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So far Circle Pharma has created 33 blog entries.

Cyclic peptide natural products chart the frontier of oral bioavailability in the pursuit of undruggable targets

2017-10-18T18:12:11+00:00 October 18th, 2017|by our Team Members, Publications|

by Matthew R. Naylor, Andrew T. Backus, Maria-Jesus Blanco, Scott Lokey Highlights

  • The pursuit of ‘undruggable’ therapeutic targets has reinvigorated interest in natural products.
  • Peptides have been traditionally considered poor pharmaceutical candidates.
  • Some large cyclic peptide natural products have proven bioactivity and oral bioavailability.
  • Cyclic peptides have been synthesized to explore ADME optimization.
  • […]

Discovery of potent and orally bioavailable macrocyclic peptide-peptoid hybrid CXCR7 modulators.

2017-10-18T17:35:18+00:00 October 18th, 2017|by our Team Members, Publications|

by Markus Boehm, Kevin Beaumont, Rhys M Jones, Amit S. Kalgutkar, Liying Zhang, Karen Atkinson, Guoyun Bai, Janice A. Brown, Heather Eng, Gilles H. Goetz, Brian R Holder, Bhagyashree Khunte, Sarah Lazzaro, Chris Limberakis, Sangwoo Ryu, Michael J Shapiro, Laurie Tylaska, Jiangli Yan, Rushia Turner, Siegfried S. F. Leung, Mahesh Ramaseshan, David A. Price, Spiros Liras, Matthew P Jacobson, David J. Earp, R. Scott Lokey, Alan M Mathiowetz, and Elnaz Menhaji-Klotz ABSTRACT: The chemokin […]

Circle Pharma announces expansion of Series A financing and appointment of James C. Lu to its board

2017-09-25T14:41:44+00:00 April 5th, 2017|Press Releases|

Funds will be used to advance Circle’s computational and synthetic chemistry platform for macrocyclic peptide therapeutics Circle Pharma, Inc. today announced that it has completed an expansion of its Series A financing, with new investors W.I. Harper Group, Elements Partners, LLC, Whitesun Healthcare Ventures Limited and LifeForce Capital joining the round. Mission Bay Capital led Circle’s Series A, with Pfizer Inc. (NYSE:PFE), ShangPharma Investment Group, Ltd. and a syndicated group of in […]

Nonclassical Size Dependence of Permeation Defines Bounds for Passive Adsorption of Large Drug Molecules

2017-09-25T14:46:59+00:00 January 6th, 2017|by our Team Members, Publications|

by Cameron R. Pye, William M. Hewitt, Joshua Schwochert, Terra D. Haddad, Chad E. Townsend, Lyns Etienne, Yongtong Lao, Chris Limberakis, Akihiro Furukawa, Alan M. Mathiowetz, David A. Price, Spiros Liras, and R. Scott Lokey

Macrocyclic peptides are considered large enough to inhibit “undruggable” targets, but the design of passively cell-permeable molecules in this space remains a challenge due to the poorly understood role of molecular size on passive membrane permeability. Usi […]

Circle Pharma announces Series A financing and appoints Walter H. Moos, Ph.D., to its board

2017-09-25T09:59:00+00:00 December 21st, 2016|Press Releases|

Circle Pharma, Inc. today announced a Series A financing round in which it has issued over $4.5M of shares of Series A Preferred Stock. The financing was led by Mission Bay Capital, with Pfizer Inc. (NYSE:PFE), ShangPharma Investment Group, Ltd. and a syndicated group of individual investors joining the round. In connection with the financing, Walter H. Moos, Ph.D., representing ShangPharma, has joined the Circle Board of Directors.

“We are delighted with the participation of such high calibe […]

Passive Membrane Permeability in Cyclic Peptomer Scaffolds Is Robust to Extensive Variation in Side Chain Functionality and Backbone Geometry

2017-09-19T11:47:52+00:00 October 3rd, 2016|by our Team Members, Publications|

by Akihiro Furukawa, Chad E. Townsend, Joshua Schwochert, Cameron R. Pye, Maria A. Bednarek, and R. Scott Lokey

Synthetic and natural cyclic peptides provide a testing ground for studying membrane permeability in nontraditional drug scaffolds. Cyclic peptomers, which incorporate peptide and N-alkylglycine (peptoid) residues, combine the stereochemical and geometric complexity of peptides with the functional group diversity accessible to peptoids. We synthesized cyclic peptomer librar […]

Circle Pharma enters into an agreement with Pfizer to build screening library of macrocyclic peptides

2017-09-25T12:43:52+00:00 September 12th, 2016|Press Releases|

CirclePharma, Inc., today announced that it will apply its computational design and synthetic chemistry platform to design and create a physical screening library of novel macrocyclicpeptides. Once completed, the library is initially expected to comprise several hundred macrocycles that will be designed to potentially disrupt bioactive conformations commonly found in protein-protein interactions known to drive disease processes, and will deploy backbone scaffolds screened in silica for intrinsic […]

Stereochemistry Balances Cell Permeability and Solubility in the Naturally Derived Phepropeptin Cyclic Peptides

2017-09-19T11:49:36+00:00 June 6th, 2016|by our Team Members, Publications|

by Joshua Schwochert, Yongtong Lao, Cameron R. Pye, Matthew R. Naylor, Prashant V. Desai, Isabel C. Gonzalez Valcarcel, Jaclyn A. Barrett, Geri Sawada, Maria-Jesus Blanco, and R. Scott Lokey

Cyclic peptide (CP) natural products provide useful model systems for mapping “beyond-Rule-of-5” (bRo5) space. We identified the phepropeptins as natural product CPs with potential cell permeability. Synthesis of the phepropeptins and epimeric analogues revealed much more rapid cellular permeabil […]

Simple Predictive Models of Passive Membrane Permeability Incorporating Size-Dependent Membrane-Water Partition

2017-09-26T11:28:09+00:00 May 23rd, 2016|by our Team Members, Publications|

by Leung SS, Sindhikara D, Jacobson MP

We investigate the relationship between passive permeability and molecular size, in the context of solubility-diffusion theory, using a diverse compound set with molecular weights ranging from 151 to 828, which have all been characterized in a consistent manner using the RRCK cell monolayer assay. Computationally, each compound was subjected to extensive conformational search and physics-based permeability prediction, and multiple linear regress […]