July Publication
NR Kong and LH Jones. Clinical translation of targeted protein degraders. Clin. Phar. Ther. 2023, in press.
pubmed.ncbi.nlm.nih.gov/37399310/
NR Kong and LH Jones. Clinical translation of targeted protein degraders. Clin. Phar. Ther. 2023, in press.
pubmed.ncbi.nlm.nih.gov/37399310/
Presentations
Lyn Jones - Targeted Protein Degrader Safety and Emerging Applications of Functional Genomic and Proteomic Profiling. Drug Safety Gordon Research Conference, Easton, MA, June 2022
Lyn Jones - Targeted Protein Degrader Safety and Emerging Applications of Functional Genomic and Proteomic Profiling. Drug Safety Gordon Research Conference, Easton, MA, June 2022
May Publication
H Huang and LH Jones. Covalent drug discovery using sulfur(VI) fluoride exchange warheads. Exp. Opin. Drug Disc. 2023, 18, 725-735.
https://pubmed.ncbi.nlm.nih.gov/37243622/
H Huang and LH Jones. Covalent drug discovery using sulfur(VI) fluoride exchange warheads. Exp. Opin. Drug Disc. 2023, 18, 725-735.
https://pubmed.ncbi.nlm.nih.gov/37243622/
Presentations
Lyn H. Jones - Zinc Finger Transcription Factor Drug Discovery Using Molecular Glue Degraders.
Northeastern Regional Meeting of the ACS, Boston, May 2023.
Lyn H. Jones - Zinc Finger Transcription Factor Drug Discovery Using Molecular Glue Degraders.
Northeastern Regional Meeting of the ACS, Boston, May 2023.
May New Hire
Emily Agnello – joins the CPD as a Scientist I with our biochemistry team.
Welcome to the team, Emily!
Emily Agnello – joins the CPD as a Scientist I with our biochemistry team.
- Emily recently obtained her PhD in Biochemistry and Molecular Biology in Brian Kelch’s lab at the University of Massachusetts Chan Medical School. Her PhD work focused on elucidating the structure of tail proteins from thermophilic bacteriophage using cryogenic electron microscopy. This structural work allowed Emily to understand the mechanistic assembly of the long tail tube and assignment of previously unkown proteins in the tail-tip complex,
Welcome to the team, Emily!
April Publications
T Tsang, F Huerta, Y Liu, J Che, R Metivier, S Ferrao, K Donovan, LH Jones, BL Zerfas, RP Nowak. HiBiT-SpyTag: A minimal tag for covalent protein capture and degrader development. ACS Chem. Biol. 2023, 18, 933-941.
https://pubs.acs.org/doi/abs/10.1021/acschembio.3c00084
Y Gao, B Jiang, H Kim, MJ Berberich, J Che, KA Donovan, JM Hatcher, F Huerta, NP Kwiatkowski, Y Liu, PP Liuni, RJ Metivier, VK Murali, RP Nowak, T Zhang, ES Fischer, NS Gray, LH Jones. Catalytic degraders effectively address kinase site mutations in EML4-ALK oncogenic fusions. J. Med. Chem. 2023, 66, 5524-5535.
https://pubs.acs.org/doi/abs/10.1021/acs.jmedchem.2c01864
T Tsang, F Huerta, Y Liu, J Che, R Metivier, S Ferrao, K Donovan, LH Jones, BL Zerfas, RP Nowak. HiBiT-SpyTag: A minimal tag for covalent protein capture and degrader development. ACS Chem. Biol. 2023, 18, 933-941.
https://pubs.acs.org/doi/abs/10.1021/acschembio.3c00084
Y Gao, B Jiang, H Kim, MJ Berberich, J Che, KA Donovan, JM Hatcher, F Huerta, NP Kwiatkowski, Y Liu, PP Liuni, RJ Metivier, VK Murali, RP Nowak, T Zhang, ES Fischer, NS Gray, LH Jones. Catalytic degraders effectively address kinase site mutations in EML4-ALK oncogenic fusions. J. Med. Chem. 2023, 66, 5524-5535.
https://pubs.acs.org/doi/abs/10.1021/acs.jmedchem.2c01864
2023 AACR Conference Presentations
Presenter – Lyn H. Jones
“Emerging Opportunities for Non-Degrading Molecular Superglues”. AACR Chemistry to the Clinic Educational Session: Leveraging Induced Proximity – Beyond Targeted Protein Degradation (Chair).
Presenter – Jianwei Che
“Catalytic Degraders Effectively Address Kinase Site Mutations in EML-ALK Oncogenic Fusions”. AACR Minisymposium - New Targeted Protein Degraders: Discovery and Novel Design Strategies.
Presenter – Lyn H. Jones
“Emerging Opportunities for Non-Degrading Molecular Superglues”. AACR Chemistry to the Clinic Educational Session: Leveraging Induced Proximity – Beyond Targeted Protein Degradation (Chair).
Presenter – Jianwei Che
“Catalytic Degraders Effectively Address Kinase Site Mutations in EML-ALK Oncogenic Fusions”. AACR Minisymposium - New Targeted Protein Degraders: Discovery and Novel Design Strategies.
Presentations
Lyn Jones - Targeted Protein Degrader Safety and Emerging Applications of Functional Genomic and Proteomic Profiling. Society of Toxicology, Nashville, TN, March 2023.
Lyn Jones - Targeted Protein Degrader Safety and Emerging Applications of Functional Genomic and Proteomic Profiling. Society of Toxicology, Nashville, TN, March 2023.
February Publications
GP Dann, H Liu, RP Nowak and LH Jones. Cereblon target validation using a covalent inhibitor of neosubstrate recruitment. Methods Enzymol. 2023, 681, 155-167.
https://www.sciencedirect.com/science/article/abs/pii/S0076687922003810?via%3Dihub
BL Zerfas, F Huerta, H Liu, G Du, NS Gray, LH Jones, RP Nowak. Advancing targeted protein degrader discovery by measuring cereblon engagement in cells. Methods Enzymol. 2023, 681, 169-188.
https://www.sciencedirect.com/science/article/abs/pii/S007668792200338X
GP Dann, H Liu, RP Nowak and LH Jones. Cereblon target validation using a covalent inhibitor of neosubstrate recruitment. Methods Enzymol. 2023, 681, 155-167.
https://www.sciencedirect.com/science/article/abs/pii/S0076687922003810?via%3Dihub
BL Zerfas, F Huerta, H Liu, G Du, NS Gray, LH Jones, RP Nowak. Advancing targeted protein degrader discovery by measuring cereblon engagement in cells. Methods Enzymol. 2023, 681, 169-188.
https://www.sciencedirect.com/science/article/abs/pii/S007668792200338X
Presentations
Lyn Jones - Kinase Targeting Using Covalent and Degrader Modalities.
Kinase Drug Discovery Symposium, Karolinska Institute, Stockholm, Sweden, March 2023.
Lyn Jones - Kinase Targeting Using Covalent and Degrader Modalities.
Kinase Drug Discovery Symposium, Karolinska Institute, Stockholm, Sweden, March 2023.
Chinese New Year Celebration | January 23
CPD held its first annual Chinese New Year Celebration!
May the Year of the Rabbit bring us all good fortune, success, and endless opportunities
CPD held its first annual Chinese New Year Celebration!
May the Year of the Rabbit bring us all good fortune, success, and endless opportunities
Lyn Jones, Yingde Zhu, Yingpeng Liu, Yangchun Chen, Ravid Inbar, Devin Ryan, Nikki Kong, Justin Cruite, Jeevan GC, Bart Luttderbach, Henning Arlt, Jianwei Che, Jasmin Kruell, Shatha AbuHammad, Jingyi Wang, Breanna Zerfas, Jirong Luo, Tiffany Tsang
Jirong Luo, Pratik Vikhe, Yinpeng Liu
|
Stephen Xie, Devin Ryan; Jasmin Kruell, Ravid Inbar
Kishan Mahase, Jingyi Wang
|
January Publication
RP Nowak, J Che, S Ferrao, NR Kong, H Liu, BL Zerfas, and LH Jones. Structural rationalization of GSPT1 and IKZF1 degradation by thalidomide molecular glue derivatives. RSC Med. Chem. 2023, 14, 501-506.
https://pubs.rsc.org/en/content/articlelanding/2023/md/d2md00347c/unauth
RP Nowak, J Che, S Ferrao, NR Kong, H Liu, BL Zerfas, and LH Jones. Structural rationalization of GSPT1 and IKZF1 degradation by thalidomide molecular glue derivatives. RSC Med. Chem. 2023, 14, 501-506.
https://pubs.rsc.org/en/content/articlelanding/2023/md/d2md00347c/unauth
January New Hire
Ravid Inbar - joins the CPD as a RA I with our biochemistry team.
Welcome aboard, Ravid!
Ravid Inbar - joins the CPD as a RA I with our biochemistry team.
- Ravid recently graduated in December 2022 from the University of Massachusetts, Amherst with a B.S. in both biochemistry and psychology. During his time at UMass, he studied the effect of various known mutations on the activity of CaMKII.
Welcome aboard, Ravid!
November Publication
M Kostic and LH Jones. Beyond inhibition: Ligand-based pharmacological exploration as a strategy towards new targets and modalities. Book chapter in Protein Homeostasis in Drug Discovery: A Chemical Biology Perspective. 2022 Eds. M Kostic and LH Jones.
https://onlinelibrary.wiley.com/doi/book/10.1002/9781119774198
M Kostic and LH Jones. Beyond inhibition: Ligand-based pharmacological exploration as a strategy towards new targets and modalities. Book chapter in Protein Homeostasis in Drug Discovery: A Chemical Biology Perspective. 2022 Eds. M Kostic and LH Jones.
https://onlinelibrary.wiley.com/doi/book/10.1002/9781119774198
CPD Science Day | November 3
Annual offsite at Brandegee Estate
Jingyi Wang, Bart Lutterbach, Devin Ryan, Shatha AbuHammad, Yingpeng Liu, Leah Ragosta, Frank Chen, Tiffany Tsang, Breanna Zerfas, Nikki Kong, Jeevan GC, Justin Cruite, Jasmin Kruell, Katherine Donovan, Jirong, Luo, Lyn Jones, Fidel Huerta, Jonathan Tosi, Yang Yang, Henning Arlt, Yingde Zhu, John Che, Radek Nowak, Pratik Vikhe, Stephen Xie
Lyn Jones, Director, presenting to CPD
October Conference Presentations
Presenter - Justin Cruite
"Cereblon Covalent Modulation through Rational Design of Histidine Targeting Chemical Probes", 5th Annual Targeted Protein Degradation Summit - Pre-Conference Bootcamp, Boston North Shore, 10/25 - 10/28
Presenter - Nikki R. Kong
"Employing phenotypic assays to dissect mechanisms of molecular glue degraders", Discovery on Target - PROTACs and Molecular Glues, Boston 10/17-10/20; Panelist in interactive discussion: "Targeted Protein Degradation – Where Are We Headed?"
Presenter - Pratik Vikhe
"Modulation of T Helper Cells by IMiDs", Discovery on Target - Pre-conference symposium on Emerging Immune Modulation Strategies, Boston, 10/17-10/20
"Employing phenotypic assays to dissect mechanisms of molecular glue degraders", Discovery on Target - PROTACs and Molecular Glues, Boston 10/17-10/20; Panelist in interactive discussion: "Targeted Protein Degradation – Where Are We Headed?"
Presenter - Pratik Vikhe
"Modulation of T Helper Cells by IMiDs", Discovery on Target - Pre-conference symposium on Emerging Immune Modulation Strategies, Boston, 10/17-10/20
Team CPD | 2022 Jimmy Fund Walk October 2
Yingde Zhu, John Che, Nikki Kong & Spouse, Breanna Zerfas, Justin Cruite, Lyn Jones, Hellen Kim, Jennifer Lawrence, Jonathan Tosi & Family, Yingde Zhu, Pratik Vikhe, Jirong Luo, Huang Huang, Jingyi Wang, Kishan Mahase, Leah Ragosta, Radek Nowak, Katherine Donovan, Bart Lutterbach | Oct 2, 2022
Yingde Zhu, Yingpeng Liu, Huang Huang, John Che, Radek Nowak, Jirong Luo, Jennifer Lawrence, Bart Lutterbach, Jonathan Tosi & Family, Lyn Jones, Jingyi Wang, Leah Ragosta, Hellen Kim, Kishan Mahase, Nikki Kong, Breanna Zerfas
Yingde Zhu & spouse (below), John Che, Pratik Vikhe, Jennifer Lawrence, Hellen Kim, Devin Ryan, Breanna Zerfas, Jonathan Tosi & Family, Nikki Kong & spouse (right), Jirong Luo, Justin Cruite, Katherine Donovan, Lyn Jones, Leah Ragosta | Oct 2, 2022
September Publication
J Che and LH Jones. Covalent drugs targeting histidine – An unexploited opportunity? RSC Med. Chem. 2022, 13, 1121-1126.
https://pubs.rsc.org/en/content/articlehtml/2022/md/d2md00258b
J Che and LH Jones. Covalent drugs targeting histidine – An unexploited opportunity? RSC Med. Chem. 2022, 13, 1121-1126.
https://pubs.rsc.org/en/content/articlehtml/2022/md/d2md00258b
CPD Cricket Game | Sept 23, 2022
Our first cricket game as we bid farewell to summer
Devin Ryan, Joann Kalabathula, Bart Lutterbach, Leah Ragosta, Justin Cruite | Sept 23, 2022
CPD Leadership team | September 20
CPD Leadership completes leadership development training conducted by Jennifer Lawrence, Katie Ward, and Lyn Jones, PhD
Huang Huang, Radek Nowak, Jonathan Tosi, John Che, Katie Ward, Jennifer Lawrence, Breanna Zerfas, Hellen Kim, Lyn Jones, Kishan Mahase, Nikki Kong | Sept 20, 2022
Presentation
Lyn Jones - Assessing Cereblon Engagement by Targeted Protein Degraders.
Fall ACS, Chicago, August 2022.
Lyn Jones - Assessing Cereblon Engagement by Targeted Protein Degraders.
Fall ACS, Chicago, August 2022.
August New Hires
Shatha AbuHammad - Joins the CPD as a Scientist I with our Biology Team
Jeevan GC - Joins the CPD as a Scientist I with our Computation Team
Shatha AbuHammad - Joins the CPD as a Scientist I with our Biology Team
- Shatha just finished her postdoc at DFCI, where she investigated how TFE3 fusion proteins bind RNA to drive renal cell carcinoma. Prior to that, Shatha completed her PhD work at University of Melbourne, where she identified combinational therapies to co-target CDK4 and PRMT5, which will benefit melanoma patients. Shatha also has extensive CRISPR/Cas9 base-editing and phenotypic screening experiences.
Jeevan GC - Joins the CPD as a Scientist I with our Computation Team
- Jeevan came from Professor Joachim Frank Lab at Columbia University where he used MD simulation and single particle Cryo-EM to study conformational changes in Ryanodine receptors and allosteric modulation of GABAB receptor. Jeevan is an expert in MD simulations and conformational analysis.
July New Hires
Yang Yang - Joins the CPD as a Scientist I with our Biology Team
Jirong (Eric) Luo - Joins the CPD as a Scientist I with our Chemistry Team
Yang Yang - Joins the CPD as a Scientist I with our Biology Team
- We are excited to welcome Yang to the CPD & Biology team! Her postdoc training was completed at MGH, where she focused on small molecule and functional genomics screens to discover new therapeutic targets in idiopathic pulmonary fibrosis. Through her PhD and postdoc training, she has extensive experience in microscopy, CRISPR/Cas9 screens, and primary cell culturing.
Jirong (Eric) Luo - Joins the CPD as a Scientist I with our Chemistry Team
- We are also excited to welcome Jirong to the CPD! He received his PhD of Organic Chemistry at University of Houston (Supervisor: Jeremy A. May). He was focusing the development of enantioselective conjugate addition methodology and application to the total synthesis of Cannabinoids and Mucronatins during his PhD training.
Publication
JT Cruite, GP Dann, J Che, KD Donovan, S Ferrao, SB Ficarro, ES Fischer, NS Gray, F Huerta, NR Kong, H Liu, JA Marto, RJ Metivier, RP Nowak, BL Zerfas and LH Jones. Cereblon covalent modulation through structure-based design of histidine targeting chemical probes. RSC Chem. Biol. 2022, accepted.
https://pubs.rsc.org/en/content/articlelanding/2022/cb/d2cb00078
JT Cruite, GP Dann, J Che, KD Donovan, S Ferrao, SB Ficarro, ES Fischer, NS Gray, F Huerta, NR Kong, H Liu, JA Marto, RJ Metivier, RP Nowak, BL Zerfas and LH Jones. Cereblon covalent modulation through structure-based design of histidine targeting chemical probes. RSC Chem. Biol. 2022, accepted.
https://pubs.rsc.org/en/content/articlelanding/2022/cb/d2cb00078
Publication
LH Jones, CA Mitchell, L Loberg, M Pavlovic, M Rao, R Roberts, K Stamp, L Volak, MB Wittwer, S Pettit. Targeted protein degraders: a call for collective action to advance safety assessment. Nat. Rev. Drug Disc. 2022, 21, 401-402.
https://www.nature.com/articles/d41573-022-00055-9
LH Jones, CA Mitchell, L Loberg, M Pavlovic, M Rao, R Roberts, K Stamp, L Volak, MB Wittwer, S Pettit. Targeted protein degraders: a call for collective action to advance safety assessment. Nat. Rev. Drug Disc. 2022, 21, 401-402.
https://www.nature.com/articles/d41573-022-00055-9
Presentation
Lyn Jones - Covalent Modulation of Cereblon Using Sulfonyl Exchange Chemistry. DFCI Targeted Protein Webinar Series, June 2022.
Lyn Jones - Covalent Modulation of Cereblon Using Sulfonyl Exchange Chemistry. DFCI Targeted Protein Webinar Series, June 2022.
April New Hire
Jingyi Wang - Joins the CPD as a Scientist I with our Chemistry Team
Jingyi Wang - Joins the CPD as a Scientist I with our Chemistry Team
- We are excited to welcome Jingyi to the CPD! She worked at GSK as a medicinal chemist and developed an innovative drug-screening platform using solid-phase DNA Encoded Library technology. Before joining GSK, she received her PhD of Organic Chemistry at Boston College (Supervisor: X. Peter Zhang). During her PhD training, she developed several CoII-catalyzed asymmetric cyclization and C-H activation reactions to construct complex structures with stereoselectivities.
March New Hire
Yangchun (Frank) Chen - Joins the CPD as our Computational Biologist.
Yangchun (Frank) Chen - Joins the CPD as our Computational Biologist.
- Frank’s expertise is in analysis of correlations between genomics (including expressions) and phenotypes (including cellular and patient level). He will take a deep dive into the omics datasets from both public (e.g. depmap) and proprietary (e.g. proteomics, RRM screens) sources to identify potential targets of interest.
Presentation
Lyn Jones - Targeted Covalent Inhibitors and Molecular Superglues.
SMR/SCI Experimental and In Silico Approaches to Target Selection and Tractability for Drug Discovery, Francis Crick Institute, London, UK, March 2022.
Lyn Jones - Targeted Covalent Inhibitors and Molecular Superglues.
SMR/SCI Experimental and In Silico Approaches to Target Selection and Tractability for Drug Discovery, Francis Crick Institute, London, UK, March 2022.
Publication
ES Fischer and LH Jones. Small molecule modulation of protein polymerization. Chem. Soc. Rev. 2022, 51, 2392-2396
https://pubs.rsc.org/en/content/articlelanding/2022/cs/d2cs00070a
ES Fischer and LH Jones. Small molecule modulation of protein polymerization. Chem. Soc. Rev. 2022, 51, 2392-2396
https://pubs.rsc.org/en/content/articlelanding/2022/cs/d2cs00070a
Presentation
Lyn Jones - A Background to Targeted Protein Degradation
HESI PROTACs and Molecular Glues Safety Workshop (virtual), October 2021.
Lyn Jones - A Background to Targeted Protein Degradation
HESI PROTACs and Molecular Glues Safety Workshop (virtual), October 2021.
Publication:
NR Kong, H Liu, J Che, LH Jones. Physicochemistry of cereblon modulating drugs determines pharmacokinetics and disposition. ACS Med. Chem. Lett. 2021, 12, 1861-1865.
https://pubs.acs.org/doi/abs/10.1021/acsmedchemlett.1c00475
NR Kong, H Liu, J Che, LH Jones. Physicochemistry of cereblon modulating drugs determines pharmacokinetics and disposition. ACS Med. Chem. Lett. 2021, 12, 1861-1865.
https://pubs.acs.org/doi/abs/10.1021/acsmedchemlett.1c00475
Presentation:
Lyn Jones - Towards the Rational Design and Development of Targeted Protein Degraders
Gulf Coast Consortium, 2nd Annual Innovative Drug Discovery and Development Conference, Houston TX (virtual), May 2021.
Lyn Jones - Towards the Rational Design and Development of Targeted Protein Degraders
Gulf Coast Consortium, 2nd Annual Innovative Drug Discovery and Development Conference, Houston TX (virtual), May 2021.
Publication
R Nowak and LH Jones. Target validation using PROTACs: applying the 4 pillars framework. SLAS Disc. 2021, 26, 474-483
https://journals.sagepub.com/doi/full/10.1177/2472555220979584
R Nowak and LH Jones. Target validation using PROTACs: applying the 4 pillars framework. SLAS Disc. 2021, 26, 474-483
https://journals.sagepub.com/doi/full/10.1177/2472555220979584
Publication
M Kostic and LH Jones. Critical assessment of targeted protein degradation as a research tool and pharmacological modality. Trends Pharmacol. Sci. 2020, 41, 305-317.
https://www.cell.com/trends/pharmacological-sciences/fulltext/S0165-6147(20)30059-6
M Kostic and LH Jones. Critical assessment of targeted protein degradation as a research tool and pharmacological modality. Trends Pharmacol. Sci. 2020, 41, 305-317.
https://www.cell.com/trends/pharmacological-sciences/fulltext/S0165-6147(20)30059-6