BPS 2016
Novel Synthetic Strategies for Insulin and Related Peptides
Fa Liu
Director of Chemistry, Novo Nordisk
ABSTRACT
The challenges involved in the chemical synthesis of insulin and its analogs hinder the exploration of the structure-function relationships of this indispensable therapeutic. Problematic features such as the hydrophobicity of the A-chain and the complexity of the disulfide architecture are unique to insulin and have required implementation of specialized strategies. Our efforts have centered on two fundamental approaches: the single chain biomimetic route and the two-chain directed disulfide method. An example of the former is our use a novel single chain precursor “desDi†which enabled superior folding efficiency and proved to be less sensitive to individual substitutions. The latter approach is exemplified by the directed disulfide approach using orthogonally protected cysteine pairs to form insulin. We have additionally expanded the scope of the two-chain directed disulfide method to other insulin like peptides which contain oxidation-sensitive residues through the use of an iodine-free method employing Phacm cysteine protection and enzymatic conversion to form the (A7-B7) disulfide bond. We will also highlight application of the isoacyl concept to address the hydrophobicity of the A-chain and preparative recovery of both chains. Application of the isoacyl route afforded human insulin in 24% overall yield based on initial resin substitution representing the most efficient chemical synthesis of human insulin to date.
BIO
Information for BPS Presenters
The Boulder Peptide Foundation was established to further the science and knowledge of peptide technology to develop novel therapeutics, biomaterials, medical diagnostics and other beneficial uses for mankind. As part of this goal we run several programs to support career advancement, seminars and educational events. Join us on our mission to expand the applications of peptide science.
Information for BPS Presenters
The purpose of the Boulder Peptide Symposium is to encourage sharing of information related to peptide therapeutic development with an emphasis on the technical, scientific and regulatory aspects of the pharmaceutical development. Presentations that demonstrate original thinking or share experiences from case studies in product development shall receive priority over others.
The Boulder Peptide Symposium offers multiple opportunities for participants to present.
Oral Presentations in Scientific Sessions
The session topics for Scientific Program are Peptides in the Clinic, Drug Delivery, Chemistry of Complex Peptides, Spotlight on Discovery, and Peptide Showcase. Abstracts may be submitted via the Apply to Present page on the website. Submissions will be reviewed by the Scientific Advisory Board on a monthly basis and the speaker will be notified of a decision.
Presentation length: Format is 25-30 minutes slide presentation with 5-10 minutes for Q&A, with the exception of Peptide Showcase talks which are 10 minute slide presentations with 5 minutes for Q&A. Please confirm with your session chair to confirm the exact presentation length.
Invited Speakers: Speakers are requested to supply their presentation details 30 days after receiving an invitation to present.
Program Book Deadline: Final abstract and title must be provided no later than September 1st. No changes to the program are possible after this date.
Presentation Format: Oral presenters please provide your presentation slides to the A/V table on the day of your presentation.
Lodging: All speakers are requested to reserve their own room. Discount rates at the conference hotel are available until August 16th.
Registration: All speakers, excluding sponsored presentation speakers, receive a complimentary registration upon approval of the abstract.
Peptide Showcase Description
The Peptide Showcase is an opportunity for an individual or company to “showcase” new ideas, technology and pipeline assets. Priority shall be given to presentations from biotech and startup companies. Service providers and vendors are not eligible. Speakers in the session receive a complimentary event registration.
Posters
Posters can be presented on any topic relevant to peptides including original research, innovative products and technologies.
Eligibility- Any attendee (from academia, industry, biotech or vendor/sponsor) can present a poster. The presentation must contain original scientific thinking. To submit a poster go to the Submit a Poster link from the meeting menu. All submissions are reviewed on a rolling basis and will be notified of approval. September 1st is the last day to submit a poster abstract. Approved posters are published on the BPF website.
A 30 ” x 40″ board shall be provided with thumb tacks. Board will be on an easel and can be rotated for either landscape or portrait formats. Once you apply for a poster, you will get email confirmation that your poster was accepted. The poster session and number assignments will be emailed one week before the Symposium.
Poster boards shall be available for display from 8am to 8pm the day of your assigned poster session. See the program agenda for the poster session schedule.
Public Release
Every presentation at the Boulder Peptide Symposium is automatically recorded. Speakers are required to give consent for sharing of the presentation video with the peptide community.