Peptide Analogs

Zelos Therapeutics (www.zelostherapeutics.com) is developing a novel peptide analog of the parathyroid hormone (PTH) for postmenopausal osteoporosis, called Ostabolin-C (in Phase II trial).

“PTH has two important signaling domains, the first domain activates adenylate cyclase, and the second domain stimulates protein kinase C activity. Studies in in vitro and animal models revealed that the adenylate cyclase signaling component was responsible for the bone-stimulating activity of PTH. We realized that modulating adenylate cyclase had important implications for osteoporosis therapy,“ says Paul Morley, Ph.D., scientific founder and CSO of Zelos Therapeutics.

“Ostabolin-C activates bone-stimulation mechanisms, but does not affect bone resorption activity. Bone resorption leads to the side effects observed with existing injectable PTH drugs. Also, these injectables are more effective at reducing vertebral fractures than fractures of the hip or wrist. We anticipate that our peptide drug will have a lower incidence and severity of side effects and induce the formation of better quality bone at all of these sites,“ says Dr. Morley. Zelos has partnered with Nektar (www.nektar.com) to develop a pulmonary delivery formulation of Ostabolin-C.

Natural Vs. Combichem Approach

Ambryx Biotechnology (www.ambryxbiotech.com) performs systematic screening of naturally derived peptides. It has an anticancer peptide in the preclinical stage with three more in R&D. “We assessed secreted protein fractions derived from embryonic cells for apoptotic effects in multiple in vitro cancer cell models. We discovered a native protein that binds to zinc resulting in a conformation change revealing active peptide domains that have anticancer activity. We subsequently isolated the active peptide domain,“ says Helen Chen, Ph.D., VP of business development at Ambryx.

Ambryx anticancer peptide drug has natural glycosylation, so it has the potential to last longer in vivo and be truly bioavailable. “The peptide was 8 to 10 times more active than native protein as it does not require zinc for activity,“ says Dr. Chen. The company is currently gathering data in animal obesity models.

Peptide Drug Discovery Research

Peptides play an important role in modulating many physiological processes in our body. Some of the benefits of working with peptides are: they are small, easily optimized, and can be quickly investigated for therapeutic potential. However, the field of peptide drug discovery was hampered by their high manufacturing costs, short half-life, and limited in vivo bioavailability. All that is changing now. Waheed Danho, Ph.D., distinguished research leader at Hoffmann-La Roche (www.roche.com), says “Advancements in peptide manufacturing and improvements in peptide drug delivery systems have re-energized this field. It is now easier to screen a large number of targets with peptides and eliminate the unpromising ones early on in the discovery process.“ Rational drug design, an informed approach to drug discovery, is the preferred route for Roche, which has a fully integrated peptide research program based on rational drug design. “The quick-acting nature of peptides is often a disadvantage in many disease conditions. We perform extensive structure-activity-relationship studies to define peptide hot spots and use this information to design more potent, more specific, and more long-acting peptides,“ explains Dr. Danho

Bangalore BIO: BioPortEurope Makes Access To EU Markets Easy

An industry is considered to have arrived when allied businesses begin picking up steam. At the biotech capital of India, Bangalore, the country premier biotech show is on and among the announcements made is the low-key launch of BioPortEurope.

BioPortEurope is a one-stop-shop solution to facilitate Indian life sciences companies’ entry into the European market. Considering that India’s biotech industry has touched the $2 billion mark and is slated to grow at a fast pace, the service is timely and much needed, what with a number of Indian companies aspiring to enter the global markets.

BioPortEurope provides access to a mature network of experienced life sciences professionals in The Netherlands and in the EU member states including France, Switzerland, Germany, Spain, UK, Italy, Austria and Spain via its headquarters in Amsterdam. The service is available across the areas of pharmaceuticals, generics, vaccines, diagnostics, OTC & natural products, fine chemicals and technologies.

“We are business catalysts for the industry, providing services that range from market assessments to distribution,” said Dr Maarten van Dongen. He represents InnoTact Consulting, the company that has launched the concept of BioPortEurope in India. Dr Maarten is currently in the process of scouting for an office space in India. InnoTact Consulting is likely to open office in Bangalore.