AN-0128 / Pfizer - LARVOL DELTA

Boron-Containing Drug Candidates in Clinical Trials. (PubMed, Handb Exp Pharmacol) - "The agents reviewed include borofalan, delanzomib, flovagatran, dutogliptin, talabostat, numidargistat, OATD-02, AN0128, epetraborole, ganfeborole, acoziborole, taniborbactam, xeruborbactam, and sodium borocaptate, as well as the five FDA-approved boroncontaining drugs (bortezomib, ixazomib, crisaborole, tavaborole, vaborbactam). The review also highlights how clinical success depends on matching pharmacology with unmet need, feasible administration, competitive differentiation, and durable development partnerships. Ongoing advances in scaffold design, delivery, combination therapy, and indication selection are expected to broaden the therapeutic impact of boron-containing medicines."

Journal • Cardiovascular • Head and Neck Cancer • Hematological Disorders • Infectious Disease • Oncology • Pulmonary Disease • Respiratory Diseases • Solid Tumor • Thrombosis • Tuberculosis

Full-length transcriptomic profiling reveals age-associated isoform remodeling and altered coding potential in the mouse ovary. (PubMed, J Ovarian Res) - "Exploratory WGCNA highlighted modules associated with aging and cell-type specificity, including an Esr1-derived hub transcript, TALONT000180938, from a gene previously linked to ovarian function and disease. Many disease-associated genes exhibited cell-type-specific isoform usage, with several novel isoforms undetectable at the gene level. Our results indicate that long-read sequencing improves isoform-level resolution of ovarian transcriptomic diversity and identifies candidate aging-associated transcript alterations that may be relevant to reproductive decline."

Journal • Preclinical • ER

Chairside clinicomicrobiological assessment of subgingival boric acid irrigation in periodontitis patients: A randomized controlled trial. (PubMed, J Indian Soc Periodontol) - "Elemental boron has a positive role in many functions in the human body, such as immune regulation, wound healing, bone health maintenance, etc. A boron-containing molecule (AN0128) has shown additional antimicrobial properties against virulent red-complex bacteria...Outcomes of the present trial demonstrated boron's significant role in clinical improvements. Adjunctive subgingival boric acid irrigation can be effective in healing following phase-I therapy."

Clinical • Journal • Dental Disorders • Periodontitis

Halogenated Dipyridine Alkaloids from Actinoalloteichus cyanogriseus and Its Mutant Strain upon Precursor Feeding. (PubMed, J Nat Prod) - "Nineteen uncovered 2,2'-dipyridine alkaloids (1-19), along with six previously reported analogues (20-25), were isolated from the wild strain Actinoalloteichus cyanogriseus OUCMDZ-413 and its mutant strain CRM005...The molecular structures of these compounds were determined through spectroscopic analysis. Notably, the novel compounds showed cytotoxicity against the HCT-116, B16, and K562 tumor cell lines, with IC50 values ranging from 0.16 to 11 μM."

Journal • Oncology

Ring Expansion of Cyclic Boronates via Oxyboration of Arynes. (PubMed, J Am Chem Soc) - "A series of 2-aryl-1,3,2-dioxaborolane derivatives were reacted with aryne precursors in the presence of CsF to give the corresponding ring-expanded seven-membered borinic acid esters via selective boron-oxygen bond activation. Preliminary experimental mechanistic studies and density functional theory (DFT) calculations suggest that this unprecedented aryne oxyboration proceeds through the formation of boron ate complexes of arylboronates with CsF, followed by aryne insertion into the boron-oxygen bond."

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