SDpress December 2015

 

WuXi News

Dr. Ge Li Receives Executive of the Year Award from SCRIP

WuXi and MedImmune Form Strategic Alliance to Develop Innovative Biologics in China for AstraZeneca

WuXi and Lilly Collaborate to Develop Novel Therapeutics in China

WuXi Global Forum 2016 at J.P. Morgan Conference

WuXi Healthcare Ventures II Closes with Oversubscription

Gilead Sciences and WuXi Partner for a Dedicated Analytical and Stability Testing Facility

Cancer, Meet the Alamo: San Antonio Enlists WuXi NextCODE to Speed Unparalleled Open-access Cancer Genome Project

Congratulations to Novira Therapeutics for its Acquisition Agreement with Johnson & Johnson
Innovation That Matters

Combating the Hep B Virus: An Interview with George Hartman, Novira Therapeutics
Perspectives

Combining Service and Investment: An Interview with Wei Li, Co-Founder of WuXi Healthcare Ventures

Developing a Novel ADC for Global Market via Innovative Three-party Collaboration – An Interview with Dr. Jiawen Han, VP of WuXi Biologics

Prospects for Cell and Gene Therapy: An Interview with Alan Moore, VP of Strategic Accounts and Cell Manufacturing

Meet IDSU Leadership: An Interview with Tao Guo, VP of Medicinal Chemistry
In This Issue:
Industry Beats

FDA Approvals & Designations

Upcoming Events

January 12, 2016
DNC Auditorium
The Scripps Research Institute
 
January 20-22, 2016
Salk Institute
February 24, 2016
The Lodge at Torrey Pines

 

 

IDSUpress December 2015

Meet IDSU Leadership

Meet IDSU Leadership: Tao Guo, Vice President of Medicinal Chemistry

 

IDSU Collaborator Publications

Innovation That Matters

Combatting the Hep B Virus: An Interview with George Hartman, Novira Therapeutics

 

WuXi News

 

WuXi and Lilly Collaborate to Develop Novel Therapeutics in China

Congratulations to Novira Therapeutics for its Acquisition Agreement with Johnson & Johnson
In Case You Missed It

Medicinal Chemistry

Novel recurrent mutations in ethanolamine kinase 1 (ETNK1) gene in systemic mastocytosis with eosinophilia and chronic myelomonocytic leukemia. T L Lasho et. al. Blood Cancer Journal 2015 5(e275).

Broad anti-tumor activity of a small molecule that selectively targets the Warburg effect and lipogenesis. Colin. A. Flaveny et al. Cancer Cell (2015) 28, pp. 42-56. 

Inhibiting one kinase to kill them all, Leslie K. Ferrarelli. Science Signaling, 2015, 8 (397) pp. ec284.

 

Remote control of therapeutic T cells through a small molecule-gated chimeric receptor Chia-Yung Wu, et. al. Science, 2015, 8 (399), pp. ec300.

Synthetic Chemistry

A fluorinated ligand enables room-temperature and regioselective pd-catalyzed fluorination of aryl triflates and bromides. Aaron C. Sather et. al. Journal of the American Chemical Society, 2015.  

In This Issue
Industry Beats

 

Merck Serono Expands Biopharmaceutical R&D Facility to Accelerate Innovation at Darmstadt Headquarters (Source: EMD Group)

 

FDA Updates

Upcoming Events

December 3, 2015
London, U.K.
December 15-20, 2015
Honolulu, HI
January 20-21, 2016
London, U.K.
February 21-24, 2016
San Diego, CA
February 24-26, 2016
Budapest, Hungary
 
February 29-March 2, 2016
San Diego, CA

 

An Interview with Tao Guo, VP of Medicinal Chemistry

Dr. Tao Guo Interview Banner

 

Dr. Tao Guo serves as Vice President of Medicinal Chemistry, International Discovery Service Unit (IDSU). Dr. Guo joined WuXi AppTec in December 2008, bringing with him a wealth of experience in medicinal chemistry and drug discovery. He is an inventor of 10 preclinical candidate compounds with 2 advanced to Phase III and 1 advanced to Phase II. He is the recipient of 37 issued U.S. patents and the author of over 50 peer-reviewed papers. He has served on the NIH Expert Review Panels, the Princeton ACS Fall Organic Chemistry Symposium Organizing Committee, the Editorial Board of ChemTracts – Organic Chemistry, and as the President and CEO of the CGP-Doering Foundation. In 2011, Dr. Guo received the Shanghai inaugural “Thousands Plan” award. We sat down with Dr. Guo to learn more about his background in medicinal chemistry and his insights on IDSU.

Dr. Guo, you are an experienced medicinal chemist, a veteran in the field. Can you tell us more about your background before joining WuXi?

Tao: I have known Dr. Ge Li for many years from our time together at Columbia University and Pharmacopeia. I greatly admire his courage and vision in founding WuXi. At Pharmacopeia, I worked with WuXi’s FTE teams for a number of programs that I led and was extremely impressed by the high quality work and the impact that WuXi had on my projects. I ultimately decided to join WuXi in 2008 because I was inspired by Dr. Li’s vision in transforming drug discovery through an open access platform. I am excited to be here and to contribute to WuXi’s growth.

After years of working in biotech in the U.S., you are now working with our IDSU teams in China. How is working in China different from working in the U.S.?

Tao: The teams in China are young and energetic. The average age of WuXi employees in China is 29. We offer numerous training programs at WuXi for young scientists. For young chemists, we have a range of chemistry and management training including synthetic chemistry, medicinal chemistry, and program management. Coming to work every day, I feel the strong enthusiasm and energy from our young scientists. I am very proud to see the rapid growth of our young employees and their impactful contributions to our partners’ programs.

What sort of results and impact have you seen with our IDSU teams in China?

Tao: IDSU teams in China have demonstrated strong capabilities in synthetic and medicinal chemistry. Over the last year, the teams have delivered over 70,000 compounds for over 100 clients from pharma, biotech, and non-profit organizations. The teams have discovered over 25 preclinical candidate compounds, including compounds that have received breakthrough therapy designations from FDA, serving as examples of our vision, “invented in China, for the world”. The teams’ efforts have made positive contributions to the successful IPO/partnering of 5 biotech companies.

IDSU has achieved a lot in the past decade. What do you see as future directions for IDSU?

Tao: We are building IDSU to be the best solutions provider in synthetic and medicinal chemistry to clients around the globe. As IDSU has become the largest capability and technology platform for discovery chemistry service in pharmaceutical and biotech industry, the insights gained from our many years of deep experience help us develop a range of tailored solutions to best meet the different needs of our diverse customers. We also continue to strengthen our technology capabilities to keep our leadership position in discovery chemistry.

Thank you for taking the time to talk with us. To finish, would you like to share an inspiring experience or event in the field that has impacted you?

Tao: The Nobel Prize Committee awarding William C. Campbell, Satoshi Omura, and Youyou Tu with the 2015 Nobel Prizes in Physiology and Medicine for their discovery of ivermectin and (+)-artminsinin was very inspirational to me this year. Ivermectin and Artminsin are used to cure diseases caused by parasitic roundworms and malaria, respectively. William C. Campbell was a chemist at Merck when he made his discovery of ivermectin; his recognition was encouraging to all in the drug discovery industry. Youyou Tu’s recognition was especially impactful for all Chinese scientists and chemists here in WuXi, as she was the first Chinese scientist to earn the Nobel Prize.

 

Medicinal Chemistry

 

Novel recurrent mutations in ethanolamine kinase 1 (ETNK1) gene in systemic mastocytosis with eosinophilia and chronic myelomonocytic leukemia. T L Lasho et. al. Blood Cancer Journal 2015 5(e275).

 

A new family of choline kinase inhibitors with antiproliferative and antitumor activity derived from natural products. A. Estvez-Braun, et. al.,Clinical Translational Oncology. 2015, 7(1) pp. 74-84.

 

Phosphoenolpyruvate Is a Metabolic Checkpoint of Anti-tumor T Cell Responses. Ho PC, et. al., Cell, 2015, 162(6), pp.1217-28.

 

Broad anti-tumor activity of a small molecule that selectively targets the Warburg effect and lipogenesis. Colin. A. Flaveny et al. Cancer Cell (2015) 28, pp. 42-56. 

 

Differentiation of pluripotent stem cells to muscle fiber to model Duchenne muscular dystrophy. Jerome Chal, et. al., Nature Biotechnology, 2015, 33, pp. 962-969.

 

ST2 blockade reduces sST2-producing T cells while maintaining protective mST2-expressing T cells during graft-versus-host disease, Jilu Zhang et. al., Science Translational Medicine, 2015, 7 (308)

 

Tet2 is required to resolve inflammation by recruiting Hdac2 to specifically repress IL-6. Qian Zhang, et. al., Nature, 2015, 525, pp. 389-393.

 

Identification of the first inverse agonist of retinoid-related orphan receptor (ROR) with dual selectivity for RORB and RORyT. Christian Gege, et. al. Bioorganic & Medicinal Chem Letters. 2014, 24(22), pp. 5265-7. 

 

Nicotinamide N-methyltransferase regulates hepatic nutrient metabolism through Sirt1 protein stabilization. Shangyu Hong et. al. Nature Medicine, 2015, 21(8), pp. 887-94.

 

A small-molecule antivirulence agent for treating Clostridium difficile infection, Kristina Oresic Bender et. al., Science Translational Medicine, 2015, 7 (306).

 

GPR3, a therapeutic target for AD? Orla Smith. Science Signalling, 2015, 8 (399), pp. ec305.

 

Loss of GPR3 reduces the amyloid plaque burden and improves memory in Alzheimer’s disease mouse models. Yunhong Huang, et. al., Science Translational Medicine, 2015, 7 (309) pp. 309ra164.

 

Nuclear receptor Nurr1 agonists enhance its dual functions and improve behavioral deficits in an animal model of Parkinson’s disease. Chun-Hyung Kim et. al., Proceedings of the National Academy of Sciences of the United States of America. 2015, 112(28) pp.8756-61.

 

Combination cancer immunotherapy and new immunomodulatory targets. Kathleen M. Mahoney et. al. Nature Reviews Drug Discovery, 2015, 14, pp. 561-584.

 

Big opportunities for small molecules in immuno-oncology. Jerry L. Adams, etc. al. Nature Reviews Drug Discovery, 2015, 14, 603-622.

 

Inhibiting one kinase to kill them all, Leslie K. Ferrarelli. Science Signaling, 2015, 8 (397) pp. ec284.

 

Targeting human cancer by a glycosaminoglycan binding malaria protein. Ali Salanti et al. Cancer Cell, 2015, 28 (4), pp. 500-514. 

 

Finding the good in malaria. Leslie K. Ferrarelli. Science Signaling, 2015, 8 (397), pp. ec297.

 

BET inhibitor resistance emerges from leukaemia stem cells. Chun Yew Fong, et al. Nature, 2015, 525, pp. 538-542.

 

Transcriptional plasticity promotes primary and acquired resistance to BET inhibition. Philipp Rathert, et al. Nature, 2015, 525, pp. 543-547.

 

Combined inhibition of BET family proteins and histone deacetylases as a potential epigenetics-based therapy for pancreatic ductal adenocarcinoma. Pawel Mazur, et al. Nature Medicine, 2015, 21, pp.1163-1171.

 

PET imaging of tumor glycolysis downstream of hexokinase through noninvasive measurement of pyruvate kinase M2. Timothy Witney, et. al. Science Translational Medicine, 2015, 7(310) pp. 310ra169.

 

The proinflammatory role of HECTD2 in innate immunity and experimental lung injury. Tiffany Coon et.al. Science Translational Medicine, 2015, 7(295). pp. 295ra109.

 

TH2 and TH17 inflammatory pathways are reciprocally regulated in asthma. David Choy, et. al. Science Translational Medicine, 2015, 7 (301), pp. 301ra129.

 

Reversal of diet-induced obesity and insulin resistance by inducible genetic ablation of GRK2. Rocio Vila-Bedmar, et. al. Science Signaling, 2015 8 (386), pp. ra73.

 

PCSK6-mediated corin activation is essential for normal blood pressure, Shenghan Chen, et. al. Nature Medicine, 2015, 21, pp. 1048-1053.

 

Dengue virus NS1 triggers endothelial permeability and vascular leak that is prevented by NS1 vaccination. P. Robert Beatty, et. al. Science Translational Medicine. 2015, 7 (304), pp. 304ra141.

 

Disruption of mGluR5 in parvalbumin-positive interneurons induces core features of neurodevelopmental disorders. S. A. Barnes et. al. Molecular Psychiatry. 2015, 20, pp. 1161-1172.

 

UDCA exerts beneficial effect on mitochondrial dysfunction in LRRK2G2019S carriers and in vivo. Heather Mortiboys, et. al. Neurology. 2015, 85 (10), pp. 846-852.

 

Human Acid B-Glucosidase Inhibition by Carbohydrate Derived Iminosugars: Towards New Pharmacological Chaperones for Gaucher Disease. Camilla Parmeggiani, et. al. Chembiochem, 2015, 16 (14), pp. 2054-64.

 

Speedy repair with stabilized B-catenin. Tanya J Shaw, Science Translational. 2015, 7 (297), pp. 297ec125.

 

The Dishevelled-binding protein CXXC5 negatively regulates cutaneous wound healing. Soung H. Lee et al., JEM, 2015, 7 (297), pp. 297ec125.

 

Neuronal PAC1 receptors mediate delayed activation and sensitization of trigeminocervical neurons: Relevance to migraine. Simon Akerman, et. al. Science Translational Medicine, 2015, 7 (308), pp. 308ra157.

 

FTO obesity variant circuitry and adipocyte browning in humans. Melina Claussnitzer, et. al. New England Journal of Medicine, 2015, 373, pp. 895-907.
Remote control of therapeutic T cells through a small molecule-gated chimeric receptor Chia-Yung Wu, et. al. Science, 2015, 8 (399), pp. ec300.

 

Synthetic Chemistry

A fluorinated ligand enables room-temperature and regioselective pd-catalyzed fluorination of aryl triflates and bromides. Aaron C. Sather et. al. Journal of the American Chemical Society, 2015.  

 

Phthalimide conjugation as a strategy for in vivo target protein degradation. Georg E. Winter et. al. Science, 2015, 348 (6241), pp. 1376-1381. 

 

Dosage delivery of sensitive reagents enables glove-box-free synthesis. Stephen L. Buchwald et. al. Nature, 2015, 524, pp. 208-211.