varas, M; Cabrera, R; Lagos, CF & Chávez FP. Dictyostelium discoideum as a surrogate host-microbe model for antivirulence screening in Pseudomonas aeruginosa PAO1. Int J Antimicrob Agents 2016, 47(5): 403-409.

Martinez-Aguayo, A; Campino, C; Baudrand, R; Carvajal, CA; García, H; Aglony, M; Bancalari, R; García, L; Loureiro, C; Vecchiola, A; Tapia-Castillo, A; Valdivia, C; Sanhueza, S; Fuentes, CA; Lagos, CF; Solari, S; Allende, F; Kalergis, AM; Fardella, CE. Cortisol/cortisone ratio and matrix metalloproteinase-9 activity are associated with pediatric primary hypertension. J Hypertens 2016, 34:1808–1814.

*Vera, G.; *Lagos, CF; Almendras, S.; Hebel, D.; Flores, F.; Valle-Corvalán, G.; Pessoa-Mahana, C.; Mella-Raipán, J.; Montecinos, R.; Recabarren-Gajardo, G., Extended N-Arylsulfonylindoles as 5-HT6 Receptor Antagonists: Design, Synthesis & Biological Evaluation. Molecules 2016, 21 (8), 1070. *Equally contributor authors

Campino, C.; Hill, C.; Baudrand, R.; Martinez-Aguayo, A.; Aglony, M.; Carrasco, C. A.; Ferrada, C.; Loureiro, C.; Vecchiola, A.; Bancalari, R.; Grob, F.; Carvajal, C. A.; Lagos, CF; Valdivia, C.; Tapia-Castillo, A.; Fuentes, C. A.; Mendoza, C.; Garcia, H.; Uauy, R.; Fardella, C. E., Usefulness and Pitfalls in Sodium Intake Am J Hypertens 2016, 29(10):1212-1217. doi: 10.1093/ajh/hpw056

Bashamboo, A.; Donohoue, P. A.; Vilain, E.; Rojo, S.; Calvel, P.; Seneviratne, S. N.; Buonocore, F.; Barseghyan, H.; Bingham, N.; Rosenfeld, J. A.; Mulukulta, S. N.; Jain, M.; Burrage, L.; Dhar, S.; Balasubramanyam, A.; Lee, B.; UDN, M. o.; Eozenou, C.; Suntharalingham, JP; de Silva, K.; Lin, L.; Bignon-Topalovic, J.; Poulat, F.; Lagos, CF; McElreavey, K.; Achermann, J. C., A recurrent p.Arg92Trp variant in steroidogenic factor-1 (NR5A1) can act as a molecular switch in human sex development. Human Molecular Genetics 2016, 25(16): 3446-3453.

Nuñez-Navarro, NE; Segovia, GF; Burgos, RA; Lagos, CF; Fuentes-Ibacache, N; Faúndez, MA; Zacconi, FM. Microwave Assisted Synthesis of Novel Six-Membered 4-C, 4-O and 4-S Lactams Derivatives: Characterization and in vitro Biological Evaluation of Cytotoxicity and Anticoagulant Activity. J. Braz. Chem. Soc. 2017, 28 (2), 203-207. doi : 10.21577/0103-5053.20160292 *Portada de Revista

Vargas AA, Cisterna BA, Saavedra-Leiva F, Urrutia C, Cea LA, Vielma A, Gutierrez-Maldonado SE, Martin AJ, Pareja-Barrueto C, Escalona Y, Schmachtenberg O, Lagos CF, Pérez-Acle T and Sáez JC.On Biophysical Properties and Sensitivity to Gap Junction Blockers of Connexin 39 Hemichannels Expressed in HeLa Cells. Front. Physiol. 2017, 8:38. doi: 10.3389/fphys.2017.00038

Apablaza G, Montoya L, Morales-Verdejo C, Mellado M, Cuellar M, Lagos CF, Soto-Delgado J, Chung H, Pessoa-Mahana CD, Mella J. 2D-QSAR and 3D-QSAR/CoMSIA Studies on a Series of (R)-2-((2-(1H-Indol-2-yl)ethyl)amino)-1-Phenylethan-1-ol with Human beta(3)-Adrenergic Activity. Molecules 2017, 22 (3): 404. doi:10.3390/molecules22030404

Romero-Parra J, Chung H, Tapia RA, Faúndez M, Morales-Verdejo C, Lorca M, Lagos CF, Di Marzo V, David Pessoa-Mahana C, Mella-Raipán J. Combined CoMFA and CoMSIA 3D-QSAR study of benzimidazole and benzothiophene derivatives with selective affinity for the CB2 cannabinoid receptor. Eur J Pharm Sci. 2017, 28;101:110. doi: 10.1016/j.ejps.2017.01.037

Mella J, Villegas F, Morales-Verdejo C, Lagos, CF, Recabarren-Gajardo G. Structure-activity relationships studies on weakly basic N-arylsulfonylindoles with an antagonistic profile in the 5-HT6 receptor. Journal of Molecular Structure 2017, 1139, 362-370. Doi: 10.1016/j.molstruc.2017.03.067

Kyriakakis, N; Shonibare, T; Kyaw-Tun, J. Lynch, J; Lagos, CF; Achermann, JC; Murray, RD. Late-onset X-linked adrenal hypoplasia (DAX-1, NR0B1): two new adult-onset cases from a single center. Pituitary 2017, 20:585-593 doi: 10.1007/s11102-017-0822-x

Lagos, CF; Segovia, GE; Nuñez-Navarro, N; Faúndez, MA; Zacconi, FC. Novel FXa Inhibitor Identification through Integration of Ligand- and Structure-Based Approaches. Molecules 2017, 22(10): 1588. doi:10.3390/molecules22101588

Slater, PG; Gutierrez-Maldonado, SE; Gysling, K; Lagos CF. Molecular modeling of structures and interaction of human CFR binding protein and CRF type-2 receptor. Frontiers in Endocrinology. 2018, 9:43. doi:10.3389/fendo.2018.00043

Carvajal, CA; Tapia-Castillo, A; Valdivia, CP; Allende, F; Solari, S; Lagos, CF.; Campino, C; Martínez-Aguayo, A; Vecchiola, A.; Pinochet, C.; Godoy, C.; Iturrieta, V.; Baudrand, R.; Fardella, C. E. Serum Cortisol and Cortisone as Potential Biomarkers of Partial 11β-Hydroxysteroid Dehydrogenase Type 2 Deficiency. American Journal of Hypertension 2018, 31, 910-918. https://doi.org/10.1093/ajh/hpy051

Campino, C.; Baudrand, R.; Valdivia, C. A.; Carvajal, C.; Vecchiola, A.; Tapia-Castillo, A.; Martínez-Aguayo, A.; Garcia, H.; García, L.; Allende, F.; Solari, S.; Fuentes, C. A.; Lagos, C. F.; Rojas, M. P.; Muñoz, D.; Fardella, C. E. Sodium Intake Is associated With Endothelial Damage Biomarkers and Metabolic Dysregulation. American Journal of Hypertension 2018, 31, 1127-1132. https://doi.org/10.1093/ajh/hpy097

Diethelm, B; Lagos, CF; Recabarren-Gajardo, G. 1-Adamantylamidoxime. Molbank 2018, (2):M992. https://doi.org/10.3390/M992

Tapia-Castillo, A.; Baudrand, R.; Vaidya, A.; Campino, C.; Allende, F.; Valdivia, C.; Vecchiola, A.; Lagos, C.F.; Fuentes, C.; Solari, S.; Martínez –Aguayo, A.; García, H.; Carvajal, C. A.; Fardella, C. Clinical, Biochemical and Genetic Characteristics of “Non-Classical” Apparent Mineralocorticoid Excess Syndrome. J Clin Endocr Metab 2019, 104: 595-603. https://doi.org/10.1210/jc.2018-01197

Tobar, HE; Cataldo, LR; González, T; Rodríguez, R; Serrano, V; Arteaga, A; Álvarez-Mercado, A; Lagos, CF; Vicuña, L; Miranda, JP; Pereira, A; Bravo, C; Aguilera, CM; Eyheramendy, S; Uauy, R; Martínez, A; Gil, P; Francone, O; Rigotti, A; Santos, JL.Identification and functional analysis of missense mutations in the lecithin cholesterol acyltransferase gene in a Chilean patient with hypoalphalipoproteinemia. Lipids in Health and Disease 2019, 18:132. https://doi.org/10.1186/s12944-019-1045-0

Campos, F; Álvarez, JA; Ortíz-Severín, J; Varas, MA; Lagos, CF; Cabrera, R; Álvarez, RA; Chávez FP. Fluorescence enzymatic assay for bacterial polyphosphate kinase 1 (PPK1) as a platform for screening antivirulence molecules. Infection and Drug Resistance 2019, 12:2237-2242. https://doi.org/10.2147/IDR.S181906

Buonocore, F.; Clifford-Mobley, O.; King, TFJ.; Striglioni, N.; Man, E.; Suntharalingham, JP.; del Valle, I.; Lin, L.; Lagos, CF.; Rumsby, G.; Conway, G. S.; Achermann, J. C. Next generation sequencing reveals novel genetic variants (SRY, DMRT1, NR5A1, DHH, DHX37) in adults with 46,XY DSD. Journal of the Endocrine Society 2019. js.2019-00306. https://doi.org/10.1210/js.2019-00306

Arteaga, E.; Valenzuela, F.; Lagos, CF; Lagos, M.; Martinez, A.; Baudrand, R.; Carvajal, C.; Fardella, CE. Detection of a novel severe mutation affecting the CYP21A2 gene in a Chilean male with salt wasting congenital adrenal hyperplasia. Endocrine 2020, 67, 258-263. https://doi.org/10.1007/s12020-019-02097-3

Santana-Romo, F.; Lagos, CF.; Duarte, Y.; Castillo, F.; Moglie, Y.; Maestro, MA.; Charbe, N.; Zacconi, FC. Innovative Three-Step Microwave-Promoted Synthesis of N-Propargyltetrahydroquinoline and 1,2,3-Triazole Derivatives as a Potential Factor Xa (FXa) Inhibitors: Drug Design, Synthesis, and Biological Evaluation. Molecules 2020, 25, 491. https://doi.org/10.3390/molecules25030491

Cisterna, BA.; Vargas, AA.; Puebla, C; Fernández, P.; Escamilla, R.; Lagos, CF.; Matus, MF.; Vilos, C.; Cea, LA.; Barnafi, E.; Gaete, H.; Escobar, DF.; Cardozo, CP.; Sáez, JC. Active acetylcholine receptors prevent the atrophy of skeletal muscles and favor reinnervation. Nature Communications 2020, 11, 1073. https://doi.org/10.1038/s41467-019-14063-8

Vecchiola, A.; Fuentes, C. A.; Solar, I.; Lagos, CF.; Opazo, MC.; Muñoz-Durango, N.; Riedel, CA.; Owen, G. I.; Kalergis, A. M.; Fardella, C. E. Eplerenone Implantation Improved Adipose Dysfunction Averting RAAS Activation and Cell Division. Frontiers in Endocrinology 2020, 11. https://doi.org/10.3389/fendo.2020.00223

Arrieta-Rodríguez, L; Espinoza-Rosales, D; Vera, G; Cho, YH; Cabezas, D; Vásquez-Velásquez, D; Mella-Raipán, J; Lagos, CF; Recabarren-Gajardo, G. Novel N-Arylsulfonylindoles Targeted as Ligands of the 5-HT6 Receptor. Insights on the Influence of C-5 Substitution on Ligand Affinity. Pharmaceuticals 2021, 14, 528. https://doi.org/10.3390/ph14060528

Vecchiola, A.; Fuentes, C. A.; Carvajal, C. A.; Campino, C.; Allende, F.; Tapia-Castillo, A.; Lagos, C. F.; Fardella, C. E. Testosterona inhibe la actividad de la aldosterona sintasa silvestre y quimérica in vitro. Revista Médica de Chile; 2021, 149(11). http://dx.doi.org/10.4067/S0034-98872021001101539

McGlacken-Byrne, S. M., I. Del Valle, P. L. Quesne Stabej, L. Bellutti, L. Garcia-Alonso, L. A. Ocaka, M. Ishida, J. P. Suntharalingham, A. Gagunashvili, O. K. Ogunbiyi, T. Mistry, F. Buonocore, B. Crespo, N. Moreno, P. Niola, T. Brooks, C. E. Brain, M. T. Dattani, D. Kelberman, R. Vento-Tormo, C. F. Lagos, G. Livera, G. S. Conway and J. C. Achermann. Pathogenic variants in the human m6A reader YTHDC2 are associated with primary ovarian insufficiency. JCI Insight 2022, 7 (5). https://doi.org/10.1172/jci.insight.154671