2nd Targeted Protein Degradation Summit in Boston
Alessio and Will both spoke at the 2nd Targeted Protein Degradation Summit in Boston. Read more about the 2nd Targeted Protein Degradation Summit. The meeting was held in Boston during 22-24 October 2019
Structure of the E3 ligase SOCS2 with bound substrate
Ciulli Lab reveals how the E3 ligase SOCS2 latches on to its protein substrates. Read full article on Nature Communications website. Read University of Dundee press release: “Ciulli Lab reveals how the E3 ligase SOCS2 latches on to its protein…
Congratulations to Guilherme
Congratulations to Guilherme for successfully defending his PhD thesis viva today!
Will delivers a Targeted Protein Degradation Webinar with C&EN
You can view Will’s presentation during the webinar on YouTube or TOCRIS website.
New paper: Design and Characterization of SGK3-PROTAC1 an Isoform Specific SGK3 Kinase PROTAC Degrader
Congratulations to Hannah in Dario Alessi’s group for the great job on this study. Well done Andrea for the compound design and synthetic contributions to the project! Read the open access article Title: Design and Characterization of SGK3-PROTAC1, an Isoform Specific SGK3 Kinase PROTAC…
Our review on bispecific small molecules that bring proteins together is published in Current Opinion in Chemical Biology
Well done Chiara! Read the full article. Authors: Chiara Maniaci and Alessio Ciulli* Title: Bifunctional chemical probes inducing protein-protein interactions. Abstract Inducing biomolecular interactions with synthetic molecules to impact biological function is a concept of enormous appeal. Recent years have seen…
University of Dundee and Eisai enter partnership
University of Dundee and Eisai enter partnership for cancer drug discovery using targeted protein degradation. Read the full press release from Eisai Related links Eisai PR: EISAI ENTERS INTO COLLABORATION RESEARCH AGREEMENT WITH UNIVERSITY OF DUNDEE ON TARGETED PROTEIN DEGRADATION…
XXVI National Meeting in Medicinal Chemistry (NMMC 2019)
Alessio delivers one of the plenary lectures at the XXVI National Meeting in Medicinal Chemistry (NMMC 2019) in Milan, Italy. Read more about conference in the ChemMedChem’s Editorial: “Overview of the XXVI National Meeting in Medicinal Chemistry” by Prof. Marina Carini and Prof.…
University and Boehringer Ingelheim collaborate for free access of PROTAC compounds
Order MZ1 for free today! Related Links University and Boehringer Ingelheim collaborate for free access of PROTAC compound University of Dundee and Boehringer Ingelheim collaborate for free access of PROTAC compound on opnMe.com Drug Discovery Today® features Dundee / Boehringer…
Dodgeball Tournament
The Group’s mighty team “Focaccia” won the 2019 PiCLS Dodgeball Tournament. Well done team! Congrats to Adam, Alessandra, Conner, Daniela, and Ryan. Good work guys – Graduate students rule!
Dundee and Boehringer Ingelheim collaborate on video
Dundee and Boehringer Ingelheim collaborate on video PR for the launch of PROTAC degraders on BI’s open innovation platform OpnMe Check our OpnMe videos here: 1) MZ1 PROTAC’s Journey to research labs (video) 2) ACBI1 PROTAC’s Journey to research labs (video)…
Dundee and Boehringer Ingelheim scientists degrade undruggable cancer targets SMARCA2/4
Read the article Open Access as SharedIt version Fantastic job Will, Manfred and team! Researchers can now access the SMARCA2/4 degrader ACBI1 for their own research – order the molecule completely free of charge from OpnMe. Related Links UoD PR: Boehringer…
Our new paper describing an SPR kinetic assay to monitor PROTAC ternary complexes is now out in ACS Chemical Biology
Measuring kinetics by surface plasmon resonance (SPR), we reveal how striking differences in stability and lifetime of target:PROTAC:ligase ternary complexes influence initial rates of PROTAC induced protein degradation. Congratulations to Michael, Scott, Claire, Will and our colleagues at Boehringer Ingelheim. Read…
Our collaboration with Dario Alessi’s Lab on deploying improved HaloPROTACs against CRISPR’ed halo-tagged endosomal proteins is now out in ACS Chem Biol
Read the open access article Congratulations to Hannah Tovell in Dario Alessi’s group for the excellent job on this study. Well done Andrea and Chiara for the chemistry contributions to the project!
Dundee scientist front and centre of the PROTAC revolution
In an article in the journal Nature, Megan Scudellari reflects on the short history of PROTACs – a new type of drug design that is galvanising the Pharmaceutical industry, with the first PROTAC drug from Arvinas about to enter phase-1 clinical…
CRBN versus VHL
Our new PROTAC paper on hijacking E3 ligases against each others is now published in Bioorg. Med. Chem. Read the full paper Open Access. Well done Miriam, Chiara, Scott and Andrea on this work!
VHL ligands as spy molecules for 19F NMR screening
Our latest paper describing novel fluorinated VHL ligands as spy molecules for 19F NMR screening is out in Chemical Communications. Well done to Guilherme and congrats on his first first-author article!
A Roadmap for PROTAC Development
Our SAR story disclosing dual Brd7/9 PROTAC degrader VZ185 is published in J. Med. Chem. Congratulations to Vittoria, Scott, Chiara and Andrea, and all our collaborators for their contributions to this work! Related Links Promega Connections blog: “A Roadmap for PROTAC Development”
Christmas party 2018
The Lab Christmas Dinner was held at Lands of Loyal, Alyth. It was a productive and fun Year, Merry Christmas everyone! Merry Christmas to everyone! It has been a very productive, intense and fun year. Thank You all and congratulations…
Alessio delivers a Chemistry World webinar
Alessio delivers a Chemistry World webinar titled “Targeted protein degradation using small molecules” You can view Alessio’s PROTAC webinar on Chemistry World website.
Two ligandable pockets on the surface of the VHL E3 ligase
Two ligandable pockets on the surface of the VHL E3 ligase are revealed in our new paper just out in J Med Chem Well done to Xavi and Inge! Read our paper Open Access.
Introducing 3-Fluoro-4-hydroxyprolines
Introducing 3-Fluoro-4-hydroxyprolines: Synthesis, conformational analysis and stereoselective recognition by VHL E3 ligase for protein degradation. Very proud of Lab’s work just out in @JACS by Andrea, Xavi and coworkers! well done everyone at @UoDLifeSciences and beyond, and thanks to @ERC_Research @MSCActions for funding Read our article…
Molecular recognition of helical histone tail by PHD finger domains
Our paper on the molecular recognition of helical histone tail by PHD finger domains is now published in Biochemical Journal. Well done to Alessio B., Anastasia, Xavi – and Manuel! Read the full paper open access.
First ternary crystal structure of a PROTAC bound to to its E3 ligase VHL and Brd4 target
Our paper reporting the first ternary crystal structure of a PROTAC bound to to its E3 ligase VHL and Brd4 target is now published in Nature Chemical Biology! Our work provides unprecedented insights into how PROTACs work. Congratulations to Morgan, Andrea, Xavi and Kwok-Ho for a…
Recognition and small-molecule mimicry of degrons by E3 ligases
Our review on recognition and small-molecule mimicry of degrons by E3 ligases is now published in Current Opinion in Structural Biology. Well done Xavi! Read our review. Highlights: Abstract The ubiquitin–proteasome system is a master regulator of protein homeostasis, by…
Thioamide substitution to probe the hydroxyproline recognition of VHL ligands
The article is a contribution to the journal’s Special Issue for the 2018 Tetrahedron Young Investigators Award for Matthew Fuchter. Read our article Open Access Congratulations Pedro and Xavi, well done! The article is a contribution to the journal’s Special…
Ligandability of PHD finger domains of BAZ2A and BAZ2B
Read our Open Access article Congratulations to Anastasia, Xavi and colleagues! Read our Open Access article Congratulations to Anastasia, Xavi and colleagues!
Molecular recognition of ternary complexes for targeted protein degradation
Read our review Read our review
First crystal structure of the VHL-EloBC-Cul2-Rbx1 multi-subunit complex
Read our article open access
Our paper studying the effect of linking on the mechanism of action of BET degraders
Read our paper open access here. The article will be published as part of the a Special Issue on “Inducing Protein Degradation as a Therapeutic Strategy“.
New paper: Structure-guided design of peptides
Read our full paper open access
Relationships leading to the potent VHL inhibitor VH298
The article will be part of the journal Special Issue on “Inducing Protein Degradation as a New Therapeutic Strategy”, edited by Prof. Craig Crews and Prof. Shameng Wang. Read our article Open Access
VHL inhibitor VH298 as novel chemical probe of the hypoxia signalling pathway
Our paper characterising VHL inhibitor VH298 as novel chemical probe of the hypoxia signalling pathway is now published in Nature Communications. Read our open access article. Featured in the UoD News websites Access VH298 from the Chemical Probes portal. Related Links
Promotions for academic staff
Congratulations to Alessio for being promoted to Professor (Chair) from 1st October 2016. Alessio Ciulli, Vicki Cowling, Sonia Rocha, Helen Walden and Sarah Coulthurst were all successful in being promoted during this year’s round of Academic Staff Review for the…
Target validation: Switching domains
Alessio’s News & Views article titled “Target validation: Switching domains” is now published in Nat Chem Biol. Read the news and views article. Read the “Sensitivity and engineered resistance of myeloid leukemia cells to BRD9 inihibition” by Hohmann et al.
Fellow of the Royal Society of Chemistry (FRSC)
Alessio has been admitted as a Fellow of the Royal Society of Chemistry (FRSC). Dr Alessio Ciulli, from the Division of Biological Chemistry and Drug Discovery, in the School of Life Sciences at the University of Dundee is now a…
Boehringer Ingelheim and University of Dundee collaborate to develop new class of medicines
Collaboration aims to develop PROteolysis TArgeting Chimeric molecules (PROTACs) – a new therapeutic modality that is able to degrade proteins playing a central role in disease processes PROTACs and their new mechanism of action are expected to open new horizons…
Advanced chemical genetics for epigenetics
Our review on advanced chemical genetics for epigenetics is now published in Current Opinion in Chemical Biology! Well done Andrew, Kwok-Ho and Michael! Read our review open access. Review synopsis In conventional chemical genetics, cell-active small-molecules directly block protein activity,…
Alessio Ciulli winner MedChemComm award
Alessio Ciulli is designated as the winner of the 2016 MedChemComm Emerging Investigator Lectureship. Learn more about the MedChemComm award. Alessio delivered his Prize lecture at the European Federation of Medicinal Chemistry International Symposium on Medicinal Chemistry (EFMC-ISMC) held in…
Selectivity of chemical probes targeting bromodomains
Our review on selectivity of chemical probes targeting bromodomains is now published in Future Medicinal Chemistry. Read our open access review without restriction .
An HFSP fellowship that sowed the seeds for PROTAC drug development
HFSP Matters: An HFSP fellowship that sowed the seeds for PROTAC drug development. by Alessio Ciulli In 2009, Alessio Ciulli was awarded an HFSP Short-Term Fellowship1 to support his 3-month research visit to Yale University to start a collaboration between his…
Royal Society of Chemistry award for Alessio Ciulli
Alessio Ciulli is awarded the 7th Capps Green Zomaya Award from the Royal Society of Chemistry. Dr Alessio Ciulli of the University of Dundee has been named the winner of a major award from the Royal Society of Chemistry. Dr Ciulli,…
Xavi wins Best Poster Prize
Xavi wins Best Poster Prize at the 2016 EFMC-ISMC conference in Manchester. Well done!
Alessio Ciulli awarded 2015 EFMC Prize
Alessio Ciulli is designated as the winner of the 2015 EFMC Prize for a Young Medicinal Chemist in Academia. Alessio Ciulli of the Division of Biological Chemistry and Drug Discovery has been awarded the European Federation for Medicinal Chemistry (EFMC)…
Cyclic and macrocyclic peptides as chemical tools to probe PPIs
Our review on cyclic and macrocyclic peptides as chemical tools to probe PPIs is now out in ChemMedChem. Read our Open Access article.
Triazolo-benzodiazepine chemistry to I-BET/JQ1 analogues for the bump-and-hole approach and BD2-selectivity
Our new paper on triazolo-benzodiazepine chemistry to I-BET/JQ1 analogues for the bump-and-hole approach and BD2-selectivity is now published in J. Med. Chem. You can read our open access Article ASAP. Obtain our compound “TC AC 28” (6-(1H-Indol-4-yl)-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine-4-acetic acid methyl ester)…
Our Lab 2015 Away Day
Our Lab 2015 Away Day was at Braemar / Balmoral / Cairn-na-Cuimhne.
Alessio Ciulli receives 2015 ICBS Young Chemical Biologist Award
Alessio Ciulli is designated as the winner of the 2015 ICBS Young Chemical Biologist Award. Read more about the International Chemical Biology Society. Alessio was presented the award and invited to give a presentation during the special “Rising Stars in…
BRD4 intra-BET selective chemical degraders hijacking the VHL E3 ubiquitin ligase
Ciulli Lab develops super-targeted method of destroying tumour proteins. Scientists at the University of Dundee have developed a super-targeted method of destroying malevolent proteins in tumour cells, removing the threat of collateral damage to surrounding proteins. The research team led…
Crystallography of SOCS2-EloB-EloC complex by Arsenic SAD
Our new paper on crystallography of SOCS2-EloB-EloC complex by Arsenic SAD is now published in PLoS One. Read our paper.
FortBio and Drug Discovery talks
Alessio Bortoluzzi is invited to speak at the ForteBio Protein Analysis & Characterization Spring Workshop in London on April 22nd; and Alessio Ciulli is invited to speak at the Drug Discovery Chemistry meeting (Epigenetics) in San Diego on April 21,…
Structure, protein-protein interactions and drug discovery targeting Cullin RING E3 Ubiquitin Ligases
Our review on structure, protein-protein interactions and drug discovery targeting Cullin RING E3 Ubiquitin Ligases is now published in the Biochemical Journal. You can read our paper Open Access.
Structural basis of histone tail recognition by human BAZ2A (TIP5) and BAZ2B epigenetic reader domains PHD finger and bromodomain
Our paper on structural basis of histone tail recognition by human BAZ2A (TIP5) and BAZ2B epigenetic reader domains PHD finger and bromodomain now published in Structure. Read our Open Access full-text article
Alessio wins the 2014 Talented Young Italians Award
Alessio Ciulli has won a 2014 Talented Young Italians Prize, awarded by the Italian Chamber of Commerce and Industry for the UK. Eight awards were conferred in four categories, with Alessio receiving the award for the “Research and Innovation” category,…
Christmas 2014
The Group Christmas dinner is held at the Lands of Loyal, Alyth
Biophysical investigation of interactions and assembly of full-size SOCS2:EloBC:Cul5:Rbx2 E3 ubiquitin ligase
Our paper on biophysical investigation of interactions and assembly of full-size SOCS2:EloBC:Cul5:Rbx2 E3 ubiquitin ligase is now published in J. Biol. Chem. Read our Just In Press article.
Chemical genetics bump-and-hole approach to engineer controlled selectivity of BET bromodomain inhibitors
Just published in Science! Our paper describing a chemical genetics bump-and-hole approach to engineer controlled selectivity of BET bromodomain inhibitors. Read our paper open-access in Europe PMC Highlighted in the BBSRC website Highlighted in Cancer Discovery Research Watch. Highlighted in Nature Chemical Biology Highlighted…
Best Poster Prize for Carles Galdeano and international talk for Alessio Bortoluzzi
Carles Galdeano wins the Best Poster Prize at the 2014 EFMC-ISMC conference in Lisbon. Alessio Bortoluzzi speaks at the EMBO Workshop “Advances in protein–protein interaction analysis and modulation” in Hyeres, France.
Elucidating binding hotspots of the BAZ2B bromodomain:histone interaction
Our paper elucidating binding hotspots of the BAZ2B bromodomain:histone interaction now published in Biochemistry. Read our paper on ACS publication website.
Structure-guided optimization of nanomolar inhibitors of the VHL-HIFalpha protein-protein interaction
Our paper on structure-guided optimization of nanomolar inhibitors of the VHL-HIFalpha protein-protein interaction is now published in J. Med. Chem. Read our paper on ACS Publications website.
NMR approaches in structure-based lead discovery for targeting multi-protein complexes
Our review on NMR approaches in structure-based lead discovery for targeting multi-protein complexes is now published in Prog. Biophys. Mol. Biol. You can read our paper open-access .
Lab 2014 Away Day
Our Lab 2014 Away Day was at Glen Doll / Corrie Fee National Natural Reserve.
ESMEC 2014
Alessio is invited to speak at the European School of Medicinal Chemistry (ESMEC 2014) in Urbino, Italy
Awarded prize at the 47th International School of Crystallography
Our Lab’s poster on chemical & structural biology of bromodomains was awarded the “Special Mention” Prize at the 47th International School of Crystallography “Structural Basis of Pharmacology” in Erice, Italy
Lab Christmas Dinner 2013
Our Lab Christmas Dinner was held at The Grange Inn at St. Andrews.
Biophysical Screening for the Discovery of Small-Molecule Ligands
Alessio’s book chapter “Biophysical Screening for the Discovery of Small-Molecule Ligands” is now published in Methods Mol. Biol Read the full chapter.
Targeting the low-druggability BAZ2B bromodomain using fragment-based drug design
Our paper targeting the low-druggability BAZ2B bromodomain using fragment-based drug design is now published in J. Med. Chem. You can read our paper open-access.
Alessio is invited to speak at the 15th RSC Bioorganic Group Firbush Conference
Alessio is invited to speak at the 15th RSC Bioorganic Group Firbush Conference “The chemistry and biology of protein modification” in Killin. Read more about the meeting on the RSC website.
DrugDesign 2013 meeting
Carles speaks at the DrugDesign 2013 meeting “Fragment- and Ligand-based Drug Design” in Oxford. Read more about the meeting on the LPM Healthcare website.
Team move to School of Life Sciences
The Ciulli Laboratory moves to the College of Life Sciences at the University of Dundee
Alessio delivers the course at the University of Messina
Alessio delivers the course “Drug Discovery” to the Dept. of Pharmaceutical Chemistry at the University of Messina, under the realm of the new MIUR-funded programme Messaggeri della Conoscenza. Learn more about this news on the Messaggeri della Conoscenza.
Affinity and structural assembly of the ASB9 CRL
Our paper on the affinity and structural assembly of the ASB9 CRL is now published in Biochemistry. You can read our Open-Access paper.
Bio-NMR project
Our Bio-NMR project in collaboration with the SON NMR Large Scale Facility starts in Utrecht. Read more about the Bio-NMR project.
BCDD Divisional BBQ
The Group attends in full the BCDD Divisional BBQ.
Our paper interrogating the NMR binding detection limits of fragments targeting the VHL-HIF1α PPI
Read our paper published in ACS Med. Chem. Lett. about interrogating the NMR binding detection limits of fragments targeting the VHL-HIF1α PPI. You can read our open-access paper.
Alessio is invited to speak at the ESBOC 2013
The European Symposium on Biological and Organic Chemistry (ESBOC) 2013 meeting “Chemical Probes for Cellular Processes” held in Gregynog, Wales. Details of the annual meetings can be found on the ESBOC website. Read the blog about the day and history…