M.A. Maestro
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View article: Synthesis, Molecular Docking and Biological Evaluation of A-Ring-Carborane-Vitamin D Analogues
Synthesis, Molecular Docking and Biological Evaluation of A-Ring-Carborane-Vitamin D Analogues Open
The active form of vitamin D3, 1α,25-dihydroxyvitamin D3 (1,25D3), regulates a number of physiological and pathological processes, including cell proliferation and differentiation. Thousands of analogues of 1,25D3 have been developed with …
View article: Further Studies on the Highly Active Des-C-Ring and Aromatic-D-Ring Analogues of 1α,25-Dihydroxyvitamin D<sub>3</sub> (Calcitriol): Refinement of the Side Chain
Further Studies on the Highly Active Des-C-Ring and Aromatic-D-Ring Analogues of 1α,25-Dihydroxyvitamin D<sub>3</sub> (Calcitriol): Refinement of the Side Chain Open
Current efforts in the vitamin D field are directed toward the development of highly antiproliferative yet noncalcemic analogues of the natural hormone 1α,25-dihydroxyvitamin D3 (1,25D3). We have recently reported the…
View article: The Centennial Collection of VDR Ligands: Metabolites, Analogs, Hybrids and Non-Secosteroidal Ligands
The Centennial Collection of VDR Ligands: Metabolites, Analogs, Hybrids and Non-Secosteroidal Ligands Open
Since the discovery of vitamin D a century ago, a great number of metabolites, analogs, hybrids and nonsteroidal VDR ligands have been developed. An enormous effort has been made to synthesize compounds which present beneficial properties …
View article: The HASTER lncRNA promoter is a cis-acting transcriptional stabilizer of HNF1A
The HASTER lncRNA promoter is a cis-acting transcriptional stabilizer of HNF1A Open
View article: Design, Synthesis, Biological Activity, and Structural Analysis of Novel Des-C-Ring and Aromatic-D-Ring Analogues of 1α,25-Dihydroxyvitamin D<sub>3</sub>
Design, Synthesis, Biological Activity, and Structural Analysis of Novel Des-C-Ring and Aromatic-D-Ring Analogues of 1α,25-Dihydroxyvitamin D<sub>3</sub> Open
The toxic calcemic effects of the natural hormone 1α,25-dihydroxyvitamin D3 (1,25D3, 1,25-dihydroxycholecalciferol) in the treatment of hyperproliferative diseases demand the development of highly active and noncalcem…
View article: Pancreas agenesis mutations disrupt a lead enhancer controlling a developmental enhancer cluster
Pancreas agenesis mutations disrupt a lead enhancer controlling a developmental enhancer cluster Open
Sequence variants in cis-acting enhancers are important for polygenic disease, but their role in Mendelian disease is poorly understood. Redundancy between enhancers that regulate the same gene is thought to mitigate the pathogenic impact …
View article: REST is a major negative regulator of endocrine differentiation during pancreas organogenesis
REST is a major negative regulator of endocrine differentiation during pancreas organogenesis Open
Multiple transcription factors have been shown to promote pancreatic β-cell differentiation, yet much less is known about negative regulators. Earlier epigenomic studies suggested that the transcriptional repressor REST could be a suppress…
View article: <i>Hnf1b</i> -CreER causes efficient recombination of a Rosa26-RFP reporter in duct and islet δ cells
<i>Hnf1b</i> -CreER causes efficient recombination of a Rosa26-RFP reporter in duct and islet δ cells Open
The Hnf1b-CreERT2 BAC transgenic (Tg(Hnf1b-cre/ERT2)1Jfer) has been used extensively to trace the progeny of pancreatic ducts in developmental, regeneration, or cancer models. Hnf1b-CreERT2 transgenics h…
View article: Design, Synthesis, Evaluation and Structure of Allenic 1α,25‐Dihydroxyvitamin D<sub>3</sub> Analogs with Locked Mobility at C‐17
Design, Synthesis, Evaluation and Structure of Allenic 1α,25‐Dihydroxyvitamin D<sub>3</sub> Analogs with Locked Mobility at C‐17 Open
Vitamin D receptor ligands have potential for the treatment of hyperproliferative diseases and disorders related to the immune system. However, hypercalcemic effects limit their therapeutical uses and call for the development of tissue‐sel…
View article: <i>Hnf1b</i>-CreER causes efficient recombination of a Rosa26-RFP reporter in duct and islet δ cells
<i>Hnf1b</i>-CreER causes efficient recombination of a Rosa26-RFP reporter in duct and islet δ cells Open
The Hnf1b -CreER T2 BAC transgenic (Tg(Hnf1b-cre/ERT2)1Jfer) has been used extensively to trace the progeny of pancreatic ducts in developmental, regeneration, or cancer models. Hnf1b -CreER T2 transgenics have been used to show that cells…
View article: <i>HASTER</i> is a transcriptional stabilizer of <i>HNF1A</i>
<i>HASTER</i> is a transcriptional stabilizer of <i>HNF1A</i> Open
The biological purpose and disease relevance of long noncoding RNAs (lncRNAs) is poorly understood. We examined HASTER , a lncRNA antisense to HNF1A . Haploinsufficient mutations in HNF1A , encoding a homeodomain transcription factor, caus…
View article: Neonatal diabetes mutations disrupt a chromatin pioneering function that activates the human insulin gene
Neonatal diabetes mutations disrupt a chromatin pioneering function that activates the human insulin gene Open
Despite the central role of chromosomal context in gene transcription, human noncoding DNA variants are generally studied outside of their genomic location. This limits our understanding of disease-causing regulatory variants. INS promoter…
View article: REST is a major negative regulator of endocrine differentiation during pancreas organogenesis
REST is a major negative regulator of endocrine differentiation during pancreas organogenesis Open
SUMMARY Understanding genomic regulatory mechanisms of pancreas differentiation is relevant to the pathophysiology of diabetes mellitus, and to the development of replacement therapies. Numerous transcription factors promote β cell differe…
View article: The biliary epithelium gives rise to liver progenitor cells: RODRIGO-TORRES ET AL.
The biliary epithelium gives rise to liver progenitor cells: RODRIGO-TORRES ET AL. Open
Severe liver diseases are characterized by expansion of liver progenitor cells (LPC), which correlates with disease severity. However, the origin and role of LPC in liver physiology and in hepatic injury remains a contentious topic. We fou…
View article: Neonatal diabetes mutations disrupt a chromatin pioneering function that activates the human insulin gene
Neonatal diabetes mutations disrupt a chromatin pioneering function that activates the human insulin gene Open
Despite the central role of chromosomal context in gene transcription, human noncoding DNA variants are generally studied outside of their endogenous genomic location. This poses major limitations to understand the true consequences of cau…
View article: HNF1A recruits KDM6A to activate differentiated acinar cell programs that suppress pancreatic cancer
HNF1A recruits KDM6A to activate differentiated acinar cell programs that suppress pancreatic cancer Open
Defects in transcriptional regulators of pancreatic exocrine differentiation have been implicated in pancreatic tumorigenesis, but the molecular mechanisms are poorly understood. The locus encoding the transcription factor HNF1A harbors su…
View article: Microwave-Mediated Synthesis of N-allyl/Propargyl Derivatives: Enzymatic Analysis as a Potential Factor Xa (FXa) Inhibitor, Theoretical and Computational Molecular Docking
Microwave-Mediated Synthesis of N-allyl/Propargyl Derivatives: Enzymatic Analysis as a Potential Factor Xa (FXa) Inhibitor, Theoretical and Computational Molecular Docking Open
View article: 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
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 Open
The coagulation cascade is the process of the conversion of soluble fibrinogen to insoluble fibrin that terminates in production of a clot. Factor Xa (FXa) is a serine protease involved in the blood coagulation cascade. Moreover, FXa plays…
View article: CCDC 1830953: Experimental Crystal Structure Determination
CCDC 1830953: Experimental Crystal Structure Determination Open
View article: HNF1A recruits UTX to activate a differentiation program that suppresses pancreatic cancer
HNF1A recruits UTX to activate a differentiation program that suppresses pancreatic cancer Open
Defects in transcriptional regulators of pancreatic exocrine differentiation have been implicated in pancreatic tumorigenesis, but the molecular mechanisms are poorly understood. The locus encoding the transcription factor HNF1A harbors su…
View article: Vitamin D and Its Synthetic Analogs
Vitamin D and Its Synthetic Analogs Open
For many individuals, in particular during winter, supplementation with the secosteroid vitamin D3 is essential for the prevention of bone disorders, muscle weakness, autoimmune diseases, and possibly also different types of can…
View article: Aromatic-Based Design of Highly Active and Noncalcemic Vitamin D Receptor Agonists
Aromatic-Based Design of Highly Active and Noncalcemic Vitamin D Receptor Agonists Open
We report the design, synthesis, biological evaluation, and structural analysis of a new class of vitamin D analogues that possess an aromatic m-phenylene D-ring and an alkyl chain replacing the C-ring. A key feature of the synthetic strat…
View article: 1β,25-Dihydroxyvitamin D3: A new vitamin D metabolite in human serum
1β,25-Dihydroxyvitamin D3: A new vitamin D metabolite in human serum Open
View article: CCDC 1534334: Experimental Crystal Structure Determination
CCDC 1534334: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 999113: Experimental Crystal Structure Determination
CCDC 999113: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: <strong>Propargylic-Amines and Alcohols Through <em>anti</em>-Selective Mannich and Aldol Reactions</strong>
<strong>Propargylic-Amines and Alcohols Through <em>anti</em>-Selective Mannich and Aldol Reactions</strong> Open
Herein we present a practical and selective route to synthetically usefull propargylic amines and alcohols.[1] The key of both approaches is the combined use of an α,α-dialkylprolinol ether catalyst and a Brønsted acid that leads to adduct…
View article: Carborane-based design of a potent vitamin D receptor agonist
Carborane-based design of a potent vitamin D receptor agonist Open
The development of a promising clinical antitumor vitamin D analog possessing a side-chain o-carborane cluster that efficiently binds to VDR by unconventional dihydrogen bonding (BH⋯HN) is described.
View article: Pit-1 inhibits BRCA1 and sensitizes human breast tumors to cisplatin and vitamin D treatment
Pit-1 inhibits BRCA1 and sensitizes human breast tumors to cisplatin and vitamin D treatment Open
The POU class 1 homeobox 1 (POU1F1, also known as Pit-1), pertaining to the Pit-Oct-Unc (POU) family of transcription factors, has been related to tumor growth and metastasis in breast. However, its role in response to breast cancer therap…
View article: TEAD and YAP regulate the enhancer network of human embryonic pancreatic progenitors
TEAD and YAP regulate the enhancer network of human embryonic pancreatic progenitors Open