UK-383367 / Pfizer - LARVOL DELTA

BMP1 Appears to be Involved in GPER1-mediated Progression and Tamoxifen Resistance of Luminal A Breast Cancer Cells. (PubMed, Cancer Genomics Proteomics) - "BMP1 appears to be involved in GPER1-mediated progression of luminal A breast cancer cells. In addition, BMP1 may play a role in tamoxifen-resistance."

Journal • Breast Cancer • Hormone Receptor Breast Cancer • Oncology • Solid Tumor • GPER1

BMP-1 inhibition modulates tumor growth and cytokine responses in combination with doxorubicin in a mouse model of metastatic breast cancer (CICON 2025) - "This study was supported by TÜBİTAK 122Z177. Keywords: Breast cancer, BMP-1, UK-383367, Doxorubicin, cytokines"

Combination therapy • Metastases • Preclinical • Breast Cancer • Oncology • Solid Tumor • IFNG • IL10 • IL6 • TNFA

BMP1 inhibitor UK383367 improves MI-induced cardiac remodeling and fibrosis in mice via ameliorating macrophage polarization and mitochondrial dysfunction. (PubMed, Acta Pharmacol Sin) - "Overall, these results reveal a pivotal yet detrimental role for BMP1 in driving myocardial fibrosis and amplifying inflammatory cascades after MI. This study highlights the therapeutic potential of the BMP1 inhibitor UK383367 as a promising alternative to conventional antifibrotic strategies, potentially curbing the progression toward HF."

Journal • Preclinical • Cardiovascular • Congestive Heart Failure • Fibrosis • Heart Failure • Immunology • Inflammation • Metabolic Disorders • Myocardial Infarction • IL6 • TNFA

Poldip2 mediates blood-brain barrier disruption and cerebral edema by inducing AQP4 polarity loss in mouse bacterial meningitis model. (PubMed, CNS Neurosci Ther) - "Poldip2 inhibition alleviated brain edema and preserved the integrity of BBB partially by relieving the loss of AQP4 polarity via MMPs/β-DG pathway."

Journal • Preclinical • Cardiovascular • CNS Disorders • Infectious Disease • Ischemic stroke • Glial Fibrillary Acidic Protein • POLD1

Inhibitors of BMP-1/tolloid-like proteinases: efficacy, selectivity and cellular toxicity. (PubMed, FEBS Open Bio) - "...As a first step towards the identification of suitable tools to be used in functional studies, we have undertaken a systematic comparison of seven molecules known to affect the proteolytic activity of human astacins including three hydroxamates (FG-2575, UK383,367, S33A), the protein sizzled, a new phosphinic inhibitor (RXP-1001) and broad-spectrum protease inhibitors (GM6001, actinonin)...We found that these molecules display very different potency and selectivity profiles, with hydroxamate FG-2575 and the protein sizzled being very powerful and selective inhibitors of BMP-1, whereas phosphinic peptide RXP-1001 behaves as a broad-spectrum inhibitor of astacins. Their use should therefore be carefully considered in agreement with the aim of the study to avoid result misinterpretation."

Clinical • Journal • Biosimilar • Oncology • Ophthalmology

BMP1 inhibitor UK-383,367 attenuates renal fibrosis and inflammation in CKD. (PubMed, Am J Physiol Renal Physiol) - "In vitro, UK383,367 pretreatment inhibited the induction of collagen I/III, fibronectin, and α-SMA in both mPTCs and NRK-49F cells treated with TGF-β1. Taken together, these findings indicated that BMP1 inhibitor UK383,367 could serve as a potential drug in antagonizing CKD renal fibrosis by acting on the maturation and deposition of collagen and subsequent profibrotic response and inflammation."

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Bone morphogenetic protein 1 cleaves the linker region between ligand-binding repeats 4 and 5 of the LDL receptor and makes the LDL receptor non-functional. (PubMed, Hum Mol Genet) - "This conclusion is based upon the use of the specific BMP1 inhibitor UK 383367, silencing of the BMP1 gene by the use of siRNA or CRISPR/Cas9 technology and overexpression of wild-type BMP1 or the loss-of-function mutant E214A-BMP1...Targeting BMP1 could represent a novel strategy to increase the number of functioning LDLRs in order to lower plasma LDL cholesterol levels. However, a concern by using BMP1 inhibitors as cholesterol-lowering drugs, could be the risk of side-effects due to the important role of BMP1 in collagen assembly."

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