A. Testa

发表

New Molecular and Therapeutic Insights into Canine Diffuse Large B Cell Lymphoma Elucidates the Role of the Dog As a Model for Human Disease

L. Cascione, E. Gaudio, M. Milan, 2018, Blood.

3-Fluoro-4-hydroxyprolines: Synthesis, Conformational Analysis, and Stereoselective Recognition by the VHL E3 Ubiquitin Ligase for Targeted Protein Degradation

A. Ciulli, X. Lucas, A. Runcie, 2018, Journal of the American Chemical Society.

Translating PROTAC chemical series optimization into functional outcomes underlying BRD7 and BRD9 protein degradation

D. Daniels, M. Urh, Kristin M. Riching, 2021, Current Research in Chemical Biology.

Development of BromoTag: A “Bump-and-Hole”–PROTAC System to Induce Potent, Rapid, and Selective Degradation of Tagged Target Proteins

D. Alessi, J. Blow, Thomas Macartney, 2021, Journal of medicinal chemistry.

Trivalent PROTACs enhance protein degradation via combined avidity and cooperativity

Nancy Murphy, D. Daniels, M. Urh, 2021, Nature Chemical Biology.

Understanding and Improving the Membrane Permeability of VH032-Based PROTACs

Chad E. Townsend, R. Lokey, A. Ciulli, 2020, ACS medicinal chemistry letters.

Design and Characterization of SGK3-PROTAC1, an Isoform Specific SGK3 Kinase PROTAC Degrader

D. Alessi, N. Shpiro, A. Ciulli, 2019, ACS chemical biology.

Cereblon versus VHL: Hijacking E3 ligases against each other using PROTACs

A. Ciulli, A. Testa, Chiara Maniaci, 2019, Bioorganic & medicinal chemistry.

Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds

A. Ciulli, A. Testa, Kwok-Ho Chan, 2017, Journal of medicinal chemistry.

Improved synthesis of the hypoxia probe 5-deutero-5-fluoro-5-deoxy- azomycin arabinoside (FAZA) as a model process for tritium radiolabeling

M. Zanda, A. Testa, C. Zanato, 2013 .

The rise and rise of protein degradation: opportunities and challenges ahead.

A. Testa, I. Churcher, S. Hughes, 2021, Drug discovery today.

Cereblon versus VHL: Hijacking E3 Ligases Against Each Other Using PROTACs

A. Ciulli, A. Testa, Chiara Maniaci, 2019 .

PET Tracers To Study Clinically Relevant Hepatic Transporters.

M. Zanda, C. Elmore, A. Testa, 2015, Molecular pharmaceutics.

Structure‐Based Design of a Macrocyclic PROTAC

A. Ciulli, X. Lucas, A. Testa, 2019, Angewandte Chemie.

High‐Affinity “Click” RGD Peptidomimetics as Radiolabeled Probes for Imaging αvβ3 Integrin

M. Mori, K. Williams, M. Piras, 2017, ChemMedChem.

Trivalent PROTACs enhance protein degradation through cooperativity and avidity

Nancy Murphy, D. Daniels, M. Urh, 2020 .

Development of NanoLuc-targeting protein degraders and a universal reporter system to benchmark tag-targeted degradation platforms

J. Silke, Ngee Kiat Chua, S. A. Cobbold, 2022, Nature Communications.

Optimization of a “bump-and-hole” approach to allele-selective BET bromodomain inhibition† †Electronic supplementary information (ESI) available: Supplemental results (Fig. S1–S13 and Tables S1–S10). Crystallography data collection and refinement statistics. Experimental section. Detailed compound s

K. Read, A. Ciulli, M. Baud, 2018, Chemical science.

Stereoselective synthesis of allele-specific BET inhibitors.

A. Ciulli, A. Testa, A. Bond, 2020, Organic & biomolecular chemistry.

Diastereoselective protocols for the synthesis of 2,3-trans- and 2,3-cis-6-methoxy-morpholine-2-carboxylic acid derivatives.

M. L. Gelmi, A. Testa, S. Pellegrino, 2012, The Journal of organic chemistry.

Design and Synthesis of an RGD Peptidomimetic-Paclitaxel Conjugate Targeting αvβ3 Integrin for Tumour-Directed Drug Delivery

M. Piras, M. Zanda, A. Testa, 2017, Synlett.

Structural basis of PROTAC cooperative recognition for selective protein degradation

D. Lamont, A. Ciulli, X. Lucas, 2017, Nature chemical biology.

Iterative Design and Optimization of Initially Inactive Proteolysis Targeting Chimeras (PROTACs) Identify VZ185 as a Potent, Fast, and Selective von Hippel–Lindau (VHL) Based Dual Degrader Probe of BRD9 and BRD7

M. Koegl, D. Daniels, Kristin M. Riching, 2018, Journal of medicinal chemistry.

The bromodomain and extra-terminal domain degrader MZ1 exhibits preclinical anti-tumoral activity in diffuse large B-cell lymphoma of the activated B cell-like type

L. Cascione, A. Stathis, E. Gaudio, 2021, Exploration of targeted anti-tumor therapy.

Rapid and Reversible Knockdown of Endogenously Tagged Endosomal Proteins via an Optimized HaloPROTAC Degrader

A. Prescott, D. Alessi, Thomas Macartney, 2019, ACS chemical biology.

Crystal structure of macrocyclic PROTAC 1 in complex with the second bromodomain of human Brd4 and pVHL:ElonginC:ElonginB

A. Ciulli, A. Testa, S. Hughes, 2019 .

An intramolecular bivalent degrader glues an intrinsic BRD4-DCAF16 interaction

M. Nakasone, G. Winter, M. Wegner, 2023, bioRxiv.

New molecular and therapeutic insights into canine diffuse large B-cell lymphoma elucidates the role of the dog as a model for human disease

L. Cascione, E. Gaudio, M. Wymann, 2018, Haematologica.

Inducible Degradation of Target Proteins through a Tractable Affinity-Directed Protein Missile System

G. Sapkota, I. Ganley, Thomas Macartney, 2020, Cell chemical biology.

Functional E3 ligase hotspots and resistance mechanisms to small-molecule degraders

Hana Imrichová, G. Winter, A. Ciulli, 2022, bioRxiv.

as a comparative model for human

L. Cascione, E. Gaudio, L. Marconato, 2019 .

Tricyclic Fused Pyrazoles with a ‘Click’ 1,2,3-Triazole Substituent in Position 3 Are Nanomolar CB1 Receptor Ligands

M. Cascio, M. Zanda, P. Lazzari, 2015, Synthesis.

Homo-PROTACs: bivalent small-molecule dimerizers of the VHL E3 ubiquitin ligase to induce self-degradation

D. Alessi, S. Rocha, D. Lamont, 2017, Nature Communications.

Preclinical Evaluation of [18F]LCATD as a PET Tracer to Study Drug-Drug Interactions Caused by Inhibition of Hepatic Transporters

D. Dawson, M. Zanda, C. Elmore, 2018, Contrast media & molecular imaging.

Mind the Metal: A Fragment Library-Derived Zinc Impurity Binds the E2 Ubiquitin-Conjugating Enzyme Ube2T and Induces Structural Rearrangements

H. Walden, F. Morreale, A. Ciulli, 2017, Journal of medicinal chemistry.

1 Title : Structural basis of PROTAC cooperative recognition for selective protein 1 degradation 2

D. Lamont, A. Ciulli, X. Lucas, 2017 .

Synthesis and Superpotent Anticancer Activity of Tubulysins Carrying Non-hydrolysable N-Substituents on Tubuvaline.

N. Zaffaroni, M. Zanda, P. Lazzari, 2017, Chemistry.

Design, synthesis, in vitro characterization and preliminary imaging studies on fluorinated bile acid derivatives as PET tracers to study hepatic transporters.

M. Zanda, C. Elmore, A. Testa, 2017, Bioorganic & medicinal chemistry.