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So far Circle Pharma has created 33 blog entries.

Circle Pharma Announces Appointment of Co-Founder Prof. Matthew Jacobson to Department Chair

2017-09-25T12:45:19+00:00 January 19th, 2016|Press Releases|

Circle Pharma, Inc., today announced that co-founder Prof. Matthew Jacobson has been appointed Chair of the UCSF Department of Pharmaceutical Chemistry.
 
“This is a terrific recognition of Matt’s exceptional accomplishments as a scientist and his passionate commitment as an educator,” said David J. Earp, JD, PhD, Circle’s President and CEO. “We are very appreciative of the guidance and leadership that our two co-founders – Matt Jacobson and Scott Lokey – continue to provide to Circle.”
[…]

Circle Pharma Announces Receipt of Additional Seed Investment, and Relocation to New Laboratory Facility

2017-09-25T10:00:43+00:00 January 7th, 2016|Press Releases|

Circle Pharma, Inc., today announced that it has extended its seed funding round with an investment from ShangPharma Investment Group Limited. In conjunction with this investment, Circle has relocated to office and laboratory space in South San Francisco.

“The addition of laboratory operations to our computational chemistry platform marks the next stage of Circle’s development,” said David J. Earp, J.D., Ph.D., Circle’s President and CEO, “and we have now initiated work on Circle’s internal p […]

Starting up and spinning out: The changing nature of partnerships between pharma and academia

2017-09-19T08:55:30+00:00 September 4th, 2015|In the News|

In 2005, two chemists decided to work together to develop libraries of cyclic peptides—strings of amino acids formed in the shape of a circle—that could be used to treat a range of infectious diseases, autoimmunity and cancer. Thanks to their flexibility, these cyclic peptides can access different parts of a protein target and so bind to …

Read article at natureM […]

Going Out on a Limb: Delineating The Effects of β-Branching, N-Methylation, and Side Chain Size on the Passive Permeability, Solubility, and Flexibility of Sanguinamide A Analogues

2017-09-19T11:41:12+00:00 August 26th, 2015|by our Team Members, Publications|

by Andrew T. Bockus, Joshua A. Schwochert, Cameron R. Pye, Chad E. Townsend, Vong Sok, Maria A. Bednarek, and R. Scott Lokey

It is well established that intramolecular hydrogen bonding and N-methylation play important roles in the passive permeability of cyclic peptides, but other structural features have been explored less intensively. Recent studies on the oral bioavailability of the cyclic heptapeptide sanguinamide A have raised the question of whether steric occlusion of polar gr […]

Beyond cyclosporine A: conformation-dependent passive membrane permeabilities of cyclic peptide natural products

2017-09-19T11:58:18+00:00 June 12th, 2015|by our Team Members, Publications|

by Christopher L Ahlbach, Katrina W Lexa, Andrew T Bockus, Valerie Chen, Phillip Crews, Matthew P Jacobson & R Scott Lokey

Many cyclic peptide natural products are larger and structurally more complex than conventional small molecule drugs. Although some molecules in this class are known to possess favorable pharmacokinetic properties, there have been few reports on the membrane permeabilities of cyclic peptide natural products. Here, we present the passive membrane permeabilities of […]

Peptide to Peptoid Substitutions Increase Cell Permeability in Cyclic Hexapeptides

2017-09-19T11:32:50+00:00 June 5th, 2015|by our Team Members, Publications|

by Joshua Schwochert, Rushia Turner, Melissa Thang, Ray F Berkeley, Alexandra R Ponkey, Kelsie M. Rodriguez, Siegfried S F Leung, Bhagyashree Khunte, Gilles Goetz, Chris Limberakis, Amit S. Kalgutkar, Heather Eng, Michael J. Shapiro, Alan M. Mathiowetz, David A. Price, Spiros Liras, Matthew P. Jacobson, and R. Scott Lokey

The effect of peptide-to-peptoid substitutions on the passive membrane permeability of an N-methylated cyclic hexapeptide is examined. In general, substitutions mai […]

Probing the Physicochemical Boundaries of Cell Permeability and Oral Bioavailability in Lipophilic Macrocycles Inspired by Natural Products

2017-09-19T11:53:16+00:00 May 7th, 2015|by our Team Members, Publications|

by Andrew T. Bockus, Katrina W. Lexa, Cameron R. Pye, Amit S. Kalgutkar, Jarret W. Gardner, Kathryn C. R. Hund, William M. Hewitt, Joshua A. Schwochert, Emerson Glassey, David A. Price, Alan M. Mathiowetz, Spiros Liras, Matthew P. Jacobson, and R. Scott Lokey

Cyclic peptide natural products contain a variety of conserved, nonproteinogenic structural elements such as d-amino acids and amide N-methylation. In addition, many cyclic peptides incorporate γ-amino acids and other elements d […]

Cell-permeable cyclic peptides from synthetic libraries inspired by natural products

2017-09-25T11:59:19+00:00 January 21st, 2015|by our Team Members, Publications|

by Hewitt WM, Leung SS, Pye CR, Ponkey AR, Bednarek M, Jacobson MP, Lokey RS

Drug design efforts are turning to a new generation of therapeutic targets, such as protein-protein interactions (PPIs), that had previously been considered “undruggable” by typical small molecules. There is an emerging view that accessing these targets will require molecules that are larger and more complex than typical small molecule drugs. Here, we present a methodology for the discovery of geometrically […]

Optimizing the Permeability and Oral Bioavailability of Macrocycles

2017-09-25T12:51:15+00:00 October 16th, 2014|by our Team Members, Publications|

by Alan M. Mathiowetz, Siegfried S. F. Leung and Matthew P. Jacobson

Macrocycles have a number of inherent advantages that improve their prospects for achieving oral bioavailability, even when their physical properties lie outside the traditional Rule-of-5 chemistry space. This chapter provides an overview of these advantages, with particular attention given to the potential for macrocycles to adopt three-dimensional conformations that overcome barriers to permeability. An overview o […]