Molecules of the Month

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Introduction to Molecules of the Month
This series highlights small molecules with recently published data or stories that are relevant and inspirational to our work. Scroll down to learn more.


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BMS-820132 (Bristol Myers Squibb) is an oral glucokinase (GK) partial activator intended for diabetes. GK activators for diabetes were hotly pursued in the late 2000s, with well over 100 industry patents on GK activators by 2009. The pursuit was triggered by the discovery of the first allosteric activators of glucokinase from an enzymatic screen of 120k compounds at Roche in 2003, leading to the first GK activator studied in diabetes patients. Initial clinical glucokinase full activators [...]


Unlike protein kinases, glucokinase (GK, hexokinase IV) phosphorylates glucose to glucose-6-phosphate. GK is not saturated at physiological glucose levels (~5 mM, enzyme Km ~8 mM) allowing it to have a role in “sensing” glucose levels. GK’s role in glucose control and relevance to diabetes is validated by human genetics: loss of function results in a form of diabetes called MODY-2, and gain of function results in persistent hypoglycemia. GK activation reduces blood sugar levels, but too much GK activation can lead to hypoglycemia (low blood sugar).


Mechanism of Action
To mitigate the risk of hypoglycemia, the BMS team, like some others, sought “partial” GK activators, rather than “full” activators. A partial GK activator would avoid lowering GK’s glucose Km too much, making GK activity still dependent on physiological glucose concentrations.


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The Molecules of the Month Process
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Research publications and news from each month are reviewed
Nominations for selection are accepted from readers and reviewers
Review blurb
Candidates are finalized by the editorial team and sent for community review and comment
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Molecules of the Month are published for public feedback
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Corresponding authors are notified for comment or correction and final edits are made
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What Makes a Great Molecule
Reviewers and editors focus on:
  1. First disclosures of molecules or new properties
  2. Clinical candidates with interesting profiles
  3. Non-clinical molecules with intriguing modes of action
  4. Interesting structures or unique properties
  5. Drug discovery stories with educational value
  6. Nominations by readers and reviewers

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