Fragment-Based Drug Discovery: The MagHelix™ FBDD Platform by Creative Biostructure, Slides of Biology

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Fragment-based lead

discovery

Fragment-based drug discovery (FBDD) is one of the mainstream

strategies for lead discovery and optimization. Currently, more and

more compounds have entered the clinical stage based on this

approach. Creative Biostructure has established a MagHelix™ FBDD

Platform for early drug discovery, which covers advanced biophysical

detection instruments, such as the X-ray single crystal diffractometer,

high-performance nuclear magnetic resonance (NMR) instrument, and

surface plasmon resonance (SPR) instrument. With the FBDD platform,

we can provide customized drug discovery solutions for a wide variety

of disease areas and therapeutic targets, including complex targets

involving protein-protein interactions (PPI).

Advantages of Fragment-based Drug Discovery

• The probability of finding active small molecules is higher.
• The designed drugs has higher activity and selectivity.
• Reduce drug development costs. Screening a fragment library consisting of several

thousand fragments allows exploration of a much greater chemical space than screening

a million-level compound library.

• It is possible to find hit compounds targeting complex targets. The advantage of the

FBDD approach in identifying weakly bound fragments facilitates its targeting of PPI

targets with flat binding pockets.

How Our Fragment-based Drug Discovery Platform Works

Creative Biostructure follows the basic procedure of FBDD, namely construction of

fragment library, screening of active fragments and structural optimization of fragments,

and performs customizable fragment library design, fragment-based screening (FBS), as

well as fragment-to-lead solutions for FBDD. The following is our integrated FBDD

platform covering the entire process:

Reference

1.Van Montfort R L M.; et al. Current perspectives in fragment-based lead

discovery (FBLD). Essays in Biochemistry. 2017, 61(5): 453-464.

Related Sections

Lead Discovery and Optimization

High-throughput Screening (HTS)

MagHelix™ Library Design and Preparation

Fragment-based Screening (FBS)

Fragment-to-lead

Hit Biophysical Characterization

Thank you!

Excerpt from:

https://drug-discovery.creative-

biostructure.com/maghelix-fbdd-platform-p