Proximity-inducing pharmacology: Targeted protein degradation and beyond

22 Mayo 23

- 24 Mayo 23

Proximity-inducing pharmacology has become an important avenue of therapeutic intervention and offers significant inroads to drug the “undruggable”. Mechanistically, the involved compounds often hijack one protein’s function by inducing its interaction with another protein or transcript. Recent advances in targeted protein degradation illustrate that compound-induced proximity between an E3 ubiquitin ligase and a disease-relevant protein can lead to ubiquitination and protein degradation. In the past years, this growing field has moved from proof of concept to the development of degrader medicines in clinical trials. These advances have fueled interest in other proximity-inducing concepts that can trigger a plethora of outcomes in proteins and transcripts, ranging from mammals to bacteria. As our understanding of the molecular features that govern drug-induced interactions grows and the use of this pharmacology in disease matures, more breakthroughs are sure to follow. This conference will provide an interdisciplinary forum for researchers interested in the chemical modulation of biomolecule’s fates. Leaders in many areas of drug discovery will discuss the opportunities and challenges in this exciting new area.

Proximity-inducing pharmacology: Targeted protein degradation and beyond

Presentation

Conference organizers

Dr. Cristina Mayor-Ruiz
IRB Barcelona
Barcelona, Spain

Dr. Georg E. Winter
CeMM
Vienna, Austria

There is no registration fee for this conference, but the number of participants is limited, with a number of seats saved for IRB Barcelona alumni. Previous registration is required.

Due to the high demand for participation in this conference, the registration deadline has been brought forward on Wednesday (15 February).

Priority will be given to those who submit the highest quality abstracts for short talks or posters and the order of registration will be considered. We will contact all those registered very soon.

Abstracts should include a title, authors, affiliations, summary (max 250 words) and references

Fechas importantes

REGISTRATION DEADLINE: 15 FEBRUARY, 2023

(Note: Any issue about the registration or abstract, please contact: meritxell.gavalda@irbbarcelona.org)

Proximity inducing pharmacology: Targeted protein degradation and beyond program (127.7 KB)

Proximity inducing pharmacology: Targeted protein degradation and beyond poster (1.21 MB)

Programa

Monday, 22 May

8.30 Registration

9.00 Welcome by Directorate of IRB Barcelona and organizers

(Dr. Cristina Mayor-Ruiz and Dr. Georg E. Winter)

Session 1: Proteolysis Targeting Chimeras (PROTACs)

Chair: Dr. Marie-Helene (Barcelona, Spain)

9.15 Dr. Fleur M. Ferguson, University of California San Diego (San Diego, CA, USA)

9.45 Dr. William Farnaby, University of Dundee (Dundee, UK)

10.15 Advancing targeted protein degraders and bringing them into the clinic

Dr. Danette L. Daniels, Foghorn Therapeutics (CA, MA, USA)

10.45-11.30 Coffee break and poster session

11.30 Short talk 1: Directing the E3 ligase pair SIAH1/2 towards degradation of neosubstrates using covalent PROTACs

Lena Münzker, Boehringer Ingelheim RCV GmbH & Co KG (Vienna, Austria)

11.45 Dr. Alessio Ciulli, University of Dundee (Dundee, UK)

12.15 Dr. Craig M. Crews, Yale University (New Heaven, CT, USA)

12.45 Short talk 2: An intramolecular bivalent degrader glues an intrinsic BRD4-DCAF16 interaction

Angus Cowan, University of Dundee (Dundee, UK)

13.00-14.30 Lunch and poster session

Session 2: Molecular glues

Chair: Dr. Jay Bradner (CA, MA, USA)

14.30 Dr. Cristina Mayor-Ruiz, IRB Barcelona (Barcelona, Spain)

15.00 Dr. Eric Fischer, Dana-Farber Cancer Institute (Boston, MA, USA)

15.30 Identification and characterization of small-molecule degraders

Dr. Georg E. Winter, CeMM (Vienna, Austria)

16.00-16.45 Coffee break and poster session

16.45 Short talk 3: Understanding cooperativity effects in the drug-dependent degradation of the Cereblon neosubtrate CK1 alpha

Jordi Juárez-Jiménez, UB (Barcelona, Spain)

17.00 Dr. Nicolas Thomä, FMI (Basel, Switzerland)

17.30 Mechanism of action of velcrin small molecules
Dr. Heidi Greulich, Broad Institute (Cambridge, MA, USA)

18.00 Short talk 4: BTBBCL6 dimers as building blocks for reversible drug-induced protein oligomerization

Mikołaj Słabicki, BROAD Insitiute (Cambridge, USA)

18.15 End of session

Tuesday, 23 May

Session 3: Targeted degradation beyond the proteasome

Chair: Dr. Ingo Hartung (Darmstadt, Germany)

9.00 Dr. Green Ahn, Stanford University (Stanford, CA, USA)

9.30 BacPROTACs mediate targeted protein degradation in bacteria

Dr. Francesca E. Morreale, IMP, The Francis Crick Institute (London, UK)

10.00 Short talk 5: Development of next generation AUtophagy TArgeting Chimeras (AUTACs) to enable proximity induced degradation of mitochondria

Niyaz Zaman, University College London (London, UK)

10.15 Short talk 6: Multicomponent Reaction-Based Approach to Novel Aryl Hydrocabon Receptor Activators, PROTACs and HomoPROTACs

Ouldouz Ghashghaei, IBUB- UB (Barcelona, Spain)

10.30-11.30 Coffee break and poster session

11.30 Short talk 7: Induced self-elimination of the Clp protease system as antibiotics strategy

David M. Hoi, Institute of Molecular Pathology (Vienna, Austria)

11.45 Targeting unexplored E3 ligases with small molecules

Dr. Carles Galdeano, UB Barcelona (Barcelona, Spain)

12.15 Dr. Mathew Disney, UF Scripps Biomedical Research (La Jolla, CA, USA)

12.45-14.30 Lunch and poster session

Session 4: Inducing and removing post-translational modifications: ubiquitin and
beyond

Chair: TBD

14.30 Dr. Sayumi Yamazoe, Bristol-Myers Squibb (CA, USA)

15.00 Reimagining Druggability using Chemoproteomic Platforms

Dr. Daniel K. Nomura, University of California, Berkeley (Berkeley, CA, USA)

15.30 Short talk 8: Development of a novel type of proteolytic chimera based on direct 26S proteasome targeting

Bernat Crosas, IQAC-CSIC (Barcelona, Spain)

15.45 Short talk 9: E3-ID: an innovative system to identify targets of E3 ligases

James D. Sutherland, CIC bioGUNE (Bizkaia, Spain)

16.00-16.45 Coffee break and poster session

16.45 Dr. Amit Choudhary, Broad Institute (CA, MA, USA)

17:15 Dr. Christopher G. Parker, The Scripps Research Institute (La Jolla, CA, USA)

17.45 Short talk 10: HiBiT-SpyTag: A minimal tag for covalent protein capture and degrader development

Radosław P. Nowak, Dana-Farber Cancer Institute (Boston MA, USA)

18.00 End of session

20.30 Speakers dinner (Restaurant Can Pineda) (Sant Joan de Malta, 55)

Wednesday, 24 May

Session 5: Proximity-inducing pharmacology: new approaches and computational
methods

Chair: TBD

9.00 Short talk 11: Target- and E3-driven discovery of molecular glue degraders via accelerated molecular simulations

Carles Perez-Lopez, IRB Barcelona (Barcelona, Spain)

9.15 Short talk 12: Finding all our switches: fast global mapping of the allosteric landscape for KRAS inhibition

Ben Lehner, Wellcome Sanger Institute & CRG (Barcelona, Spain)

9.30 Dr. Patrick Aloy, IRB Barcelona (Barcelona, Spain)

10.00 Dr. Víctor Guallar, BSC (Barcelona, Spain)

10.30-11.15 Coffee break and poster session

11.15 Short talk 13: Supercharging kinase turnover – rationalizing non-obvious destabilization mechanisms

Natalie S. Scholes, CeMM (Vienna, Austria)

11.30 Short talk 14: Transcriptional chemical inducers of proximity to rewire cancer drivers

Sai Gourisankar, Stanford University (Stanford, CA, USA)

12.30 Concluding remarks and end of conference

11.45 Dr. Miquel Duran-Frigola, Ersilia Open Source Initiative (Cambridge, UK)

11.30 Short talk 15: DEGRONOPEDIA - a web server for proteome-wide inspection of degrons

Natalia A. Szulc, IIMCB (Warsaw, Poland)

12.30 Concluding remarks and end of conference

Localización

The BARCELONA BIOMED CONFERENCE Proximity-inducing pharmacology: Targeted protein degradation and beyond will be placed at the Casa Convalescència in the heart of Barcelona. Talks will take place in the Aula Magna.

Casa Convalescència
C/ Sant Antoni Maria Claret, 171
08041 Barcelona

Tel +34 934 335 000
www.uab-casaconvalescencia.org

How to reach the Casa Convalescència:

Underground
Yellow line (L4) - GUINARDÓ – HOSPITAL DE SANT PAU station
Blue line (L5) - SANT PAU – DOS DE MAIG station

By bus
Lines: 15, 19, 20, 45, 47, 50, 51, 92 and 192.

For the GPS
Introduce the following coordinates:
Latitude: 41.413702 (41° 24' 49.33'' N)
Longitude: 2.177482 (2° 10' 38.94'' E)

From the airport

* Train + Underground. At the RENFE station, take the train to Sants-Estació. Once there take the Underground's blue line (L5) till SANT PAU – DOS DE MAIG station.
* Bus + Underground. Outside the airport terminal, take the AEROBUS to Plaça Catalunya. Walk one corner till Plaça Urquinaona and take the Underground's yellow line (L4) to GUINARDÓ – HOSPITAL DE SANT PAU station.

Barcelona Metropolitan Transport webiste (with metro and bus maps)

Accomodation

Speakers will be lodged at the Hotel Catalonia Sagrada Familia
Aragó 577- 579
08026, Barcelona
Telephone: +34 93 245 89 05

www.cataloniahotels.com/en/hotel/catalonia-sagrada-familia

Other hotels
A list of additional hotels within walking distance of the Casa Convalescència can be found at: https://www.barcelona-tourist-guide.com/en/hotels/hotelmaps/eixample-right-barcelona-hotel.html
(The Casa Convalescència is located near the violet point 27/3 star). Rates will vary depending on choice of hotel and season. Please check with the hotel of your choice directly for the best offer.

Residences
Another possibility is the Lesseps Residence Hall, and is available for short-term stays.

Lesseps Residence Hall
Plaza Lesseps, 12 08023 Barcelona
View on map
Telephone: +34 933 941 600
e-mail: lesseps@resa.es
www.resa.es/en/city/barcelona

Participants registered for events in the Barcelona BioMed series should contact the hotels and residences directly to arrange bookings and payment.