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PROTAC
(PROteolysis TArgeting Chimeras)

PROTACs provide significant therapeutic potential with possible prolonged pharmacodynamics, improved potency, and ability to target proteins previously thought of as “undruggable”. PROTACs are heterobifunctional small molecules consisting of a target binding handle bridged via a chemical linker to an E3 ligase handle which hijacks the endogenous ubiquitin machinery to target proteins, resulting in subsequent ubiquitination and degradation of your target of interest.

At o2h discovery, we have strong expertise in the synthesis of PROTACs and related chemistry, providing comprehensive solutions for PROTAC building blocks, linkers, compound libraries, and related intermediates to support Targeted Protein Degradation and integrated drug discovery programs.

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protein degradation – biology

o2h biologists can support you in addressing the following questions:

Q. Is my target degraded?

Q. Is my target ubiquitinated?

Q. Do they form a ternary complex?

Q. Are they soluble and cell permeable?

Q. What is the binary affinity for POI and E3 ligase?

Q. What is the phenotypic consequence of target degradation?

Our biology evaluation suite is designed to provide comprehensive insights into ternary complex formation and the exciting realm of targeted protein degradation. Through quantitative measurements using classical Western Blotting or cutting-edge fluorescence and luminescence-based methods, we offer a range of tools for your research.

Our biophysical and biochemical methods are adept at monitoring binary or ternary complex formation, specifically for PROTAC, Protein of Interest (POI), and E3 ligase interactions. In addition, we conduct functional and biochemical activity-based assays, enabling the measurement of target function loss, employing techniques such as nanoBRET, high-content cell imaging (HCI), and kinase activity assessments.

For a complete understanding of your compounds, our ADME profiling covers essential parameters like cellular permeability and solubility, ensuring they meet the necessary criteria.

We’re also at the forefront of in-cell formation of ternary complexes using cutting-edge nanoBRET technology, involving your Protein of Interest, halo-tagged E3 ligases (VHL/CRBN), and degrader molecules.

Furthermore, our expertise extends to target ubiquitination assays, which are essential in understanding the mechanisms at play in targeted protein degradation.

Case Study

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(PROTAC-induced BRD4-VHL ternary complex formation and BRD4 protein degradation. HEK292 cells transfected with NanoLuc-BRD4 donor plasmid and Halo-Tag-VHL acceptor plasmid at 1:100 ratios. Subsequently cells treated with 1uM MZ1 or AT1 PROTAC and compared with untreated DMSO control.

(A, B) Indicates ternary complex formation at 6h (C, D) BRD4-BD2 protein levels at 6h (E, F) real-time ternary complex formation with BRD4-B2/VHL following PROTAC treatment (G, H) real-time kinetics of BRD4-BD2 protein degradation following PROTAC treatment. MG132, a potent, reversible and cell permeable proteasomal inhibitor rescues BRD4 degradation in all condition.)

If you want to Jump-start your PROTAC based drug discovery program (targeted protein degradation)or would like to get a quote, write to us at discovery@o2h.com

our team

prashant shah

Prashant Shah

CEO - o2h discovery and Co-Founder - o2h group

Prashant's Biography

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Prashant Shah

CEO - o2h discovery and Co-Founder - o2h group

Prashant is a serial entrepreneur in life sciences and tech in which one of those companies was acquired by a public company. He is currently active in seed investing (a portfolio of ~50 companies), product/IP development, services, and building lab/office infrastructure. The early career was with the Strategy group at Accenture. He has a BEng, an MSc, in which he worked on the Human Genome Program at the Sanger Centre, and an MPhil in Management from the Judge Institute. Prashant is also a General Partner in the o2h SEIS/EIS Human Health Funds.


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Sunil

Sunil Shah

CEO - o2h Ventures and Co-Founder - o2h group

Sunil's Biography

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Sunil Shah

CEO - o2h Ventures and Co-Founder - o2h group

A serial entrepreneur having begun a career in the Life Sciences team at PA Consulting group followed by co-founding two companies in the information technology and life sciences sector. The second of these companies, Oxygen Healthcare Ltd was acquired by Piramal Enterprises Ltd (BSE: PEL). Sunil co-founded o2h ventures which involves discovery services / collaborations, seeding drug discovery, academic in-licensing and biotechnology incubation. Sunil has a degree in Biochemistry and an MBA from Cambridge University


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Andy Morley

Andy Morley

Chief Scientific Officer

Andy's Biography

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Andy Morley

Chief Scientific Officer

Andy is a highly experienced and accomplished Medicinal Chemist with over 25 years of experience in major pharmaceutical companies such as Sanofi-Aventis and AstraZeneca. He has extensive experience across all phases of drug discovery and has played a key role in the development of five candidates that have reached clinical trials. Andy is a prolific author and inventor, with over 55 publications and patents to his name. Since 2013, he has been working full-time with o2h Limited, where he leads the scientific evaluation of investment opportunities and provides scientific support. He has also served as CSO for two early-stage collaborations within the o2h Ventures portfolio, demonstrating his ability to successfully guide drug discovery projects from concept to clinical development.


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David Davies - o2h

David Davies

Head of Medicinal Chemistry

David's Biography

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David Davies

Head of Medicinal Chemistry

David Davies has 25 years of experience in medicinal chemistry within the pharmaceutical industry with a focus on the antibacterial area (clavulanates, penicillinates, pseudomonates and bacterial topoisomerase inhibitors). He previously worked at GSK and currently holds a part-time academic position at University College London (UCL). He served as the Head of Medicinal Chemistry at Antabio for nearly a decade, specialising in antibacterial research, and has extensive experience managing chemistry projects in multiple countries including France, UK, India and China. He is the inventor of 40 patents and has authored 37 publications.


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