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Pharmacological effects of small molecule BCR-ABL tyrosine kinase inhibitors on platelet function [Cellular and Molecular]

ASPET

Overall, these new insights around the effects of ABL TKIs on platelet function could inform the development of targeted therapies with reduced hematologic toxicities. Significance Statement This study examines the effects of clinically relevant small molecule BCR-ABL tyrosine kinase inhibitors (TKIs) on platelet activity.

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Interactions of small molecule inhibitors with secreted phospholipase A2: A review of the structural data

Chemical Biology and Drug Design

While a number of sPLA 2 inhibitors have been described, compounds which have been co-crystallized with human sPLA 2 enzymes are of much importance as such three-dimensional structures provide valuable information regarding the structural requirements of good potency inhibitors as well as the molecular interactions between the enzyme and inhibitor.

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More LRRK2 On-Target Toxicity?

Drug Hunter

Clinical advancement of LRRK2 inhibitors was initially stalled by concerns about on-target lung findings in primates, but these were ameliorated by a Merck/Genentech/Pfizer/MJFF study showing that these lung changes were reversible, and Biogen/Denali has currently a small molecule (BIIB122/DNL151) in Ph. I ( NCT04557800 ).

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Molecules on the Move: April ’23

Drug Hunter

This article compiles 20+ recent small molecules of general interest in the news in April 2023, with structures where they are available. Drug Hunter Premium is drug discovery, distilled, so you can quickly catch up and make informed decisions based on industry examples. Get ahead now by requesting a trial. already a member?

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Metabolism of 2023 FDA Approved Small Molecules – PART 2

Metabolite Tales Blog

Table 1: Small molecule drugs approved by the FDA in 2023 with reported involvement of phase II mechanisms In vitro : In vivo differences Incubation of the SGLT2 (sodium-glucose co-transporter-2) inhibitor bexagliflozin in human liver microsomes points to metabolism through both oxidation and glucuronidation to 6 main metabolites.

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ChEMBL brings drug bioactivity data to the Protein Data Bank in Europe

The ChEMBL-og

But here's the catch: while ChEMBL provides extensive information on a molecule's activity and cross references to other data sources, it doesn't always tell us if a 3D structure is available for a specific drug-target complex. This can be a roadblock for researchers who need that structural information to design effective drugs.

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Metabolism of 2023 FDA Approved Small Molecules – PART 1

Metabolite Tales Blog

Metabolism of 2023 FDA Approved Small Molecules – PART 1 By Julia Shanu-Wilson 2023 was a fruitful year for drug approvals by the FDA, with a crop of 34 small molecules out of a total of 55 new drugs [1]. References [1] 2023 Novel Small Molecule FDA Drug Approvals. link] [4] Licea Perez et al.,