Developmental Therapeutics Program

The DF/HCC Developmental Therapeutics Program fosters the development of new anti-cancer agents by harnessing basic science and the translational and clinical resources of the DF/HCC member institutions. Residing at a key point in the pipeline of discovery, the Program provides the expertise and opportunity through which promising new leads and agents are developed first in Phase I trials and then in Phase II trials, in conjunction with DF/HCC’s disease-based programs.

The Program also serves as an important conduit for the acquisition of agents from the NCI and industry and for those agents transition to Phase II trials in disease-based programs. Increasingly, the Program’s trials seek to establish biomarkers useful in patient selection and in proof of action. It relies on multiple sources of information, including genomic analysis of initial and sequential tumor biopsies, as well as genomic studies of circulating DNA and circulating tumor cells and imaging to determine biomarkers of response and drug resistance. Developmental Therapeutics studies not only define optimal dose and schedule but also incorporate proof-of-mechanism and proof-of-principle endpoints. Currently, the Program has more than 50 members.

Recent Publications

  • Desai J, Alonso G, Kim SH, Cervantes A, Karasic T, Medina L, Shacham-Shmueli E, Cosman R, Falcon A, Gort E, Guren T, Massarelli E, Miller WH, Paz-Ares L, Prenen H, Amatu A, Cremolini C, Kim TW, Moreno V, Ou SI, Passardi A, Sacher A, Santoro A, Stec R, Ulahannan S, Arbour K, Lorusso P, Luo J, Patel MR, Choi Y, Shi Z, Mandlekar S, Lin MT, Royer-Joo S, Chang J, Jun T, Dharia NV, Schutzman JL, , Han SW. Divarasib plus cetuximab in KRAS G12C-positive colorectal cancer: a phase 1b trial. Nat Med 2023. PubMed
  • Kooshesh KA, Foy BH, Sykes DB, Gustafsson K, Scadden DT. Health Consequences of Thymus Removal in Adults. N Engl J Med 2023; 389:406-417. PubMed
  • Ascierto PA, Dummer R, Gogas HJ, Arance A, Mandala M, Liszkay G, Garbe C, Schadendorf D, Krajsova I, Gutzmer R, Chiarion-Sileni V, Dutriaux C, de Groot JWB, Yamazaki N, Loquai C, Robert C, Flaherty KT. Contribution of MEK Inhibition to BRAF/MEK Inhibitor Combination Treatment of -Mutant Melanoma: Part 2 of the Randomized, Open-Label, Phase III COLUMBUS Trial. J Clin Oncol 2023. PubMed
  • Sahu A, Wang X, Munson P, Klomp JPG, Wang X, Gu SS, Han Y, Qian G, Nicol P, Zeng Z, Wang C, Tokheim C, Zhang W, Fu J, Wang J, Nair NU, Rens JAP, Bourajjaj M, Jansen B, Leenders I, Lemmers J, Musters M, van Zanten S, van Zelst L, Worthington J, Liu JS, Juric D, Meyer CA, Oubrie A, Liu XS, Fisher DE, Flaherty KT. Discovery of Targets for Immune-Metabolic Antitumor Drugs Identifies Estrogen-Related Receptor Alpha. 2023; 13:672-701. PubMed
  • Abbou S, Klega K, Tsuji J, Tanhaemami M, Hall D, Barkauskas DA, Krailo MD, Cibulskis C, Nag A, Thorner AR, Pollock S, Imamovic-Tuco A, Shern JF, DuBois SG, Venkatramani R, Hawkins DS, Crompton BD. Circulating Tumor DNA Is Prognostic in Intermediate-Risk Rhabdomyosarcoma: A Report From the Children's Oncology Group. J Clin Oncol 2023. PubMed
  • Sun Y, Hu L, Tao Z, Jarugumilli GK, Erb H, Singh A, Li Q, Cotton JL, Greninger P, Egan RK, Tony Ip Y, Benes CH, Che J, Mao J, Wu X. Pharmacological blockade of TEAD-YAP reveals its therapeutic limitation in cancer cells. Nat Commun 2022; 13:6744. PubMed
  • Morimoto Y, Fushimi A, Yamashita N, Hagiwara M, Bhattacharya A, Cheng J, Frost TC, Ahmad R, Daimon T, Huang L, Hata T, Takahashi H, Yamamoto M, Suzuki Y, DeCaprio JA, Kufe D. Addiction of Merkel cell carcinoma to MUC1-C identifies a potential new target for treatment. Oncogene 2022; 41:3511-3523. PubMed
  • Ng TSC, Hu H, Kronister S, Lee C, Li R, Gerosa L, Stopka SA, Burgenske DM, Khurana I, Regan MS, Vallabhaneni S, Putta N, Scott E, Matvey D, Giobbie-Hurder A, Kohler RH, Sarkaria JN, Parangi S, Sorger PK, Agar NYR, Jacene HA, Sullivan RJ, Buchbinder E, Mikula H, Weissleder R, Miller MA. Overcoming differential tumor penetration of BRAF inhibitors using computationally guided combination therapy. Sci Adv 2022; 8:eabl6339. PubMed
  • Hagiwara M, Fushimi A, Yamashita N, Bhattacharya A, Rajabi H, Long MD, Yasumizu Y, Oya M, Liu S, Kufe D. MUC1-C activates the PBAF chromatin remodeling complex in integrating redox balance with progression of human prostate cancer stem cells. Oncogene 2021; 40:4930-4940. PubMed
  • Pereira B, Chen CT, Goyal L, Walmsley C, Pinto CJ, Baiev I, Allen R, Henderson L, Saha S, Reyes S, Taylor MS, Fitzgerald DM, Broudo MW, Sahu A, Gao X, Winckler W, Brannon AR, Engelman JA, Leary R, Stone JR, Campbell CD, Juric D. Cell-free DNA captures tumor heterogeneity and driver alterations in rapid autopsies with pre-treated metastatic cancer. Nat Commun 2021; 12:3199. PubMed
  • Li R, Ng TSC, Wang SJ, Prytyskach M, Rodell CB, Mikula H, Kohler RH, Garlin MA, Lauffenburger DA, Parangi S, Dinulescu DM, Bardeesy N, Weissleder R, Miller MA. Therapeutically reprogrammed nutrient signalling enhances nanoparticulate albumin bound drug uptake and efficacy in KRAS-mutant cancer. Nat Nanotechnol 2021. PubMed
  • Kalinsky K, Hong F, McCourt CK, Sachdev JC, Mitchell EP, Zwiebel JA, Doyle LA, McShane LM, Li S, Gray RJ, Rubinstein LV, Patton D, Williams PM, Hamilton SR, Conley BA, O'Dwyer PJ, Harris LN, Arteaga CL, Chen AP, Flaherty KT. Effect of Capivasertib in Patients With an AKT1 E17K-Mutated Tumor: NCI-MATCH Subprotocol EAY131-Y Nonrandomized Trial. JAMA Oncol 2021; 7:271-278. PubMed
  • Flaherty KT, Gray RJ, Chen AP, Li S, McShane LM, Patton D, Hamilton SR, Williams PM, Iafrate AJ, Sklar J, Mitchell EP, Harris LN, Takebe N, Sims DJ, Coffey B, Fu T, Routbort M, Zwiebel JA, Rubinstein LV, Little RF, Arteaga CL, Comis R, Abrams JS, O'Dwyer PJ, Conley BA, . Molecular Landscape and Actionable Alterations in a Genomically Guided Cancer Clinical Trial: National Cancer Institute Molecular Analysis for Therapy Choice (NCI-MATCH). J Clin Oncol 2020; 38:3883-3894. PubMed
  • Janku F, Abdul Razak AR, Chi P, Heinrich MC, von Mehren M, Jones RL, Ganjoo K, Trent J, Gelderblom H, Somaiah N, Hu S, Rosen O, Su Y, Ruiz-Soto R, Gordon M, George S. Switch Control Inhibition of KIT and PDGFRA in Patients With Advanced Gastrointestinal Stromal Tumor: A Phase I Study of Ripretinib. J Clin Oncol 2020; 38:3294-3303. PubMed
  • Korshavn KJ, Wales TE, Bird GH, Engen JR, Walensky LD. A redox switch regulates the structure and function of anti-apoptotic BFL-1. Nat Struct Mol Biol 2020; 27:781-789. PubMed
  • Cathcart AM, Bird GH, Wales TE, Herce HD, Harvey EP, Hauseman ZJ, Newman CE, Adhikary U, Prew MS, Oo T, Lee S, Engen JR, Walensky LD. Targeting a helix-in-groove interaction between E1 and E2 blocks ubiquitin transfer. Nat Chem Biol 2020. PubMed
  • Li Q, Sun Y, Jarugumilli GK, Liu S, Dang K, Cotton JL, Xiol J, Chan PY, DeRan M, Ma L, Li R, Zhu LJ, Li JH, Leiter AB, Ip YT, Camargo FD, Luo X, Johnson RL, Wu X, Mao J. Lats1/2 Sustain Intestinal Stem Cells and Wnt Activation through TEAD-Dependent and Independent Transcription. Cell Stem Cell 2020; 26:675-692.e8. PubMed
  • Hauseman ZJ, Harvey EP, Newman CE, Wales TE, Bucci JC, Mintseris J, Schweppe DK, David L, Fan L, Cohen DT, Herce HD, Mourtada R, Ben-Nun Y, Bloch NB, Hansen SB, Wu H, Gygi SP, Engen JR, Walensky LD. Homogeneous Oligomers of Pro-apoptotic BAX Reveal Structural Determinants of Mitochondrial Membrane Permeabilization. Mol Cell 2020. PubMed
  • Flaherty KT, Gray R, Chen A, Li S, Patton D, Hamilton SR, Williams PM, Mitchell EP, Iafrate AJ, Sklar J, Harris LN, McShane LM, Rubinstein LV, Sims DJ, Routbort M, Coffey B, Fu T, Zwiebel JA, Little RF, Marinucci D, Catalano R, Magnan R, Kibbe W, Weil C, Tricoli JV, Alexander B, Kumar S, Schwartz GK, Meric-Bernstam F, Lih CJ, McCaskill-Stevens W, Caimi P, Takebe N, Datta V, Arteaga CL, Abrams JS, Comis R, O'Dwyer PJ, Conley BA, . THE MOLECULAR ANALYSIS FOR THERAPY CHOICE (NCI-MATCH) TRIAL: LESSONS for GENOMIC TRIAL DESIGN. Journal of the National Cancer Institute 2020. PubMed
  • Doebele RC, Drilon A, Paz-Ares L, Siena S, Shaw AT, Farago AF, Blakely CM, Seto T, Cho BC, Tosi D, Besse B, Chawla SP, Bazhenova L, Krauss JC, Chae YK, Barve M, Garrido-Laguna I, Liu SV, Conkling P, John T, Fakih M, Sigal D, Loong HH, Buchschacher GL, Garrido P, Nieva J, Steuer C, Overbeck TR, Bowles DW, Fox E, Riehl T, Chow-Maneval E, Simmons B, Cui N, Johnson A, Eng S, Wilson TR, Demetri GD, . Entrectinib in patients with advanced or metastatic NTRK fusion-positive solid tumours: integrated analysis of three phase 1-2 trials. Lancet Oncol. 2019. PubMed
  • Konstantinopoulos PA, Luo W, Liu JF, Gulhan DC, Krasner C, Ishizuka JJ, Gockley AA, Buss M, Growdon WB, Crowe H, Campos S, Lindeman NI, Hill S, Stover E, Schumer S, Wright AA, Curtis J, Quinn R, Whalen C, Gray KP, Penson RT, Cannistra SA, Fleming GF, Matulonis UA. Phase II Study of Avelumab in Patients With Mismatch Repair Deficient and Mismatch Repair Proficient Recurrent/Persistent Endometrial Cancer. J Clin Oncol 2019. PubMed
  • Konstantinopoulos PA, Waggoner S, Vidal GA, Mita M, Moroney JW, Holloway R, Van Le L, Sachdev JC, Chapman-Davis E, Colon-Otero G, Penson RT, Matulonis UA, Kim YB, Moore KN, Swisher EM, Färkkilä A, D'Andrea A, Stringer-Reasor E, Wang J, Buerstatte N, Arora S, Graham JR, Bobilev D, Dezube BJ, Munster P. Single-Arm Phases 1 and 2 Trial of Niraparib in Combination With Pembrolizumab in Patients With Recurrent Platinum-Resistant Ovarian Carcinoma. JAMA Oncol 2019. PubMed
  • Vinayak S, Tolaney SM, Schwartzberg L, Mita M, McCann G, Tan AR, Wahner-Hendrickson AE, Forero A, Anders C, Wulf GM, Dillon P, Lynce F, Zarwan C, Erban JK, Zhou Y, Buerstatte N, Graham JR, Arora S, Dezube BJ, Telli ML. Open-Label Clinical Trial of Niraparib Combined With Pembrolizumab for Treatment of Advanced or Metastatic Triple-Negative Breast Cancer. JAMA Oncol 2019. PubMed
  • Pantelidou C, Sonzogni O, De Oliveria Taveira M, Mehta AK, Kothari A, Wang D, Visal T, Li MK, Pinto J, Castrillon JA, Cheney EM, Bouwman P, Jonkers J, Rottenberg S, Guerriero JL, Wulf GM, Shapiro GI. PARP Inhibitor Efficacy Depends on CD8 T-cell Recruitment via Intratumoral STING Pathway Activation in BRCA-Deficient Models of Triple-Negative Breast Cancer. 2019; 9:722-737. PubMed
  • Cornell L, Wander SA, Visal T, Wagle N, Shapiro GI. MicroRNA-Mediated Suppression of the TGF-β Pathway Confers Transmissible and Reversible CDK4/6 Inhibitor Resistance. Cell Rep 2019; 26:2667-2680.e7. PubMed
  • Konstantinopoulos PA, Barry WT, Birrer M, Westin SN, Cadoo KA, Shapiro GI, Mayer EL, O'Cearbhaill RE, Coleman RL, Kochupurakkal B, Whalen C, Curtis J, Farooq S, Luo W, Eismann J, Buss MK, Aghajanian C, Mills GB, Palakurthi S, Kirschmeier P, Liu J, Cantley LC, Kaufmann SH, Swisher EM, D'Andrea AD, Winer E, Wulf GM, Matulonis UA. Olaparib and α-specific PI3K inhibitor alpelisib for patients with epithelial ovarian cancer: a dose-escalation and dose-expansion phase 1b trial. Lancet Oncol. 2019; 20:570-580. PubMed
  • Eismann J, Heng YJ, Fleischmann-Rose K, Tobias AM, Phillips J, Wulf GM, Kansal KJ. Interdisciplinary Management of Transgender Individuals at Risk for Breast Cancer: Case Reports and Review of the Literature. Clin Breast Cancer 2018. PubMed
  • Nangia V, Siddiqui FM, Caenepeel S, Timonina D, Bilton SJ, Phan N, Gomez-Caraballo M, Archibald HL, Li C, Fraser C, Rigas D, Vajda K, Ferris LA, Lanuti M, Wright CD, Raskin KA, Cahill DP, Shin JH, Keyes C, Sequist LV, Piotrowska Z, Farago AF, Azzoli CG, Gainor JF, Sarosiek KA, Brown SP, Coxon A, Benes CH, Hughes PE, Hata AN. Exploiting MCL-1 dependency with combination MEK + MCL-1 inhibitors leads to induction of apoptosis and tumor regression in KRAS mutant non-small cell lung cancer. 2018. PubMed
  • Guerra RM, Bird GH, Harvey EP, Dharia NV, Korshavn KJ, Prew MS, Stegmaier K, Walensky LD. Precision Targeting of BFL-1/A1 and an ATM Co-dependency in Human Cancer. Cell Rep 2018; 24:3393-3403.e5. PubMed
  • Reinshagen C, Bhere D, Choi SH, Hutten S, Nesterenko I, Wakimoto H, Le Roux E, Rizvi A, Du W, Minicucci C, Shah K. CRISPR-enhanced engineering of therapy-sensitive cancer cells for self-targeting of primary and metastatic tumors. Sci Transl Med 2018. PubMed
  • Hemming ML, Lawlor MA, Zeid R, Lesluyes T, Fletcher JA, Raut CP, Sicinska ET, Chibon F, Armstrong SA, Demetri GD, Bradner JE. Gastrointestinal stromal tumor enhancers support a transcription factor network predictive of clinical outcome. Proc Natl Acad Sci U S A 2018; 115:E5746-E5755. PubMed
  • Panchamoorthy G, Jin C, Raina D, Bharti A, Yamamoto M, Adeebge D, Zhao Q, Bronson R, Jiang S, Li L, Suzuki Y, Tagde A, Ghoroghchian PP, Wong KK, Kharbanda S, Kufe D. Targeting the human MUC1-C oncoprotein with an antibody-drug conjugate. JCI Insight 2018. PubMed
  • Hazar-Rethinam M, Kleyman M, Han GC, Liu D, Ahronian LG, Shahzade HA, Chen L, Parikh AR, Allen JN, Clark JW, Kwak EL, Faris JE, Murphy JE, Hong TS, Van Seventer EE, Nadres B, Hong CB, Gurski JM, Jessop NA, Dias-Santagata D, Iafrate AJ, Van Allen EM, Corcoran RB. Convergent Therapeutic Strategies to Overcome the Heterogeneity of Acquired Resistance inColorectal Cancer. 2018; 8:417-427. PubMed
  • Escudero S, Zaganjor E, Lee S, Mill CP, Morgan AM, Crawford EB, Chen J, Wales TE, Mourtada R, Luccarelli J, Bird GH, Steidl U, Engen JR, Haigis MC, Opferman JT, Walensky LD. Dynamic Regulation of Long-Chain Fatty Acid Oxidation by a Noncanonical Interaction between the MCL-1 BH3 Helix and VLCAD. Mol Cell 2018; 69:729-743.e7. PubMed
  • Moschos SJ, Sullivan RJ, Hwu WJ, Ramanathan RK, Adjei AA, Fong PC, Shapira-Frommer R, Tawbi HA, Rubino J, Rush TS, Zhang D, Miselis NR, Samatar AA, Chun P, Rubin EH, Schiller J, Long BJ, Dayananth P, Carr D, Kirschmeier P, Bishop WR, Deng Y, Cooper A, Shipps GW, Moreno BH, Robert L, Ribas A, Flaherty KT. Development of MK-8353, an orally administered ERK1/2 inhibitor, in patients with advanced solid tumors. JCI Insight 2018. PubMed
  • Maeda T, Hiraki M, Jin C, Rajabi H, Tagde A, Alam M, Bouillez A, Hu X, Suzuki Y, Miyo M, Hata T, Hinohara K, Kufe D. MUC1-C Induces PD-L1 and Immune Evasion in Triple-Negative Breast Cancer. Cancer Res 2018; 78:205-215. PubMed
  • Schmid D, Park CG, Hartl CA, Subedi N, Cartwright AN, Puerto RB, Zheng Y, Maiarana J, Freeman GJ, Wucherpfennig KW, Irvine DJ, Goldberg MS. T cell-targeting nanoparticles focus delivery of immunotherapy to improve antitumor immunity. Nat Commun 2017; 8:1747. PubMed
  • Sullivan RJ, Infante JR, Janku F, Wong DJL, Sosman JA, Keedy V, Patel MR, Shapiro GI, Mier JW, Tolcher AW, Wang-Gillam A, Sznol M, Flaherty K, Buchbinder E, Carvajal RD, Varghese AM, Lacouture ME, Ribas A, Patel SP, DeCrescenzo GA, Emery CM, Groover AL, Saha S, Varterasian M, Welsch DJ, Hyman DM, Li BT. First-in-Class ERK1/2 Inhibitor Ulixertinib (BVD-523) in Patients with MAPK Mutant Advanced Solid Tumors: Results of a Phase I Dose-Escalation and Expansion Study. 2017. PubMed
  • Bédard PL, Davies MA, Kopetz S, Juric D, Shapiro GI, Luke JJ, Spreafico A, Wu B, Castell C, Gomez C, Cartot-Cotton S, Mazuir F, Dubar M, Micallef S, Demers B, Flaherty KT. First-in-human trial of the PI3Kβ-selective inhibitor SAR260301 in patients with advanced solid tumors. Cancer 2017. PubMed
  • Weisberg EL, Schauer NJ, Yang J, Lamberto I, Doherty L, Bhatt S, Nonami A, Meng C, Letai A, Wright R, Tiv H, Gokhale PC, Ritorto MS, De Cesare V, Trost M, Christodoulou A, Christie A, Weinstock DM, Adamia S, Stone R, Chauhan D, Anderson KC, Seo HS, Dhe-Paganon S, Sattler M, Gray NS, Griffin JD, Buhrlage SJ. Inhibition of USP10 induces degradation of oncogenic FLT3. Nat Chem Biol 2017. PubMed
  • Hong TS, Wo JY, Borger DR, Yeap BY, McDonnell EI, Willers H, Blaszkowsky LS, Kwak EL, Allen JN, Clark JW, Tanguturi S, Goyal L, Murphy JE, Wolfgang JA, Drapek LC, Arellano RS, Mamon HJ, Mullen JT, Tanabe KK, Ferrone CR, Ryan DP, Iafrate AJ, DeLaney TF, Zhu AX. Phase II Study of Proton-Based Stereotactic Body Radiation Therapy for Liver Metastases: Importance of Tumor Genotype. Journal of the National Cancer Institute 2017. PubMed
  • Bouillez A, Adeegbe D, Jin C, Hu X, Tagde A, Alam M, Rajabi H, Wong KK, Kufe D. MUC1-C promotes the suppressive immune microenvironment in non-small cell lung cancer. Oncoimmunology 2017; 6:e1338998. PubMed
  • Mita MM, Mita AC, Moseley JL, Poon J, Small KA, Jou YM, Kirschmeier P, Zhang D, Zhu Y, Statkevich P, Sankhala KK, Sarantopoulos J, Cleary JM, Chirieac LR, Rodig SJ, Bannerji R, Shapiro GI. Phase 1 safety, pharmacokinetic and pharmacodynamic study of the cyclin-dependent kinase inhibitor dinaciclib administered every three weeks in patients with advanced malignancies. Br J Cancer 2017. PubMed
  • Rajabi H, Hiraki M, Tagde A, Alam M, Bouillez A, Christensen CL, Samur M, Wong KK, Kufe D. MUC1-C activates EZH2 expression and function in human cancer cells. Sci Rep 2017; 7:7481. PubMed
  • Pritz JR, Wachter F, Lee S, Luccarelli J, Wales TE, Cohen DT, Coote P, Heffron GJ, Engen JR, Massefski W, Walensky LD. Allosteric sensitization of proapoptotic BAX. Nat Chem Biol 2017; 13:961-967. PubMed
  • Ren JG, Seth P, Ye H, Guo K, Hanai JI, Husain Z, Sukhatme VP. Citrate Suppresses Tumor Growth in Multiple Models through Inhibition of Glycolysis, the Tricarboxylic Acid Cycle and the IGF-1R Pathway. Sci Rep 2017; 7:4537. PubMed
  • Winter GE, Mayer A, Buckley DL, Erb MA, Roderick JE, Vittori S, Reyes JM, di Iulio J, Souza A, Ott CJ, Roberts JM, Zeid R, Scott TG, Paulk J, Lachance K, Olson CM, Dastjerdi S, Bauer S, Lin CY, Gray NS, Kelliher MA, Churchman LS, Bradner JE. BET Bromodomain Proteins Function as Master Transcription Elongation Factors Independent of CDK9 Recruitment. Mol Cell 2017. PubMed
  • Johnson SF, Cruz C, Greifenberg AK, Dust S, Stover DG, Chi D, Primack B, Cao S, Bernhardy AJ, Coulson R, Lazaro JB, Kochupurakkal B, Sun H, Unitt C, Moreau LA, Sarosiek KA, Scaltriti M, Juric D, Baselga J, Richardson AL, Rodig SJ, D'Andrea AD, Balmaña J, Johnson N, Geyer M, Serra V, Lim E, Shapiro GI. CDK12 Inhibition Reverses De Novo and Acquired PARP Inhibitor Resistance in BRCA Wild-Type and Mutated Models of Triple-Negative Breast Cancer. Cell Rep 2016; 17:2367-2381. PubMed
  • Zhu AX, Baron AD, Malfertheiner P, Kudo M, Kawazoe S, Pezet D, Weissinger F, Brandi G, Barone CA, Okusaka T, Wada Y, Park JO, Ryoo BY, Cho JY, Chung HC, Li CP, Yen CJ, Lee KD, Chang SC, Yang L, Abada PB, Chau I. Ramucirumab as Second-Line Treatment in Patients With Advanced Hepatocellular Carcinoma: Analysis of REACH Trial Results by Child-Pugh Score. JAMA Oncol 2016. PubMed
  • Chen B, Zheng B, DeRan M, Jarugumilli GK, Fu J, Brooks YS, Wu X. ZDHHC7-mediated S-palmitoylation of Scribble regulates cell polarity. Nat Chem Biol 2016. PubMed
  • Lee S, Wales TE, Escudero S, Cohen DT, Luccarelli J, Gallagher CG, Cohen NA, Huhn AJ, Bird GH, Engen JR, Walensky LD. Allosteric inhibition of antiapoptotic MCL-1. Nat Struct Mol Biol 2016; 23:600-7. PubMed
  • Hiraki M, Suzuki Y, Alam M, Hinohara K, Hasegawa M, Jin C, Kharbanda S, Kufe D. MUC1-C Stabilizes MCL-1 in the Oxidative Stress Response of Triple-Negative Breast Cancer Cells to BCL-2 Inhibitors. Sci Rep 2016; 6:26643. PubMed
  • Kantar RS, Lashgari G, Tabet EI, Lewandrowski GK, Carvalho LA, Tannous BA. Imaging Tumor Vascularity and Response to Anti-Angiogenic Therapy Using Gaussia Luciferase. Sci Rep 2016; 6:26353. PubMed
  • Gao Y, Shen JK, Choy E, Zhang Z, Mankin HJ, Hornicek FJ, Duan Z. Pharmacokinetics and tolerability of NSC23925b, a novel P-glycoprotein inhibitor: preclinical study in mice and rats. Sci Rep 2016; 6:25659. PubMed
  • Shen JK, Cote GM, Gao Y, Choy E, Mankin HJ, Hornicek FJ, Duan Z. Targeting EZH2-mediated methylation of H3K27 inhibits proliferation and migration of Synovial Sarcoma in vitro. Sci Rep 2016; 6:25239. PubMed
  • Choi YE, Meghani K, Brault ME, Leclerc L, He YJ, Day TA, Elias KM, Drapkin R, Weinstock DM, Dao F, Shih KK, Matulonis U, Levine DA, Konstantinopoulos PA, Chowdhury D. Platinum and PARP Inhibitor Resistance Due to Overexpression of MicroRNA-622 in BRCA1-Mutant Ovarian Cancer. Cell Rep 2016; 14:429-39. PubMed
  • Richardson PG, Jagannath S, Moreau P, Jakubowiak AJ, Raab MS, Facon T, Vij R, White D, Reece DE, Benboubker L, Zonder J, Tsao LC, Anderson KC, Bleickardt E, Singhal AK, Lonial S, . Elotuzumab in combination with lenalidomide and dexamethasone in patients with relapsed multiple myeloma: final phase 2 results from the randomised, open-label, phase 1b-2 dose-escalation study. Lancet Haematol 2015; 2:e516-27. PubMed
  • Askoxylakis V, Ferraro GB, Kodack DP, Badeaux M, Shankaraiah RC, Seano G, Kloepper J, Vardam T, Martin JD, Naxerova K, Bezwada D, Qi X, Selig MK, Brachtel E, Duda DG, Huang P, Fukumura D, Engelman JA, Jain RK. Preclinical Efficacy of Ado-trastuzumab Emtansine in the Brain Microenvironment. Journal of the National Cancer Institute 2016. PubMed
  • Winter GE, Buckley DL, Paulk J, Roberts JM, Souza A, Dhe-Paganon S, Bradner JE. DRUG DEVELOPMENT. Phthalimide conjugation as a strategy for in vivo target protein degradation. Science 2015; 348:1376-81. PubMed
  • Raina D, Uchida Y, Kharbanda A, Rajabi H, Panchamoorthy G, Jin C, Kharbanda S, Scaltriti M, Baselga J, Kufe D. Targeting the MUC1-C oncoprotein downregulates HER2 activation and abrogates trastuzumab resistance in breast cancer cells. Oncogene 2014. PubMed
  • Cottini F, Hideshima T, Xu C, Sattler M, Dori M, Agnelli L, ten Hacken E, Bertilaccio MT, Antonini E, Neri A, Ponzoni M, Marcatti M, Richardson PG, Carrasco R, Kimmelman AC, Wong KK, Caligaris-Cappio F, Blandino G, Kuehl WM, Anderson KC, Tonon G. Rescue of Hippo coactivator YAP1 triggers DNA damage-induced apoptosis in hematological cancers. Nat Med 2014; 20:599-606. PubMed
  • Yin L, Kufe T, Avigan D, Kufe D. Targeting MUC1-C is synergistic with bortezomib in downregulating TIGAR and inducing ROS-mediated myeloma cell death. Blood 2014. PubMed
  • Rajabi H, Alam M, Takahashi H, Kharbanda A, Guha M, Ahmad R, Kufe D. MUC1-C oncoprotein activates the ZEB1/miR-200c regulatory loop and epithelial-mesenchymal transition. Oncogene 2014; 33:1680-9. PubMed
  • Chen Z, Akbay E, Mikse O, Tupper T, Cheng K, Wang Y, Tan X, Altabef A, Woo SA, Chen L, Reibel JB, Janne PA, Sharpless NE, Engelman JA, Shapiro GI, Kung AL, Wong KK. Co-clinical trials demonstrate superiority of crizotinib to chemotherapy in ALK-rearranged non-small cell lung cancer and predict strategies to overcome resistance. Clin Cancer Res 2014; 20:1204-11. PubMed
  • Bandopadhayay P, Bergthold G, Nguyen B, Schubert S, Gholamin S, Tang Y, Bolin S, Schumacher SE, Zeid R, Masoud S, Yu F, Vue N, Gibson WJ, Paolella BR, Mitra SS, Cheshier SH, Qi J, Liu KW, Wechsler-Reya R, Weiss WA, Swartling FJ, Kieran MW, Bradner JE, Beroukhim R, Cho YJ. BET bromodomain inhibition of MYC-amplified medulloblastoma. Clin Cancer Res 2014; 20:912-25. PubMed
  • Lu G, Middleton RE, Sun H, Naniong M, Ott CJ, Mitsiades CS, Wong KK, Bradner JE, Kaelin WG. The myeloma drug lenalidomide promotes the cereblon-dependent destruction of Ikaros proteins. Science 2014; 343:305-9. PubMed
  • Bolli N, Avet-Loiseau H, Wedge DC, Van Loo P, Alexandrov LB, Martincorena I, Dawson KJ, Iorio F, Nik-Zainal S, Bignell GR, Hinton JW, Li Y, Tubio JM, McLaren S, O' Meara S, Butler AP, Teague JW, Mudie L, Anderson E, Rashid N, Tai YT, Shammas MA, Sperling AS, Fulciniti M, Richardson PG, Parmigiani G, Magrangeas F, Minvielle S, Moreau P, Attal M, Facon T, Futreal PA, Anderson KC, Campbell PJ, Munshi NC. Heterogeneity of genomic evolution and mutational profiles in multiple myeloma. Nat Commun 2014; 5:2997. PubMed
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