Publications

LP-284, a small molecule acylfulvene, exerts potent antitumor activity in preclinical non-Hodgkin's lymphoma models and in cells deficient in DNA damage repair

Jianli Zhou, Drew Sturtevant, Cassie Love, Aditya Kulkarni, Neha Biyani, Umesh Kathad, Elizabeth Thacker, Sandeep Dave, and Kishor Bhatia

Artificial intelligence platform, RADR®, aids in the discovery of DNA damaging agent for the ultra-rare cancer Atypical Teratoid Rhabdoid Tumors

Joseph McDermott, Drew Sturtevant, Umesh Kathad, Sudhir Varma, Jianli Zhou, Aditya Kulkarni, Neha Biyani, Caleb Schimke, William C. Reinhold, Fathi Elloumi, Peter Carr, Yves Pommier and Kishor Bhatia

The acylfulvene alkylating agent, LP-184, retains nanomolar potency in non-small cell lung cancer carrying otherwise therapy-refractory mutations

Kulkarni A., McDermott J. R., Kathad U., Modali R., Richard J. P., Sharma P., Bhatia K.

A machine learning‐based gene signature of response to the novel alkylating agent LP‐184 distinguishes its potential tumor indications

Umesh Kathad, Aditya Kulkarni, Joseph Ryan McDermott, Jordan Wegner, Peter Carr, Neha Biyani, Rama Modali, Jean‐Philippe Richard, Panna Sharma and Kishor Bhatia

A machine learning‑based gene signature of response to the novel alkylating agent LP‑184 distinguishes its potential tumor indications

Kathad U., Kulkarni A., McDermott J. R., Wegner J., Carr P., Biyani N., Modali R., Richard J. P., Sharma P., Bhatia K.

Hydroxyurea derivatives of irofulven with improved antitumor efficacy

Staake M.D., Kashinatham A., McMorris T.C., Estes L.A., Kelner M.J.

Cysteine specific targeting of the functionally distinct peroxiredoxin and glutaredoxin proteins by the investigational disulfide BNP7787

Parker A.R., Petluru P.N., Nienaber V.L., Badger J., Leverett B.D., Jair K., Sridhar V., Logan C., Ayala P.Y., Kochat H., Hausheer F.H.

Novel covalent modification of human anaplastic lymphoma kinase (ALK) and potentiation of crizotinib-mediated inhibition of ALK activity by BNP7787

Parker A.R., Petluru P.N., Nienaber V.L., Zhao M., Ayala P.Y., Badger J., Chie-Leon B., Sridhar V., Logan C., Kochat H., Hausheer F.H.

Improved efficacy of acylfulvene in colon cancer cells when combined with a nuclear excision repair inhibitor

Van Midwoud P.M., Sturla S.J.

Up-regulation of human prostaglandin reductase 1 improves the efficacy of hydroxymethylacylfulvene, an antitumor chemotherapeutic agent

Yu X., Erzinger M.M., Pietsch K.E., Cervoni-Curet F.N., Whang J., Niederhuber J., Sturla S.J.

Phase I and pharmacologic study of BNP7787, a novel chemoprotector in patients with advanced non-small cell lung cancer

Masuda N., Negoro S., Hausheer F., Nakagawa K., Matsui K., Kudoh S., Takeda K., Yamamoto N., Yoshimura N., Ohashi Y., Fukuoka M.

Enantioselective total synthesis of (−)-Acylfulvene and (−)- Irofulven

Siegel D.S., Piizzi G., Piersanti G., Movassaghi M.

Influence of irofulven, a transcription-coupled repair-specific antitumor agent, on RNA polymerase activity, stability and dynamics in living mammalian cells

Escargueil A.E., Poindessous V., Soares D.G., Sarasin A., Cook P.R., Larsen A.K.

Phase I and pharmacokinetic study of the novel chemoprotector BNP7787 in combination with cisplatin and attempt to eliminate the hydration schedule

Boven E., Westerman M., van Groeningen C.J., Verschraagen M., Ruijter R., Zegers I., van der Vijgh W.J.F., Giaccone G.

Activity of irofulven against human pancreatic carcinoma cell lines in vitro and in vivo

Van Laar E.S., Roth S., Weitman S., MacDonald J.R., Waters S.J.

Apoptosis induction by the dual-action DNA- and protein-reactive antitumor drug irofulven is largely Bcl-2-independent

Herzig M.C., Trevino A.V., Liang H., Salinas R., Waters S.J., MacDonald J.R., Woynarowska B.A., Woynarowski J.M.

Anti-tumour compounds illudin S and Irofulven induce DNA lesions ignored by global repair and exclusively processed by transcription- and replication-coupled repair pathways

Jaspers N.G., Raams A., Kelner M.J., Ng J.M., Yamashita Y.M., Takeda S., McMorris T.C., Hoeijmakers J.H.

Enhanced antitumor activity of irofulven in combination with antimitotic agents

Michael J. Kelner, Trevor C. McMorris, Rafael J. Rojas, Nicole A. Trani, Tami R. Velasco, Leita A. Estes and Pharnuk Suthipinijtham

Efficacy of MGI 114 (6-hydroxymethylacylfulvene, HMAF) against the mdr1/gp170 metastatic MV522 lung carcinoma xenograft

Kelner M.J., McMorris T.C., Estes L., Samson K.M., Bagnell R.D., Taetle R.

Efficacy of HMAF (MGI-114) in the MV522 metastatic lung carcinoma xenograft model nonresponsive to traditional anticancer agents

Kelner M.J., McMorris T.C., Estes L., Wang W., Samson K.M., Taetle R.

Efficacy of acylfulvene illudili analogues against a metastatic lung carcinoma MV 522 xenograft nonresponsive to traditional anticancer agents: retention of activity against various mdr phenotypes and unusual cytotoxicity against ERCC 2

Efficacy of acylfulvene illudili analogues against a metastatic lung carcinoma MV 522 xenograft nonresponsive to traditional anticancer agents: retention of activity against various mdr phenotypes and unusual cytotoxicity against ERCC 2 and ERCC 3 DNA helicase-deficient cells

Kelner M.J., Mcmorris T.C., Estes L.A., Starr R.J., Rutherford M., Montoya M., Samson K.M., Taetle R.

Characterization of illudin S sensitivity in DNA repair-deficient Chinese hamster cells. Unusually high sensitivity of ERCC2 and ERCC3 DNA helicase-deficient mutants in comparison to other chemotherapeutic agents

Kelner M.J., McMorris T.C., Estes L., Rutherford M., Montoya M., Goldstein J., Samson K., Starr R., Taetle R.