List of works - Valeria La Pietra

A more detailed picture of the interactions between virtual screening-derived hits and the DNA G-quadruplex: NMR, molecular modelling and ITC studies

scientific article published on 30 May 2011

A novel cell-permeable, selective, and noncompetitive inhibitor of KAT3 histone acetyltransferases from a combined molecular pruning/classical isosterism approach.

scientific article

A stereoselective approach to peptidomimetic BACE1 inhibitors.

scientific article published on 6 October 2013

Apoptosis therapy in cancer: the first single-molecule co-activating p53 and the translocator protein in glioblastoma.

scientific article published on 23 April 2014

Arylsulfonamide inhibitors of aggrecanases as potential therapeutic agents for osteoarthritis: synthesis and biological evaluation

scientific article

Computer-Aided Identification and Lead Optimization of Dual Murine Double Minute 2 and 4 Binders: Structure-Activity Relationship Studies and Pharmacological Activity

scientific article published on 18 September 2017

Design, synthesis, and biological evaluation of 1-phenylpyrazolo[3,4-e]pyrrolo[3,4-g]indolizine-4,6(1H,5H)-diones as new glycogen synthase kinase-3β inhibitors

scientific article

Discovery of covalent inhibitors of glyceraldehyde-3-phosphate dehydrogenase, a target for the treatment of malaria

scientific article

Exploring the N-Terminal Region of C-X-C Motif Chemokine 12 (CXCL12): Identification of Plasma-Stable Cyclic Peptides As Novel, Potent C-X-C Chemokine Receptor Type 4 (CXCR4) Antagonists

scientific article

Human recombinant beta-secretase immobilized enzyme reactor for fast hits' selection and characterization from a virtual screening library

scientific article

Identification of glycogen synthase kinase-3 inhibitors with a selective sting for glycogen synthase kinase-3α.

scientific article published on May 2012

Identification of novel molecular scaffolds for the design of MMP-13 inhibitors: A first round of lead optimization

article

Lead Optimization of 2-Phenylindolylglyoxylyldipeptide Murine Double Minute (MDM)2/Translocator Protein (TSPO) Dual Inhibitors for the Treatment of Gliomas

scientific article

Long lasting inhibition of Mdm2-p53 interaction potentiates mesenchymal stem cell differentiation into osteoblasts

scientific article published on 28 January 2019

N-O-Isopropyl Sulfonamido-Based Hydroxamates: Design, Synthesis and Biological Evaluation of Selective Matrix Metalloproteinase-13 Inhibitors as Potential Therapeutic Agents for Osteoarthritis

article

N-O-Isopropyl sulfonamido-based hydroxamates: Kinetic characterisation of a series of MMP-12/MMP-13 dual target inhibitors

scientific article published in 2012

Non-nucleoside inhibitors of human adenosine kinase: synthesis, molecular modeling, and biological studies.

scientific article published on 14 February 2011

Novel peptidomimetics as BACE-1 inhibitors: Synthesis, molecular modeling, and biological studies

scientific article published on 14 November 2012

Potent arylsulfonamide inhibitors of tumor necrosis factor-alpha converting enzyme able to reduce activated leukocyte cell adhesion molecule shedding in cancer cell models

scientific article

Progresses in the pursuit of aldose reductase inhibitors: The structure-based lead optimization step

scientific article published on 05 March 2012

Protein flexibility in virtual screening: the BACE-1 case study

scientific article

Receptor-Bound Conformation of Cilengitide Better Represented by Its Solution-State Structure than the Solid-State Structure

scientific article published on 22 September 2014

Selective arylsulfonamide inhibitors of ADAM-17: hit optimization and activity in ovarian cancer cell models

scientific article published on 4 October 2013

Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme.

scientific article

State-of-the-art methodologies for the discovery and characterization of DNA G-quadruplex binders.

scientific article published on January 2012

Structure-based lead optimization and biological evaluation of BAX direct activators as novel potential anticancer agents.

scientific article published on 25 February 2015

Structure-based optimization of tyrosine kinase inhibitor CLM3. Design, synthesis, functional evaluation, and molecular modeling studies

scientific article published on 5 February 2014

Synthesis and biological evaluation in U87MG glioma cells of (ethynylthiophene)sulfonamido-based hydroxamates as matrix metalloproteinase inhibitors

scientific article published on 2 April 2011

p53 functional inhibitors behaving like pifithrin-β counteract the Alzheimer peptide non-β-amyloid component effects in human SH-SY5Y cells

scientific article published on 28 March 2014

List of works by Valeria La Pietra

A more detailed picture of the interactions between virtual screening-derived hits and the DNA G-quadruplex: NMR, molecular modelling and ITC studies

A novel cell-permeable, selective, and noncompetitive inhibitor of KAT3 histone acetyltransferases from a combined molecular pruning/classical isosterism approach.

A stereoselective approach to peptidomimetic BACE1 inhibitors.

Apoptosis therapy in cancer: the first single-molecule co-activating p53 and the translocator protein in glioblastoma.

Arylsulfonamide inhibitors of aggrecanases as potential therapeutic agents for osteoarthritis: synthesis and biological evaluation

Computer-Aided Identification and Lead Optimization of Dual Murine Double Minute 2 and 4 Binders: Structure-Activity Relationship Studies and Pharmacological Activity

Design, synthesis, and biological evaluation of 1-phenylpyrazolo[3,4-e]pyrrolo[3,4-g]indolizine-4,6(1H,5H)-diones as new glycogen synthase kinase-3β inhibitors

Discovery of covalent inhibitors of glyceraldehyde-3-phosphate dehydrogenase, a target for the treatment of malaria

Exploring the N-Terminal Region of C-X-C Motif Chemokine 12 (CXCL12): Identification of Plasma-Stable Cyclic Peptides As Novel, Potent C-X-C Chemokine Receptor Type 4 (CXCR4) Antagonists

Human recombinant beta-secretase immobilized enzyme reactor for fast hits' selection and characterization from a virtual screening library

Identification of glycogen synthase kinase-3 inhibitors with a selective sting for glycogen synthase kinase-3α.

Identification of novel molecular scaffolds for the design of MMP-13 inhibitors: A first round of lead optimization

Lead Optimization of 2-Phenylindolylglyoxylyldipeptide Murine Double Minute (MDM)2/Translocator Protein (TSPO) Dual Inhibitors for the Treatment of Gliomas

Long lasting inhibition of Mdm2-p53 interaction potentiates mesenchymal stem cell differentiation into osteoblasts

N-O-Isopropyl Sulfonamido-Based Hydroxamates: Design, Synthesis and Biological Evaluation of Selective Matrix Metalloproteinase-13 Inhibitors as Potential Therapeutic Agents for Osteoarthritis

N-O-Isopropyl sulfonamido-based hydroxamates: Kinetic characterisation of a series of MMP-12/MMP-13 dual target inhibitors

Non-nucleoside inhibitors of human adenosine kinase: synthesis, molecular modeling, and biological studies.

Novel peptidomimetics as BACE-1 inhibitors: Synthesis, molecular modeling, and biological studies

Potent arylsulfonamide inhibitors of tumor necrosis factor-alpha converting enzyme able to reduce activated leukocyte cell adhesion molecule shedding in cancer cell models

Progresses in the pursuit of aldose reductase inhibitors: The structure-based lead optimization step

Protein flexibility in virtual screening: the BACE-1 case study

Receptor-Bound Conformation of Cilengitide Better Represented by Its Solution-State Structure than the Solid-State Structure

Selective arylsulfonamide inhibitors of ADAM-17: hit optimization and activity in ovarian cancer cell models

Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme.

State-of-the-art methodologies for the discovery and characterization of DNA G-quadruplex binders.

Structure-based lead optimization and biological evaluation of BAX direct activators as novel potential anticancer agents.

Structure-based optimization of tyrosine kinase inhibitor CLM3. Design, synthesis, functional evaluation, and molecular modeling studies

Synthesis and biological evaluation in U87MG glioma cells of (ethynylthiophene)sulfonamido-based hydroxamates as matrix metalloproteinase inhibitors

p53 functional inhibitors behaving like pifithrin-β counteract the Alzheimer peptide non-β-amyloid component effects in human SH-SY5Y cells