Proceedings - Boulder Peptide Foundation

BPS 2023

Modulating the cardiovascular pharmacology of apelin and elabela peptide by structural constraints

Kien Tran

Postdoctoral Fellow, Universite de Montreal

ABSTRACT

Apelin receptor (APJ) belongs to the class A G-proteins coupled receptor (GPCR) and plays a major role in cardiovascular functions. Recently, small molecules targeting APJ have entered clinical stages for the treatment of heart failure and muscular aging. Those small molecules bring the treatment closer than ever to the patient, but this is made possible only by a deep understanding of the underlying pharmacology which was gained through decades of studies using peptides as an experimental tool. Apelin and elabela are two endogenous ligands of the apelin receptor. By using different methods of structural modification, such as macrocyclization, substitution by unnatural and constrained amino acids, we elucidated key binding elements of those endogenous peptides. We compared them and used this knowledge to improve the affinity, the drug like properties as well as diversified their signaling profile. Several modified analogs have lower molecule weight compared to apelin-13 but significant longer half-life (t1/2 in vivo up to 3.7 h vs apelin-13, t1/2 < 1 min in Sprague-Dawley rat) and produce sustained cardiac effects.

BIO

Kien TRAN earned his PhD in Pharmacology at the UniversitÃ© de Sherbrooke, Canada and he is currently a postdoctoral fellow at the Institute for Research in Immunology and Cancer, Universite de Montreal. The main theme of his work consists of developing macrocyclic ligands for challenging targets such as peptide-binding GPCR (apelin receptor) or protein-protein interaction interface (oncogenic Ras).

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.